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Quantitative correlation between counterion-affinity to cationic micelles and counterion-induced micellar growth

Yusof NS, Khan MN

Adv Colloid Interface Sci, 2013 Jun;193-194:12-23.
PMID: 23582713 DOI: 10.1016/j.cis.2013.03.002

The fascinating and serendipitous discovery, in 1976, of the characteristic viscoelastic behavior of wormlike micelles of cetyltrimethylammonium salicylate (CTASa) surfactant solution at ~2×10(-4) M CTASa became a catalyst for an increasing interest in both industrial application and mechanism of the origin of micellar growth of this and related wormlike micellar systems. It has been perceived for more than three decades, based upon qualitative evidence, that the extent of the strength of the counterion (X) binding to ionic micelles determines the counterion-induced micellar structural transition from spherical-to-small rodlike-to-linear long stiff/flexible rodlike/wormlike-to-entangled wormlike micelles. This perception predicts the presence of a possible quantitative correlation of counterionic micellar binding constants (KX) with counterion-induced micellar growth. The quantitative estimation of counterion binding affinity to cationic micelles, in terms of the values of the degree of counterion binding (βX), is concluded to be either inefficient or unreliable for moderately hydrophobic counterions (such as substituted benzoate ions). The values of KX, measured in terms of conventional ion exchange constants (KX(Y)), can provide a quantitative correlation between KX or KX(Y) (with a reference counterion Y=Cl(-) or Br(-)) and counterion-induced ionic micellar growth. A recent new semi-empirical kinetic (SEK) method provides the estimation of KX(Y) for Y=Br as well as ratio of counterionic micellar binding constants KX/KBr (= RX(Br)) where the values of KBr and KX have been derived from the kinetic parameters in the presence of cationic spherical and nonspherical micelles, respectively. The SEK method has been used to determine the values of KX(Br) or RX(Br) for X=2-, 3- and 4-ClC6H4CO2(-). Rheometric measurements on aqueous CTABr/MX (MX=2-,3- and 4-ClBzNa) solutions containing 0.015 M CTABr and varying values of [MX] reveal the presence of spherical micelles for MX=2-ClBzNa and long linear as well as entangled wormlike micelles for MX=3- and 4-ClBzNa. The respective values of KX(Br) or RX(Br) of 5.7, 50 and 48 for X=2-, 3- and 4-ClBz(-) give a quantitative correlation with the rheometric measurements of the structural features of micelles of 0.015 M CTABr solutions containing 2-, 3- and 4 ClBzNa.
A new semi-empirical kinetic method for the determination of ion exchange constants for the counterions of cationic micelles

Khan MN

Adv Colloid Interface Sci, 2010 Sep 15;159(2):160-79.
PMID: 20673861 DOI: 10.1016/j.cis.2010.06.005

A new method, based upon semi-empirical kinetic approach, for the determination of ion exchange constant for ion exchange processes occurring between counterions at the cationic micellar surface is described in this review article. Basically, the method involves a reaction kinetic probe which gives observed pseudo-first-order rate constants (k(obs)) for a nucleophilic substitution reaction between the nonionic and anionic reactants (R and S) in the presence of a constant concentration of both reactants as well as cationic micelles and varying concentrations of an inert inorganic or organic salt (MX). The observed data (k(obs), versus [MX]) fit satisfactorily (in terms of residual errors) to an empirical equation which could be derived from an equation explaining the mechanism of the reaction of the kinetic probe in terms of pseudophase micellar (PM) model coupled with another empirical equation. This (another) empirical equation explains the effect of [MX] on cationic micellar binding constant (K(S)) of the anionic reactant (say S) and gives an empirical constant, K(X/S). The magnitude of K(X/S) is the measure of the ability of X(-) to expel S(-) from a cationic micellar pseudophase to the bulk aqueous phase through ion exchange X(-)/S(-). The values of K(X/S) and K(Y/S) (where Y(-) is another inert counterion) give the ion exchange constant, K(X)(Y) (=K(X)/K(Y) where K(X) and K(Y) represent cationic micellar binding constants of X(-) and Y(-), respectively). The suitability of this method is demonstrated by the use of three different reaction kinetic probes and various MX.
Tobacco consumption and illegal drug use among Bangladeshi males: association and determinants

Kabir MA, Goh KL, Khan MM

Am J Mens Health, 2013 Mar;7(2):128-37.
PMID: 23065136 DOI: 10.1177/1557988312462737

This article aimed to identify the determinants of tobacco consumption and illegal drug use (IDU) as well as to examine the association between these two variables using a representative sample of 3,771 Bangladeshi males aged 15 to 54 years. Data were collected through Bangladesh Demographic and Health Survey 2007. To identify the determinants, the patterns of tobacco consumption and IDU were analyzed by age, education and occupation, residence, mass media, premarital sex, wealth, and sexually transmitted infections (STIs). Prevalence of smoking cigarette and bidi was roughly 60%. However, the prevalence of IDU was 3.4%, and this proportion is statistically significant (Z = 11.32, p = .000). After bivariate analysis, almost all variables except STIs were significantly associated with tobacco consumption. Similarly, all variables except residence and mass media were associated with IDU. Based on multivariable adjusted logistic regression analysis, the likelihood of using IDU was approximately twofold (odds ratio [OR] = 1.8, 95% confidence interval [CI] = 1.23-2.53) among bidi smokers and fourfold (OR = 3.8, 95% CI = 2.62-5.56) among cigarette smokers as compared with nonsmokers.
Synthesis of enriched boron nitride nanocrystals: A potential element for biomedical applications

Ahmad P, Khandaker MU, Muhammad N, Rehman F, Ullah Z, Khan G, et al.

Appl Radiat Isot, 2020 Dec;166:109404.
PMID: 32956924 DOI: 10.1016/j.apradiso.2020.109404

The shortcomings in Boron neutron capture therapy (BNCT) and Hyperthermia for killing the tumor cell desired for the synthesis of a new kind of material suitable to be first used in BNCT and later on enable the conditions for Hyperthermia to destroy the tumor cell. The desire led to the synthesis of large band gap semiconductor nano-size Boron-10 enriched crystals of hexagonal boron nitride (10BNNCs). The contents of 10BNNCs are analyzed with the help of x-ray photoelectron spectroscopy (XPS) and counter checked with Raman and XRD. The 10B-contents in 10BNNCs produce 7Li and 4He nuclei. A Part of the 7Li and 4He particles released in the cell is allowed to kill the tumor (via BNCT) whereas the rest produce electron-hole pairs in the semiconductor layer of 10BNNCs suggested to work in Hyperthermia with an externally applied field.
Burden of Transport-Related Injuries in the Eastern Mediterranean Region: A Systematic Analysis for the Global Burden of Disease Study 2017

GBD 2017 EMR Transport Injuries Collaborators, Safiri S, Sullman MJM, Lajunen T, Hill T, Almasi-Hashiani A, et al.

Arch Iran Med, 2021 07 01;24(7):512-525.
PMID: 34488316 DOI: 10.34172/aim.2021.74

BACKGROUND: Transport-related injuries (TIs) are a substantial public health concern for all regions of the world. The present study quantified the burden of TIs and deaths in the Eastern Mediterranean region (EMR) in 2017 by sex and age.
METHODS: TIs and deaths were estimated by age, sex, country, and year using Cause of Death Ensemble modelling (CODEm) and DisMod-MR 2.1. Disability-adjusted life years (DALYs), which quantify the total burden of years lost due to premature death or disability, were also estimated per 100000 population. All estimates were reported along with their corresponding 95% uncertainty intervals (UIs).
RESULTS: In 2017, there were 5.5 million (UI 4.9-6.2) transport-related incident cases in the EMR - a substantial increase from 1990 (2.8 million; UI 2.5-3.1). The age-standardized incidence rate for the EMR in 2017 was 787 (UI 705.5-876.2) per 100000, which has not changed significantly since 1990 (-0.9%; UI -4.7 to 3). These rates differed remarkably between countries, such that Oman (1303.9; UI 1167.3-1441.5) and Palestine (486.5; UI 434.5-545.9) had the highest and lowest age-standardized incidence rates per 100000, respectively. In 2017, there were 185.3 thousand (UI 170.8-200.6) transport-related fatalities in the EMR - a substantial increase since 1990 (140.4 thousand; UI 118.7-156.9). The age-standardized death rate for the EMR in 2017 was 29.5 (UI 27.1-31.9) per 100000, which was 30.5% lower than that found in 1990 (42.5; UI 36.8-47.3). In 2017, Somalia (54; UI 30-77.4) and Lebanon (7.1; UI 4.8-8.6) had the highest and lowest age-standardized death rates per 100,000, respectively. The age-standardised DALY rate for the EMR in 2017 was 1,528.8 (UI 1412.5-1651.3) per 100000, which was 34.4% lower than that found in 1990 (2,331.3; UI 1,993.1-2,589.9). In 2017, the highest DALY rate was found in Pakistan (3454121; UI 2297890- 4342908) and the lowest was found in Bahrain (8616; UI 7670-9751).
CONCLUSION: The present study shows that while road traffic has become relatively safer (measured by deaths and DALYs per 100000 population), the number of transport-related fatalities in the EMR is growing and needs to be addressed urgently.
Safe delivery practices: experience from cross-sectional data of Bangladeshi women

Kabir MA, Goh KL, Khan MM, Al-Amin AQ, Azam MN

Asia Pac J Public Health, 2015 Mar;27(2):NP1170-81.
PMID: 22426560 DOI: 10.1177/1010539512437401

This study examines the safe delivery practices of Bangladeshi women using data on 4905 ever-married women aged 15 to 49 years from the 2007 Bangladesh Demographic and Health Survey. Variables that included age, region of origin, education level of respondent and spouse, residence, working status, religion, involvement in NGOs, mass media exposure, and wealth index were analyzed to find correlates of safe delivery practices. More than 80% of the deliveries took place at home, and only 18% were under safe and hygienic conditions. The likelihood of safe deliveries was significantly lower among younger and older mothers than middle-aged mothers and higher among educated mothers and those living in urban areas. Economically better-off mothers and those with greater exposure to mass media had a significantly higher incidence of safe delivery practices. A significant association with religion and safe delivery practices was revealed. Demographic, socioeconomic, cultural, and programmatic factors that are strongly associated with safe delivery practices should be considered in the formulation of reproductive health policy.
Adolescent tobacco use and its determinants: evidence from Global Youth Tobacco Survey, Bangladesh 2007

Kabir MA, Goh KL, Khan MM

Asia Pac J Public Health, 2015 Mar;27(2):NP1578-90.
PMID: 23359868 DOI: 10.1177/1010539512472357

Adolescent tobacco use (ATU) is on the rise worldwide and the problem is particularly severe in developing countries. Based on nationally representative data, this study aims to investigate the association between ATU and its possible correlates for Bangladesh, where the prevalence rate of ATU is high. The data set is extracted from the Global Youth Tobacco Survey for Bangladesh conducted in 2007. The survey collected information from a total of 3113 students from 52 schools, with a response rate of 100% at the school level, while a response rate of 88.9% was achieved from the students. Students covered in the survey were in grades 7, 8, 9, and 10, with age ranging from 11 to 17 years. The prevalence rate of ATU at the time of the survey was 8.4%, while 35.6% of the students had used at least a type of tobacco products before. Logistic regressions were used to obtain the odds ratios (ORs) in favor of ATU for each of the possible determinants and the confidence intervals (CIs) of these ratios. Use of tobacco among friends (OR = 3.46; CI = 2.37-5.05), the experience of seeing others smoking at home (OR = 2.10; CI = 1.36-3.22) or other places (OR = 1.6; CI = 1.02-2.57), receiving pocket money (OR = 7.6; CI = 4.59-13.28), receiving free tobacco from vendors (OR = 2.3; CI = 1.44-3.78), and exposure to advertisements and promotions of tobacco products (OR = 1.83; CI = 1.23-2.79) were associated with a higher likelihood of ATU. Increased awareness of health hazards of tobacco use through education in schools helped mitigate the problem of ATU. The findings of this study have ramifications for tobacco control prevention strategies in Bangladesh.
Fulltext Clinical use of mood stabilizers beyond treatment for bipolar disorder: The REAP-MS study

Chen CK, Yang SY, Park SC, Jang OJ, Zhu X, Xiang YT, et al.

Asian J Psychiatr, 2023 Jul;85:103613.
PMID: 37163943 DOI: 10.1016/j.ajp.2023.103613

OBJECTIVE: Mood stabilizers are psychotropic drugs mainly used to treat bipolar disorder in the acute phase or for maintenance therapy to prevent relapse. In clinical practice, mood stabilizers are commonly prescribed for conditions other than bipolar disorder. This study investigated the distribution of mood stabilizer prescriptions for different psychiatric diagnoses and studied differences in the drugs, dosage, and plasma concentration in 10 Asian countries including Taiwan, South Korea, Malaysia, China, Thailand, India, Pakistan, Singapore, Indonesia, and Myanmar.
METHODS: Patients prescribed mood stabilizers (lithium, carbamazepine, valproic acid, or lamotrigine) for a psychiatric condition other than bipolar disorder (codes F31.0-F31.9 in the International Classification of Diseases, 10th Edition, Clinical Modification) were recruited through convenience sampling. A website-based data entry system was used for data collection.
RESULTS: In total, 1557 psychiatric patients were enrolled. Schizophrenia, schizotypal, delusional, and other non-mood psychotic disorders (F20-F29, 55.8 %) was the most common diagnosis, followed by non-bipolar mood disorders (F30, F31- F39, 25.3 %), organic mental disorder (F00-F09, 8.8 %), mental retardation (F70-F79, 5.8 %) and anxiety, dissociative, stress-related, somatoform and other nonpsychotic mental disorders (F40-F48, 4.4 %). The most frequently targeted symptoms (>20 %) were irritability (48 %), impulsivity (32.4 %), aggression (29.2 %), anger (20.8 %), and psychosis (24.1 %). Valproic acid was the most frequently used medication.
CONCLUSIONS: Clinicians typically prescribe mood stabilizers as empirically supported treatment to manage mood symptoms in patients with diagnoses other than bipolar disorders, though there is on official indication for these disorders. The costs and benefits of this add-on symptomatic treatment warrant further investigation.
Corrigendum to "Clinical use of mood stabilizers beyond treatment for bipolar disorder: The REAP-MS study" [Asian J. Psychiatry 85 (2023) 103613]

Chen CK, Yang SY, Park SC, Jang OJ, Zhu X, Xiang YT, et al.

Asian J Psychiatr, 2023 Nov;89:103650.
PMID: 37308390 DOI: 10.1016/j.ajp.2023.103650
The effect of losartan and carvedilol on vasopressor responses to adrenergic agonists and angiotensin II in the systemic circulation of Sprague Dawley rats

Abdulla MH, Sattar MA, Abdullah NA, Khan MA, Anand Swarup KR, Johns EJ

Auton Autacoid Pharmacol, 2011 Jan-Apr;31(1-2):13-20.
PMID: 21166975 DOI: 10.1111/j.1474-8673.2010.00461.x

1 Interaction between renin-angiotensin (RAS) and sympathetic nervous systems (SNS) was investigated by examining the effect of cumulative blockade of angiotensin II (Ang II) and adrenergic receptors in normal Sprague Dawley rats. 2 Rats were treated with losartan (10 mg/kg), carvedilol (5 mg/kg), or losartan plus carvedilol (10+5 mg/kg) orally for 7 days. On day 8, the animals were anaesthetized with pentobarbitone and prepared for systemic haemodynamic study. Dose-response relationships for the elevation of mean arterial pressure or change in heart rate (HR) in response to intravenous injections of noradrenaline (NA), phenylephrine (PE), methoxamine (ME) and Ang II were determined. 3 Losartan or the combination of losartan with carvedilol blunted vasopressor responses to ME and Ang II. Dose-response relationships for agonist action on HR were significantly inhibited by all treatments except for the combination of losartan and carvedilol on the decrease in HR induced by PE. Carvedilol decreased vasopressor responses to NA, PE and Ang II, and HR responses to NA, ME and Ang II. Combination treatment produced similar effects to losartan on the vasopressor and HR responses but had a greater effect on vasopressor responses to ME and Ang II, and on HR responses to NA and Ang II than carvedilol alone. 4 It is concluded that peripheral vasoconstriction induced by Ang II is partly mediated by adrenergic action and that the vasopressor responses to adrenergic agonists depend on an intact RAS. These observations suggest an interactive relationship between RAS and SNS in determining systemic haemodynamic responses in 'normal' rats.
Fulltext Anti-diabetic potential of Catharanthus roseus Linn. and its effect on the glucose transport gene (GLUT-2 and GLUT-4) in streptozotocin induced diabetic wistar rats

Al-Shaqha WM, Khan M, Salam N, Azzi A, Chaudhary AA

BMC Complement Altern Med, 2015;15:379.
PMID: 26490765 DOI: 10.1186/s12906-015-0899-6

Catharanthus roseus is an important Ayurvedic medication in traditional medicine. It is potentially used in countries like India, South Africa, China and Malaysia for the healing of diabetes mellitus. Although, the molecular mechanisms behind this effect are yet to be exclusively explored. Due to the great antidiabetic and hyperlipidemic potential of c. roseus, we hypothesized that the insulin mimetic effect of ethanolic extract of c. roseus might add to glucose uptake through improvement in the expression of genes of the glucose transporter (GLUT) family messenger RNA (mRNA) in liver.
Chromosome-level genome sequence of the Genetically Improved Farmed Tilapia (GIFT, Oreochromis niloticus) highlights regions of introgression with O. mossambicus

Etherington GJ, Nash W, Ciezarek A, Mehta TK, Barria A, Peñaloza C, et al.

BMC Genomics, 2022 Dec 15;23(1):832.
PMID: 36522771 DOI: 10.1186/s12864-022-09065-8

BACKGROUND: The Nile tilapia (Oreochromis niloticus) is the third most important freshwater fish for aquaculture. Its success is directly linked to continuous breeding efforts focusing on production traits such as growth rate and weight. Among those elite strains, the Genetically Improved Farmed Tilapia (GIFT) programme initiated by WorldFish is now distributed worldwide. To accelerate the development of the GIFT strain through genomic selection, a high-quality reference genome is necessary.
RESULTS: Using a combination of short (10X Genomics) and long read (PacBio HiFi, PacBio CLR) sequencing and a genetic map for the GIFT strain, we generated a chromosome level genome assembly for the GIFT. Using genomes of two closely related species (O. mossambicus, O. aureus), we characterised the extent of introgression between these species and O. niloticus that has occurred during the breeding process. Over 11 Mb of O. mossambicus genomic material could be identified within the GIFT genome, including genes associated with immunity but also with traits of interest such as growth rate.
CONCLUSION: Because of the breeding history of elite strains, current reference genomes might not be the most suitable to support further studies into the GIFT strain. We generated a chromosome level assembly of the GIFT strain, characterising its mixed origins, and the potential contributions of introgressed regions to selected traits.
Fulltext Micro computed tomography (Micro-CT) characterization of root and root canal morphology of mandibular first premolars: a systematic review and meta-analysis

Karobari MI, Batul R, Khan M, Patil SR, Basheer SN, Rezallah NNF, et al.

BMC Oral Health, 2024 Jan 02;24(1):1.
PMID: 38167114 DOI: 10.1186/s12903-023-03624-5

INTRODUCTION: Mandibular first premolars are familiar with their varied root canal morphology, causing difficulties and challenges for successful endodontic procedures. This systematic review and meta-analysis aim to study the characterization of root and canal morphology of the first mandibular premolar using micro-computed tomography.
METHODOLOGY: The literature search was conducted using electronic web databases like PubMed, Scopus, ScienceDirect and Cochrane with the chosen MeSH key words and data was retrieved until May 2023. Further to perform the statistical analysis, R v 4.3.1 software with "meta", 'metafor" "metaviz" " ggplot2" package was used, and results were represented by odds ratios (OR) and the percentage of forest plots along a 95 per cent confidence interval (CI).
RESULTS: The total number of studies meeting the inclusion criteria was 13; these studies were conducted on mandibular first premolar using Micro-CT; the total sample size was 1817. To scan the sample, an X-ray micro-focus CT system (Siemens Inveon CT, Erlangen, Germany) was used in four studies and seven different machines were used in the respective studies. Mimics 10.01 software (Materialize, Leuven, Belgium) and NRecon v.1.6.9 software (Bruker, Kontich, Belgium) were commonly operated. The minimum and maximum voxel size ranges between 11.94 and 50 μm. Vertucci's classification was frequently used (9), while one study applied Ahmed et al. and Vertucci's classification.
CONCLUSION: This systematic review provides essential information about the root and canal configurations, radicular grooves, accessory canals, and apical foramina through Micro-CT, aiming to improve the accuracy of endodontic treatment and help practitioners.
Fulltext Teledentistry as a Supportive Tool for Dentists in Pakistan

Subhan R, Ismail WA, Musharraf S, Khan M, Hafeez R, Alam MK

Biomed Res Int, 2021;2021:8757859.
PMID: 34540998 DOI: 10.1155/2021/8757859

The current scenario of the COVID-19 pandemic has forced dentists to seek different options for delivering healthcare services other than the in-person direct examination in clinical practice. Teledentistry is one of the options for remote patient care and monitoring. Objective. The present survey was conducted to assess the knowledge and perception of the dentists in Pakistan regarding teledentistry as an emergent supportive tool. Materials and Methods. A self-administered, close-ended, and prevalidated survey questionnaire was used, comprising 21 questions, and distributed electronically via e-mail, WhatsApp, and Facebook Messenger to evaluate the knowledge and perception of dentists regarding teledentistry. The data collected was compiled in a systematic manner and analyzed in terms of frequency (yes/no). Results. Out of a total of 350 dentists, 325 responded to the questionnaire, and it was seen that 62.5% of them did not have knowledge about teledentistry prior to COVID-19. 65.8% of dentists considered the practice of teledentistry in nonpandemic situations in the future. Conclusion. In the present study, it was observed that most of the dental professionals had inadequate knowledge about teledentistry before COVID-19, but the awareness and perception regarding teledentistry were currently satisfactory among the dental professionals in Pakistan. This emerging trend gives a positive hope for the implementation of teledentistry in the healthcare setup of Pakistan in the near future, as it will prove to be beneficial for safe dental practice during times of pandemic and even after.
Synthesis and structure-activity relationship of thiobarbituric acid derivatives as potent inhibitors of urease

Khan KM, Rahim F, Khan A, Shabeer M, Hussain S, Rehman W, et al.

Bioorg Med Chem, 2014 Aug 1;22(15):4119-23.
PMID: 24986232 DOI: 10.1016/j.bmc.2014.05.057

A series of thiobarbituric acid derivatives 1-27 were synthesized and evaluated for their urease inhibitory potential. Exciting results were obtained from the screening of these compounds 1-27. Compounds 5, 7, 8, 11, 16, 17, 22, 23 and 24 showed excellent urease inhibition with IC50 values 18.1 ± 0.52, 16.0 ± 0.45, 16.0 ± 0.22, 14.3 ± 0.27, 6.7 ± 0.27, 10.6 ± 0.17, 19.2 ± 0.29, 18.2 ± 0.76 and 1.61 ± 0.18 μM, respectively, much better than the standard urease inhibitor thiourea (IC₅₀=21 ± 0.11 μM). Compound 3, 4, 10, and 26 exhibited comparable activities to the standard with IC₅₀ values 21.4 ± 1.04 and 21.5 ± 0.61 μM, 22.8 ± 0.32, 25.2 ± 0.63, respectively. However the remaining compounds also showed prominent inhibitory potential The structure-activity relationship was established for these compounds. This study identified a novel class of urease inhibitors. The structures of all compounds were confirmed through spectroscopic techniques such as EI-MS and (1)H NMR.
Evaluation of bisindole as potent β-glucuronidase inhibitors: synthesis and in silico based studies

Khan KM, Rahim F, Wadood A, Taha M, Khan M, Naureen S, et al.

Bioorg Med Chem Lett, 2014 Apr 1;24(7):1825-9.
PMID: 24602903 DOI: 10.1016/j.bmcl.2014.02.015

Bisindole analogs 1-17 were synthesized and evaluated for their in vitro β-glucuronidase inhibitory potential. Out of seventeen compounds, the analog 1 (IC50=1.62±0.04 μM), 6 (IC50=1.86±0.05 μM), 10 (IC50=2.80±0.29 μM), 9 (IC50=3.10±0.28 μM), 14 (IC50=4.30±0.08 μM), 2 (IC50=18.40±0.09 μM), 19 (IC50=19.90±1.05 μM), 4 (IC50=20.90±0.62 μM), 7 (IC50=21.50±0.77 μM), and 3 (IC50=22.30±0.02 μM) showed superior β-glucuronidase inhibitory activity than the standard (d-saccharic acid 1,4-lactone, IC50=48.40±1.25 μM). In addition, molecular docking studies were performed to investigate the binding interactions of bisindole derivatives with the enzyme. This study has identified a new class of potent β-glucouronidase inhibitors.
Kinetics and mechanism of large rate enhancement in an acidic aqueous cleavage of the tertiary amide bond of N-(2-methoxyphenyl)-N'-morpholinophthalamide (1)

Sim YL, Ariffin A, Khan MN

Bioorg Chem, 2008 Aug;36(4):178-82.
PMID: 18440044 DOI: 10.1016/j.bioorg.2008.03.003

The rate of conversion of 1 to N-(2-methoxyphenyl)phthalimide (2) within [HCl] range 5.0x10(-3)-1.0 M at 1.0M ionic strength (by NaCl) reveals the presence of both uncatalyzed and specific acid-catalyzed kinetic terms in the rate law. Intramolecular carboxamide group-assisted cleavage of amide bond of 1 reveals rate enhancement of much larger than 10(6)-fold compared to the expected rate of analogous intermolecular reaction.
Flurbiprofen derivatives as novel α-amylase inhibitors: Biology-oriented drug synthesis (BIODS), in vitro, and in silico evaluation

Khan M, Alam A, Khan KM, Salar U, Chigurupati S, Wadood A, et al.

Bioorg Chem, 2018 12;81:157-167.
PMID: 30125730 DOI: 10.1016/j.bioorg.2018.07.038

Novel derivatives of flurbiprofen 1-18 including flurbiprofen hydrazide 1, substituted aroyl hydrazides 2-9, 2-mercapto oxadiazole derivative 10, phenacyl substituted 2-mercapto oxadiazole derivatives 11-15, and benzyl substituted 2-mercapto oxadiazole derivatives 16-18 were synthesized and characterized by EI-MS, 1H and 13C NMR spectroscopic techniques. All derivatives 1-18 were screened for α-amylase inhibitory activity and demonstrated a varying degree of potential ranging from IC50 = 1.04 ± 0.3 to 2.41 ± 0.09 µM as compared to the standard acarbose (IC50 = 0.9 ± 0.04 µM). Out of eighteen compounds, derivatives 2 (IC50 = 1.69 ± 0.1 µM), 3 (IC50 = 1.04 ± 0.3 µM), 9 (IC50 = 1.25 ± 1.05 µM), and 13 (IC50 = 1.6 ± 0.18 µM) found to be excellent inhibitors while rest of the compounds demonstrated comparable inhibition potential. A limited structure-activity relationship (SAR) was established by looking at the varying structural features of the library. In addition to that, in silico study was conducted to understand the binding interactions of the compounds (ligands) with the active site of α-amylase enzyme.
Deep eutectic solvent mediated synthesis of 3,4-dihydropyrimidin-2(1H)-ones and evaluation of biological activities targeting neurodegenerative disorders

Saleem Khan M, Asif Nawaz M, Jalil S, Rashid F, Hameed A, Asari A, et al.

Bioorg Chem, 2022 01;118:105457.
PMID: 34798458 DOI: 10.1016/j.bioorg.2021.105457

Substitution of hazardous and often harmful organic solvents with "green" and "sustainable" alternative reaction media is always desirous. Ionic liquids (IL) have emerged as valuable and versatile liquids that can replace most organic solvents in a variety of syntheses. However, recently new types of low melting mixtures termed as Deep Eutectic Solvents (DES) have been utilized in organic syntheses. DES are non-volatile in nature, have sufficient thermal stability, and also have the ability to be recycled and reused. Hence DES have been used as alternative reaction media to perform different organic reactions. The availability of green, inexpensive and easy to handle alternative solvents for organic synthesis is still scarce, hence our interest in DES mediated syntheses. Herein we have investigated Biginelli reaction in different DES for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones. Monoamine oxidases and cholinesterases are important drug targets for the treatment of various neurological disorders such as Alzheimer's disease, Parkinson's disease, depression and anxiety. The compounds synthesized herein were evaluated for their inhibitory potential against these enzymes. Some of the compounds were found to be highly potent and selective inhibitors. Compounds 1 h and 1c were the most active monoamine oxidase A (MAO A) (IC50 = 0.31 ± 0.11 µM) and monoamine oxidase B (MAO B) (IC50 = 0.34 ± 0.04 µM) inhibitors respectively. All compounds were selective AChE inhibitors and did not inhibit BChE (<29% inhibition). Compound 1 k (IC50 = 0.13 ± 0.09 µM) was the most active AChE inhibitor.
Fulltext Influence of combined hypertension and renal failure on functional alpha(1)-adrenoceptor subtypes in the rat kidney

Hye Khan MA, Sattar MA, Abdullah NA, Johns EJ

Br J Pharmacol, 2008 Mar;153(6):1232-41.
PMID: 18246093 DOI: 10.1038/bjp.2008.13

This study investigated whether the alpha(1)-adrenoceptor responsiveness of the renal vasculature was altered in the state of hypertension combined with renal failure.

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