Displaying publications 1 - 20 of 69 in total

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  1. Beh ZY, Hasan MS
    J Vasc Access, 2017 Sep 11;18(5):e57-e61.
    PMID: 28478621 DOI: 10.5301/jva.5000720
    INTRODUCTION: We report the use of a newly described regional technique, ultrasound-guided costoclavicular approach infraclavicular brachial plexus block for surgical anesthesia in two high-risk patients undergoing 2nd stage transposition of basilic vein fistula.

    METHODS: Both patients had features of difficult airway, American Society of Anesthesiologists (ASA) physical status class III and central venous occlusive disease. The common approach, i.e., ultrasound-guided supraclavicular brachial plexus block was technically difficult with inherent risk of vascular puncture due to dilated venous collaterals at the supraclavicular area possibly compromising block quality. The risk of general anesthesia (GA) was significant as patients were morbidly obese with possible risk of obstructive sleep apnea postoperatively. As an alternative, we performed the ultrasound-guided costoclavicular approach infraclavicular brachial plexus block with 20 mL local anesthetic (LA) ropivacaine 0.5% delivered at the identified costoclavicular space using in-plane needling technique. Another 10 mL of LA was infiltrated along the subcutaneous fascia of the proximal medial aspect of arm.

    RESULTS: Both surgeries of >2 hours' duration were successful, without the need of further local infiltration at surgical site or conversion to GA.

    CONCLUSIONS: Ultrasound-guided costoclavicular approach can be an alternative way of providing effective analgesia and safe anesthesia for vascular access surgery of the upper limb.

    Matched MeSH terms: Amides/administration & dosage*; Amides/adverse effects
  2. Mageswaran R, Choy YC
    Med J Malaysia, 2010 Dec;65(4):300-3.
    PMID: 21901950
    A prospective randomized double-blind study was conducted which involved, 60 ASA 1-2, aged 18-65 years patients, who had elective or emergency orthopaedic surgeries of the upper limbs. They were randomly divided into two groups: Group I received 30 mls of 0.5% ropivacaine; and Group II received 0.5% levobupivacaine for infraclavicular brachial plexus block based on the coracoid approach. The onset time required for sensory block of all required dermatomes (C5-T1) and the onset time of motor block were documented. Based on the Visual Analogue Score, pain scores were recorded every 30 minutes during surgery and at the 6th hour. The mean onset time (SD) for sensory block with ropivacaine was 13.5 +/- 2.9 minutes compared to levobupivacaine at 11.1 +/- 2.6 minutes (p = 0.003). The onset time for motor block was 19.0 +/- 2.7 minutes in Group I compared to 17.1 +/- 2.6 minutes (p = 0.013) in Group II. Patients in both groups experienced both mild to moderate pain at the 6th hour. In conclusion, there were statistically significant differences in the onset-time for sensory and motor block. However, there was no statistically significant difference in terms of effectiveness of analgesia at the 6th hour. Although the clinical advantage of levobupivacine is not substantial, its safety profile becomes a major consideration in the choice of local anaesthetic for brachial plexus block where a large volume is required for an effective result.
    Matched MeSH terms: Amides/pharmacology*
  3. Korula P, Alexander H, John JS, Kirubakaran R, Singh B, Tharyan P, et al.
    Cochrane Database Syst Rev, 2024 Feb 05;2(2):CD015219.
    PMID: 38314855 DOI: 10.1002/14651858.CD015219.pub2
    BACKGROUND: The coronavirus disease 2019 (COVID-19) pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) continues to challenge the health workforce and societies worldwide. Favipiravir was suggested by some experts to be effective and safe to use in COVID-19. Although this drug has been evaluated in randomized controlled trials (RCTs), it is still unclear if it has a definite role in the treatment of COVID-19.

    OBJECTIVES: To assess the effects of favipiravir compared to no treatment, supportive treatment, or other experimental antiviral treatment in people with acute COVID-19.

    SEARCH METHODS: We searched the Cochrane COVID-19 Study Register, MEDLINE, Embase, the World Health Organization (WHO) COVID-19 Global literature on coronavirus disease, and three other databases, up to 18 July 2023.

    SELECTION CRITERIA: We searched for RCTs evaluating the efficacy of favipiravir in treating people with COVID-19.

    DATA COLLECTION AND ANALYSIS: We used standard Cochrane methodological procedures for data collection and analysis. We used the GRADE approach to assess the certainty of evidence for each outcome.

    MAIN RESULTS: We included 25 trials that randomized 5750 adults (most under 60 years of age). The trials were conducted in Bahrain, Brazil, China, India, Iran, Kuwait, Malaysia, Mexico, Russia, Saudi Arabia, Thailand, the UK, and the USA. Most participants were hospitalized with mild to moderate disease (89%). Twenty-two of the 25 trials investigated the role of favipiravir compared to placebo or standard of care, whilst lopinavir/ritonavir was the comparator in two trials, and umifenovir in one trial. Most trials (24 of 25) initiated favipiravir at 1600 mg or 1800 mg twice daily for the first day, followed by 600 mg to 800 mg twice a day. The duration of treatment varied from five to 14 days. We do not know whether favipiravir reduces all-cause mortality at 28 to 30 days, or in-hospital (risk ratio (RR) 0.84, 95% confidence interval (CI) 0.49 to 1.46; 11 trials, 3459 participants; very low-certainty evidence). We do not know if favipiravir reduces the progression to invasive mechanical ventilation (RR 0.86, 95% CI 0.68 to 1.09; 8 trials, 1383 participants; very low-certainty evidence). Favipiravir may make little to no difference in the need for admission to hospital (if ambulatory) (RR 1.04, 95% CI 0.44 to 2.46; 4 trials, 670 participants; low-certainty evidence). We do not know if favipiravir reduces the time to clinical improvement (defined as time to a 2-point reduction in patients' admission status on the WHO's ordinal scale) (hazard ratio (HR) 1.13, 95% CI 0.69 to 1.83; 4 trials, 721 participants; very low-certainty evidence). Favipiravir may make little to no difference to the progression to oxygen therapy (RR 1.20, 95% CI 0.83 to 1.75; 2 trials, 543 participants; low-certainty evidence). Favipiravir may lead to an overall increased incidence of adverse events (RR 1.27, 95% CI 1.05 to 1.54; 18 trials, 4699 participants; low-certainty evidence), but may result in little to no difference inserious adverse eventsattributable to the drug (RR 1.04, 95% CI 0.76 to 1.42; 12 trials, 3317 participants; low-certainty evidence).

    AUTHORS' CONCLUSIONS: The low- to very low-certainty evidence means that we do not know whether favipiravir is efficacious in people with COVID-19 illness, irrespective of severity or admission status. Treatment with favipiravir may result in an overall increase in the incidence of adverse events but may not result in serious adverse events.

    Matched MeSH terms: Amides/therapeutic use
  4. Liow CH, Sahrim Ahmad, Khairiah Badri
    In-situ polymerization method was used to prepare palm-based polyurethane (PU) composites loading with 15 wt% magnetite (Fe3O4), polyaniline (PANI) and Fe3O4 coated with PANI labeled as PU15, PP and PPM, respectively. FTIR spectroscopy analysis indicated a shift in the carbonyl, C=O and NH in PP. The shift of the peak indicated that there was hydrogen bonding between the C=O (proton acceptor) of urethane with NH (proton-donator) of PANI. PPM gave the highest impact and flexural strengths at 4875 kJ/ m2 and 42 MPa, respectively but with the lowest flexural modulus (1050 MPa). Two-stage degradation behavior was observed in the TGA thermogram.
    Matched MeSH terms: Amides
  5. Wun FML, Muhd Hafizi Zainal, Syahidah Mohd Tahir, Ishak B. Ahmad, Mohammad B. Kassim
    Sains Malaysiana, 2018;47:923-929.
    The presence of two different chromophores in benzothiazole molecule namely benzothiazole and aromatic rings lead to
    interesting chemical and biological properties that attract more researches on the compounds. Three new benzothiazolylbenzoythiourea
    compounds namely 1-(1,3-benzothiazol-2-yl)-3-(benzoylthiourea) (BBT), 1-(1,3-benzothiazol-2-yl)-3-
    (4-chlorobenzoylthiourea) (BBT-4Cl) and 1-(1,3-benzothiazol-2-yl)-3-(4-methoxybenzoylthiourea) (BBT-4OCH3
    ) with
    different electron withdrawing substituents (R) at the para positions on the benzene ring of benzoylthiourea ring have
    been synthesized from the reaction of R-benzoyl isothiocyanate (R= H, Cl, and OCH3
    ) and 2-aminobenzothiazole. The
    compounds were characterized by spectroscopic techniques (infrared, 1
    H proton NMR and UV-Vis). The IR spectra showed
    the frequency signals of n (C=O), n (C=S), n (N-H) at 1664-1673, 1238-1249 and 3031-3055 cm-1, respectively. The 1
    H
    proton NMR spectra showed the presence of N-H amine and amide signals in the region of (12.14-12.35) and (14.17-14.43)
    ppm, respectively. The proton signals of the two benzothiazole and benzoylthiourea moieties appear at 7.08-8.16 ppm.
    A theoretical study based on Density Functional Theory (DFT) and Time-Dependent (TD) DFT was conducted to optimize
    the geometrical structure and investigate the electronic properties of title compounds. The highest occupied molecular
    orbital (HOMO) was found on the benzothiazole moiety; while, the lowest-unoccupied molecular orbital (LUMO) was
    located at the benzoylthiourea fragment. The DFT optimized structures possessed an intramolecular hydrogen bonding
    and the types of para substituents used influenced the properties of hydrogen bonding.
    Matched MeSH terms: Amides
  6. Lim HJ, Hasan MS, Chinna K
    Rev Bras Anestesiol, 2016 Jul-Aug;66(4):341-5.
    PMID: 27155777 DOI: 10.1016/j.bjan.2016.04.006
    A high sodium concentration is known to antagonize local anesthetics when infiltrated around neural tissue. Thus, we hypothesized that the onset time for sensory and motor blockade, in supraclavicular brachial plexus block using ropivacaine diluted with dextrose would be shorter than with saline.
    Matched MeSH terms: Amides
  7. Fauzi MB, Rashidbenam Z, Bin Saim A, Binti Hj Idrus R
    Polymers (Basel), 2020 Nov 25;12(12).
    PMID: 33255581 DOI: 10.3390/polym12122784
    Three-dimensional (3D) in vitro skin models have been widely used for cosmeceutical and pharmaceutical applications aiming to reduce animal use in experiment. This study investigate capability of ovine tendon collagen type I (OTC-I) sponge suitable platform for a 3D in vitro skin model using co-cultured skin cells (CC) containing human epidermal keratinocytes (HEK) and human dermal fibroblasts (HDF) under submerged (SM) and air-liquid interface (ALI) conditions. Briefly, the extracted OTC-I was freeze-dried and crosslinked with genipin (OTC-I_GNP) and carbodiimide (OTC-I_EDC). The gross appearance, physico-chemical characteristics, biocompatibility and growth profile of seeded skin cells were assessed. The light brown and white appearance for the OTC-I_GNP scaffold and other groups were observed, respectively. The OTC-I_GNP scaffold demonstrated the highest swelling ratio (~1885%) and water uptake (94.96 ± 0.14%). The Fourier transformation infrared demonstrated amide A, B and I, II and III which represent collagen type I. The microstructure of all fabricated sponges presented a similar surface roughness with the presence of visible collagen fibers and a heterogenous porous structure. The OTC-I_EDC scaffold was more toxic and showed the lowest cell attachment and proliferation as compared to other groups. The micrographic evaluation revealed that CC potentially formed the epidermal- and dermal-like layers in both SM and ALI that prominently observed with OTC-I_GNP compared to others. In conclusion, these results suggest that OTC_GNP could be used as a 3D in vitro skin model under ALI microenvironment.
    Matched MeSH terms: Amides
  8. Maarof M, Mohd Nadzir M, Sin Mun L, Fauzi MB, Chowdhury SR, Idrus RBH, et al.
    Polymers (Basel), 2021 Feb 08;13(4).
    PMID: 33567703 DOI: 10.3390/polym13040508
    The current strategy for rapid wound healing treatment involves combining a biomaterial and cell-secreted proteins or biomolecules. This study was aimed at characterizing 3-dimensional (3D) collagen hydrogels fortified with dermal fibroblast-conditioned medium (DFCM) as a readily available acellular skin substitute. Confluent fibroblasts were cultured with serum-free keratinocyte-specific medium (KM1 and KM2) and fibroblast-specific medium (FM) to obtain DFCM. Subsequently, the DFCM was mixed with collagen (Col) hydrogel and chondroitin-4-sulphate (C4S) to fabricate 3D constructs termed Col/C4S/DFCM-KM1, Col/C4S/DFCM-KM2, and Col/C4S/DFCM-FM. The constructs successfully formed soft, semi-solid and translucent hydrogels within 1 h of incubation at 37 °C with strength of <2.5 Newton (N). The Col/C4S/DFCM demonstrated significantly lower turbidity compared to the control groups. The Col/C4S/DFCM also showed a lower percentage of porosity (KM1: 35.15 ± 9.76%; KM2: 6.85 ± 1.60%; FM: 14.14 ± 7.65%) compared to the Col (105.14 ± 11.87%) and Col/C4S (143.44 ± 27.72%) constructs. There were no changes in both swelling and degradation among all constructs. Fourier transform infrared spectrometry showed that all groups consisted of oxygen-hydrogen bonds (O-H) and amide I, II, and III. In conclusion, the Col/C4S/DFCM constructs maintain the characteristics of native collagen and can synergistically deliver essential biomolecules for future use in skin therapeutic applications.
    Matched MeSH terms: Amides
  9. Chong KC, Lai SO, Lau WJ, Thiam HS, Ismail AF, Roslan RA
    Polymers (Basel), 2018 Jan 28;10(2).
    PMID: 30966162 DOI: 10.3390/polym10020126
    Air pollution is a widely discussed topic amongst the academic and industrial spheres as it can bring adverse effects to human health and economic loss. As humans spend most of their time at the office and at home, good indoor air quality with enriched oxygen concentration is particularly important. In this study, polysulfone (PSF) hollow fiber membranes fabricated by dry-jet wet phase inversion method were coated by a layer of polydimethylsiloxane (PDMS) or poly(ether block amide) (PEBAX) at different concentrations and used to evaluate their performance in gas separation for oxygen enrichment. The surface-coated membranes were characterized using SEM and EDX to determine the coating layer thickness and surface chemical properties, respectively. Results from the gas permeation study revealed that the PSF membrane coated with PDMS offered higher permeance and selectivity compared to the membrane coated with PEBAX. The best performing PDMS-coated membrane demonstrated oxygen and nitrogen gas permeance of 18.31 and 4.01 GPU, respectively with oxygen/nitrogen selectivity of 4.56. Meanwhile, the PEBAX-coated membrane only showed 12.23 and 3.11 GPU for oxygen and nitrogen gas, respectively with a selectivity of 3.94. It can be concluded the PDMS coating is more promising for PSF hollow fiber membrane compared to the PEBAX coating for the oxygen enrichment process.
    Matched MeSH terms: Amides
  10. Mat Yusuf SNA, Ng YM, Ayub AD, Ngalim SH, Lim V
    Polymers (Basel), 2017 Jul 27;9(8).
    PMID: 30970988 DOI: 10.3390/polym9080311
    Discovery and use of biocompatible polymers offers great promise in the pharmaceutical field, particularly in drug delivery systems. Disulphide bonds, which commonly occur in peptides and proteins and have been used as drug-glutathione conjugates, are reductively cleaved in the colon. The intrinsic stability of a disulphide relative to thiol groups is determined by the redox potential of the environment. The objective of this study was to synthesise a trimesic acid-based disulphide cross-linked polymer that could potentially be used for targeted delivery to the colon. The monomer was synthesised by an amide coupling reaction between trimesic acid and (triphenylmethyl) thioethylamine using a two-step synthesis method. The s-trityl group was removed using a cocktail of trifluoroacetic acid and triethylsilane to expose the thiols in preparation for further polymerisation. The resulting polymers (P10, P15, P21, P25, and P51, generated using different molar ratios) were reduced after 1.5 h of reduction time. Scanning electron microscopy images of the polymers showed spherical, loose, or tight patterns depending on the molar ratio of polymerisation. These polymers also exhibited efficient dissolution under various gastrointestinal conditions. Of the five polymers tested, P10 and P15 appeared to be promising drug delivery vehicles for poorly soluble drugs, due to the hydrophobic nature of the polymers.
    Matched MeSH terms: Amides
  11. Lopez JAV, Petitbois JG, Vairappan CS, Umezawa T, Matsuda F, Okino T
    Org. Lett., 2017 08 18;19(16):4231-4234.
    PMID: 28783344 DOI: 10.1021/acs.orglett.7b01869
    Two new chlorinated fatty acid amides, columbamides D (1) and E (2), along with apratoxins A and C and wewakazole, were isolated from the organic extract of a Moorea bouillonii sample from Sabah, Malaysia. Structure elucidation was accomplished by a combination of MS and NMR analyses. The total synthesis of all four stereoisomers of 1 was completed, and the absolute configuration was determined by chiral-phase HPLC and Marfey's analysis.
    Matched MeSH terms: Amides/isolation & purification*; Amides/chemistry
  12. Kee CH, Ariffin A, Awang K, Takeya K, Morita H, Hussain SI, et al.
    Org Biomol Chem, 2010 Dec 21;8(24):5646-60.
    PMID: 20941451 DOI: 10.1039/c0ob00296h
    The syntheses of fourteen unusual o-carboxamido stilbenes by the Heck protocol revealed surprising complexity related to intriguing substituent effects with mechanistic implications. The unexpected cytotoxic and chemopreventive properties also seem to be substituent dependent. For example, although stilbene 15d (with a 4-methoxy substituent) showed cytotoxicity on HT29 colon cancer cells with an IC(50) of 4.9 μM, the 3,4-dimethoxy derivative (15c) is inactive. It is interesting to observe that the 3,5-dimethoxy derivative (15e) showed remarkable chemopreventive activity in WRL-68 fetal hepatocytes, surpassing the gold standard, resveratrol. The resveratrol concentration needed to be 5 times higher than that of 15e to produce comparable elevation of NQO1.
    Matched MeSH terms: Amides/chemistry*
  13. Hussain K, Ismail Z, Sadikun A, Ibrahim P
    Nat Prod Res, 2009;23(3):238-49.
    PMID: 19235024 DOI: 10.1080/14786410801987597
    Ethanol and aqueous extracts of the different parts of Piper sarmentosum were analysed by HPLC for marker compounds to standardise these extracts. The standardised extracts were investigated for antioxidant activity (beta-carotene linoleate model and DPPH model), anti-TB activity (microplate tetrazolium assay), and estimation of total phenolic and amide contents. The extracts of the different parts exhibited different antioxidant activity, phenolic and amide contents (p < 0.01). The ethanol extracts exhibited better antioxidant activity as compared to the aqueous extracts. The leaf ethanol extract was further investigated for dose response relationship and its EC(50) was found to be 38 microg mL(-1). All the extracts have exhibited anti-TB activity with MIC/MBC 12.5 microg mL(-1). The leaf methanol extract was fractionated and the ethyl acetate fraction exhibited anti-TB activity with MIC/MBC 3.12 microg mL(-1) while MIC/MBC of isoniazid (INH) was found to be 0.5 microg mL(-1). A positive correlation was found between antioxidant activity and total polyphenols, flavonoids and amides, in the beta-carotene linoleate model (p = 0.05) and in the DPPH model (p = 0.01). The analytical method was found to have linearity >0.9922, coefficient of variance <5% and accuracy 95.5 +/- 5 to 96.9 +/- 5. This plant possesses promising antioxidant as well as anti-TB properties.
    Matched MeSH terms: Amides/chemistry*
  14. Amjad MW, Amin MC, Katas H, Butt AM
    Nanoscale Res Lett, 2012;7(1):687.
    PMID: 23270381 DOI: 10.1186/1556-276X-7-687
    Doxorubicin-loaded micelles were prepared from a copolymer comprising cholic acid (CA) and polyethyleneimine (PEI) for the delivery of antitumor drugs. The CA-PEI copolymer was synthesized via pairing mediated by N,N'-dicyclohexylcarbodiimide and N-hydroxysuccinimide using dichloromethane as a solvent. Fourier transform infrared and nuclear magnetic resonance analyses were performed to verify the formation of an amide linkage between CA and PEI and doxorubicin localization into the copolymer. Dynamic light scattering and transmission electron microscopy studies revealed that the copolymer could self-assemble into micelles with a spherical morphology and an average diameter of <200 nm. The CA-PEI copolymer was also characterized by X-ray diffraction and differential scanning calorimetry. Doxorubicin-loaded micelles were prepared by dialysis method. A drug release study showed reduced drug release with escalating drug content. In a cytotoxicity assay using human colorectal adenocarcinoma (DLD-1) cells, the doxorubicin-loaded CA-PEI micelles exhibited better antitumor activity than that shown by doxorubicin. This is the first study on CA-PEI micelles as doxorubicin carriers, and this study demonstrated that they are promising candidates as carriers for sustained targeted antitumor drug delivery system.
    Matched MeSH terms: Amides
  15. Heo HY, Tee YK, Harston G, Leigh R, Chappell MA
    NMR Biomed, 2023 Jun;36(6):e4734.
    PMID: 35322482 DOI: 10.1002/nbm.4734
    Amide proton transfer (APT) imaging, a variant of chemical exchange saturation transfer MRI, has shown promise in detecting ischemic tissue acidosis following impaired aerobic metabolism in animal models and in human stroke patients due to the sensitivity of the amide proton exchange rate to changes in pH within the physiological range. Recent studies have demonstrated the possibility of using APT-MRI to detect acidosis of the ischemic penumbra, enabling the assessment of stroke severity and risk of progression, monitoring of treatment progress, and prognostication of clinical outcome. This paper reviews current APT imaging methods actively used in ischemic stroke research and explores the clinical aspects of ischemic stroke and future applications for these methods.
    Matched MeSH terms: Amides
  16. Mollataghi A, Hadi AH, Cheah SC
    Molecules, 2012 Apr 05;17(4):4197-208.
    PMID: 22481540 DOI: 10.3390/molecules17044197
    A new dienamide, (2E,4E)-7-(3',4'-dimethoxyphenyl)-N-ethyl-6-(R)-hydroxyhepta- 2,4-dienamide, named (-)-kunstleramide (1), were isolated from the bark of Beilschmiedia kunstleri Gamble together with one neolignan: (+)-kunstlerone (2) and seven known alkaloids: (+)-nornuciferine (3), (-)-isocaryachine (4), (+)-cassythicine (5), (+)-laurotetanine (6), (+)-boldine (7), noratherosperminine (8), (+)-N-demethylphyllocaryptine (9). Their structures were established from spectroscopic techniques, most notably 1D- and 2D-NMR, UV, IR, OR, circular dichroism (CD) spectra and LCMS-IT-TOF. (-)-Kunstleramide (1) exhibited very poor dose-dependent inhibition of DPPH activity, with an IC₅₀ value of 179.5 ± 4.4 μg/mL, but showed a moderate cytotoxic effect on MTT assays of A375, A549, HT-29, PC-3 and WRL-68 with EC₅₀ values of 64.65, 44.74, 55.94, 73.87 and 70.95 µg/mL, respectively.
    Matched MeSH terms: Amides/pharmacology*; Amides/chemistry
  17. Kee CH, Ariffin A, Awang K, Noorbatcha I, Takeya K, Morita H, et al.
    Molecules, 2011 Aug 25;16(9):7267-87.
    PMID: 21869754 DOI: 10.3390/molecules16097267
    The n-butyramido, isobutyramido, benzamido, and furancarboxamido functions profoundly modulate the electronics of the stilbene olefinic and NH groups and the corresponding radical cations in ways that influence the efficiency of the cyclization due presumably to conformational and stereoelectronic factors. For example, isobutyramido- stilbene undergoes FeCl(3) promoted cyclization to produce only indoline, while n-butyramidostilbene, under the same conditions, produces both indoline and bisindoline.
    Matched MeSH terms: Amides/chemistry*
  18. Khan IA, Ahmad M, Ashfaq UA, Sultan S, Zaki MEA
    Molecules, 2021 Aug 06;26(16).
    PMID: 34443347 DOI: 10.3390/molecules26164760
    α-Glucosidase inhibitors (AGIs) are used as medicines for the treatment of diabetes mellitus. The α-Glucosidase enzyme is present in the small intestine and is responsible for the breakdown of carbohydrates into sugars. The process results in an increase in blood sugar levels. AGIs slow down the digestion of carbohydrates that is helpful in controlling the sugar levels in the blood after meals. Among heterocyclic compounds, benzimidazole moiety is recognized as a potent bioactive scaffold for its wide range of biologically active derivatives. The aim of this study is to explore the α-glucosidase inhibition ability of benzimidazolium salts. In this study, two novel series of benzimidazolium salts, i.e., 1-benzyl-3-{2-(substituted) amino-2-oxoethyl}-1H-benzo[d]imidazol-3-ium bromide 9a-m and 1-benzyl-3-{2-substituted) amino-2-oxoethyl}-2-methyl-1H-benzo[d] imidazol-3-ium bromide 10a-m were screened for their in vitro α-glucosidase inhibitory potential. These compounds were synthesized through a multistep procedure and were characterized by 1H-NMR, 13C-NMR, and EI-MS techniques. Compound 10d was identified as the potent α-glucosidase inhibitor among the series with an IC50 value of 14 ± 0.013 μM, which is 4-fold higher than the standard drug, acarbose. In addition, compounds 10a, 10e, 10h, 10g, 10k, 10l, and 10m also exhibited pronounced potential for α-glucosidase inhibition with IC50 value ranging from 15 ± 0.037 to 32.27 ± 0.050 µM when compared with the reference drug acarbose (IC50 = 58.8 ± 0.12 μM). A molecular docking study was performed to rationalize the binding interactions of potent inhibitors with the active site of the α-glucosidase enzyme.
    Matched MeSH terms: Amides/chemistry*
  19. Said N, Wong KC, Lau WJ, Khoo YS, Yeong YF, Othman NH, et al.
    Molecules, 2022 Dec 01;27(23).
    PMID: 36500475 DOI: 10.3390/molecules27238381
    Most researchers focused on developing highly selective membranes for CO2/CH4 separation, but their developed membranes often suffered from low permeance. In this present work, we aimed to develop an ultrahigh permeance membrane using a simple coating technique to overcome the trade-off between membrane permeance and selectivity. A commercial silicone membrane with superior permeance but low CO2/CH4 selectivity (in the range of 2-3) was selected as the host for surface modification. Our results revealed that out of the three silane agents tested, only tetraethyl orthosilicate (TEOS) improved the control membrane's permeance and selectivity. This can be due to its short structural chain and better compatibility with the silicone substrate. Further investigation revealed that higher CO2 permeance and selectivity could be attained by coating the membrane with two layers of TEOS. The surface integrity of the TEOS-coated membrane was further improved when an additional polyether block amide (Pebax) layer was established atop the TEOS layer. This additional layer sealed the pin holes of the TEOS layer and enhanced the resultant membrane's performance, achieving CO2/CH4 selectivity of ~19 at CO2 permeance of ~2.3 × 105 barrer. This performance placed our developed membrane to surpass the 2008 Robeson Upper Boundary.
    Matched MeSH terms: Amides*
  20. Moshikur RM, Ali MK, Wakabayashi R, Moniruzzaman M, Goto M
    Mol Pharm, 2021 08 02;18(8):3108-3115.
    PMID: 34250805 DOI: 10.1021/acs.molpharmaceut.1c00324
    Coronavirus disease 2019 (COVID-19) has spread across the world, and no specific antiviral drugs have yet been approved to combat this disease. Favipiravir (FAV) is an antiviral drug that is currently in clinical trials for use against COVID-19. However, the delivery of FAV is challenging because of its limited solubility, and its formulation is difficult with common organic solvents and water. To address these issues, four FAV ionic liquids (FAV-ILs) were synthesized as potent antiviral prodrugs and were fully characterized by nuclear magnetic resonance (NMR) spectroscopy, Fourier-transform infrared (FT-IR) spectrometry, powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA), derivative thermogravimetry (DTG), and differential scanning calorimetry (DSC). The aqueous solubility and in vivo pharmacokinetic properties of the FAV-ILs were also evaluated. The FAV-ILs exhibited improved aqueous solubility by 78 to 125 orders of magnitude when compared with that of free FAV. Upon oral dosing in mice, the absolute bioavailability of the β-alanine ethyl ester FAV formulation was increased 1.9-fold compared with that of the control FAV formulation. The peak blood concentration, elimination half-life, and mean absorption time of FAV were also increased by 1.5-, 2.0-, and 1.5-fold, respectively, compared with the control. Furthermore, the FAV in the FAV-ILs exhibited significantly different biodistribution compared with the control FAV formulation. Interestingly, drug accumulation in the lungs and liver was improved 1.5-fold and 1.3-fold, respectively, compared with the control FAV formulation. These results indicate that the use of ILs exhibits potential as a simple, scalable strategy to improve the solubility and oral absorption of hydrophobic drugs, such as FAV.
    Matched MeSH terms: Amides/administration & dosage*; Amides/chemical synthesis; Amides/pharmacokinetics; Amides/chemistry
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