Displaying publications 1 - 20 of 96 in total

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  1. 3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors
    Osman H, Idris NH, Kamarulzaman EE, Wahab HA, Hassan MZ
    Acta Pharm Sin B, 2017 Jul;7(4):479-484.
    PMID: 28752033 DOI: 10.1016/j.apsb.2017.04.009
    Dengue is a severe mosquito-borne viral infection causing half a million deaths annually. Dengue virus NS2B/NS3 protease is a validated target for anti-dengue drug design. A series of hitherto unreported 3,5-bis(arylidene)-4-piperidones analogues 4a-4j were synthesized and screened in silico against DENV2 NS2B/NS3 protease to elucidate their binding mechanism and orientation around the active sites. Results were validated through an in vitro DENV2 NS2B/NS3 protease assay using a fluorogenic Boc-Gly-Arg-Arg-AMC substrate. Nitro derivatives of 3,5-bis(arylidene)-4-piperidones (4e and 4j) emerged as promising lead molecules for novel protease inhibitors with an IC50 of 15.22 and 16.23 µmol/L, respectively, compared to the standard, panduratin A, having IC50 of 57.28 µmol/L.
  2. Fulltext 4-Thiazolidinone coumarin derivatives as two-component NS2B/NS3 DENV flavivirus serine protease inhibitors: synthesis, molecular docking, biological evaluation and structure-activity relationship studies
    Yusufzai SK, Osman H, Khan MS, Abd Razik BM, Ezzat MO, Mohamad S, et al.
    Chem Cent J, 2018 Jun 12;12(1):69.
    PMID: 29896651 DOI: 10.1186/s13065-018-0435-0
    A series of novel 4-thiazolidinone inhibitors SKYa-SKYg, containing coumarin as a core structure were synthesized via facile and efficient method. The structures of the synthesized compounds were established by extensive spectroscopic studies (FT IR, 1D NMR, 2D NMR, LC-MS) and elemental analysis. All the synthesized hybrids were further evaluated for their potential as anti-tubercular agents against Mycobacterium tuberculosis H37Rv ATCC 25618, and anti-bacterial agents against Escherichia coli, Enterobacter aerogenes, Salmonella typhi, Streptococcus pneumoniae and Staphylococcus aureus. Interestingly, the hybrids displayed potent bioactivity. However, compounds SKYc, SKYd, and SKYe appeared to be more effective against the tested bacterial strains, among which compound SKYb showed the highest inhibition against all the bacterial strains ranging from 41 to 165 μg/mL, as compared to the standards, streptomycin, kanamycin and vancomycin. Moreover, derivative SKYa was found to be the strongest against M. tuberculosis (83 μg/mL). Additionally, the anti-dengue potential of the coumarin hybrids as two-component NS2B/NS3 DENV flavivirus serine protease inhibitors was calculated using computational molecular docking approach, with reference to the standards 4-hydroxypanduratin, panduratin and ethyl 3-(4-(hydroxymethyl)-2-methoxy-5-nitrophenoxy)propanoate with DS of - 3.379, - 3.189 and - 3.381, respectively. The docking results revealed that the synthesized hybrids exhibited potent anti-dengue activity among which compounds SKYf, SKYd, SKYc and SKYe were found to be the best ones with docking scores of - 4.014, - 3.964, - 3.905 and - 3.889. In summary, we discovered 4-thiazolidinone coumarin derivatives as a new scaffold that may eventually yield useful compounds in the treatment of bacterial and viral infections.
  3. Fulltext A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives
    Brishty SR, Hossain MJ, Khandaker MU, Faruque MRI, Osman H, Rahman SMA
    Front Pharmacol, 2021;12:762807.
    PMID: 34803707 DOI: 10.3389/fphar.2021.762807
    Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential heterocyclic drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore of naturally occurring active biomolecules, benzimidazole derivatives have significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers have synthesized plenty of benzimidazole derivatives in the last decades, amidst a large share of these compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we have summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012-2021) with their available structure-activity relationship. Compounds bearing benzimidazole nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects to the world's most virulent diseases. Several promising therapeutic candidates are undergoing human trials, and some of these are going to be approved for clinical use. However, notable challenges, such as drug resistance, costly and tedious synthetic methods, little structural information of receptors, lack of advanced software, and so on, are still viable to be overcome for further research.
  4. Fulltext A Sustainable Approach to the Stereoselective Synthesis of Diazaheptacyclic Cage Systems Based on a Multicomponent Strategy in an Ionic Liquid
    Suresh Kumar R, Almansour AI, Arumugam N, Altaf M, Menéndez JC, Kumar RR, et al.
    Molecules, 2016 Jan 29;21(2):165.
    PMID: 26840282 DOI: 10.3390/molecules21020165
    The microwave-assisted three-component reactions of 3,5-bis(E)-arylmethylidene]tetrahydro-4(1H)-pyridinones, acenaphthenequinone and cyclic α-amino acids in an ionic liquid, 1-butyl-3-methylimidazolium bromide, occurred through a domino sequence affording structurally intriguing diazaheptacyclic cage-like compounds in excellent yields.
  5. A facile chemo-, regio- and stereoselective synthesis and cholinesterase inhibitory activity of spirooxindole-pyrrolizine-piperidine hybrids
    Kia Y, Osman H, Kumar RS, Murugaiyah V, Basiri A, Perumal S, et al.
    Bioorg Med Chem Lett, 2013 May 15;23(10):2979-83.
    PMID: 23570788 DOI: 10.1016/j.bmcl.2013.03.027
    A series of novel hybrid spiro heterocycles comprising pyrrolizine, spiroxindole and piperidine moieties was synthesized chemo-, regio- and stereoselectively in good yields from 1,3-dipolar cycloaddition reaction of a series of 1-acryloyl-3,5-bisarylmethylidenepiperidin-4-ones with azomethine ylides generated in situ from 5-choloroisatin and l-proline in methanol. These cycloadducts displayed significant cholinesterase inhibitory activity. Among the compounds screened, 8g and 8e, showed maximum inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinestrase (BChE) with IC50 values of 3.33 and 3.13μM, respectively.
  6. A facile stereoselective synthesis of dispiro-indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids and evaluation of their antimycobacterial, anticancer and AchE inhibitory activities
    Bharkavi C, Vivek Kumar S, Ashraf Ali M, Osman H, Muthusubramanian S, Perumal S
    Bioorg Med Chem, 2016 11 15;24(22):5873-5883.
    PMID: 27687968 DOI: 10.1016/j.bmc.2016.09.044
    A facile stereoselective synthesis of novel dispiro indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids has been achieved by 1,3-dipolar cycloaddition of azomethine ylides, generated in situ from ninhydrin and sarcosine/thiaproline, on a series of 3-benzylidenethiochroman-4-ones. The synthesised compounds were screened for their antimycobacterial, anticancer and AchE inhibition activities. Compound 4l (IC50 1.07μM) has been found to exhibit the most potent antimycobacterial activity compared to cycloserine (12 times), pyrimethamine (37 times) and ethambutol (IC50 <1.56μM) and 6l (IC50=2.87μM) is more active than both cycloserine (4 times) and pyrimethamine (12 times). Three compounds, 4a, 6b and 6i, display good anticancer activity against CCRF-CEM cell lines. Compounds 6g and 4g display maximum AchE inhibitory activity with IC50 values of 1.10 and 1.16μmol/L respectively.
  7. A pioneering study of the radiological mapping in the world's largest mangrove forest (the Sundarbans) and implications for the public and environment
    Al Mahmud J, Siraz MMM, Alam MS, Dewan MJ, Rashid MB, Khandaker MU, et al.
    Mar Pollut Bull, 2024 May;202:116349.
    PMID: 38604081 DOI: 10.1016/j.marpolbul.2024.116349
    Coastal Mangroves are facing growing threats due to the harmful consequences of human activities. This first-ever detailed study of natural radioactivity in soil samples collected from seven tourist destinations within the Sundarbans, the world's largest mangrove forest, was conducted using HPGe gamma-ray spectrometry. Although the activity levels of 226Ra (11 ± 1-44 ± 4 Bq/kg) and 232Th (13 ± 1-68 ± 6 Bq/kg) generally align with global averages, the concentration of 40K (250 ± 20-630 ± 55 Bq/kg) was observed to surpass the worldwide average primarily due to factors like salinity intrusion, fertilizer application, agricultural runoff, which suggests the potential existence of potassium-rich mineral resources near the study sites. The assessment of the hazard parameters indicates that the majority of these parameters are within the recommended limits. The soil samples do not pose a significant radiological risk to the nearby population. The results of this study can establish important radiological baseline data before the Rooppur Nuclear Power Plant begins operating in Bangladesh.
  8. AChE inhibitor: a regio- and stereo-selective 1,3-dipolar cycloaddition for the synthesis of novel substituted 5,6-dimethoxy spiro[5.3']-oxindole-spiro-[6.3″]-2,3-dihydro-1H-inden-1″-one-7-(substituted aryl)-tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole
    Ashraf Ali M, Ismail R, Choon TS, Kumar RS, Osman H, Arumugam N, et al.
    Bioorg Med Chem Lett, 2012 Jan 1;22(1):508-11.
    PMID: 22142546 DOI: 10.1016/j.bmcl.2011.10.087
    Pyrrolothiazolyloxindole analogues share vital pharmacological properties, considered useful in Alzheimer's disease (AD). The aim of this study was synthesis and evaluate pyralothiazolyloxindole analogues if possess acetyl cholinesterase (AChE) inhibitory activity. The easily accessible one-pot synthesis of these compounds resulted to be significantly less difficult and expensive than that of donepezil. Several compounds possess anti-cholinesterase activity in the order of micro and sub-micromolar. Particularly, compound was the most potent inhibitors of the series against acetyl cholinesterase enzyme with IC(50) 0.11μmol/L.
  9. Advocating Electrically Conductive Scaffolds with Low Immunogenicity for Biomedical Applications: A Review
    Ahmad Ruzaidi DA, Mahat MM, Shafiee SA, Mohamed Sofian Z, Mohmad Sabere AS, Ramli R, et al.
    Polymers (Basel), 2021 Oct 02;13(19).
    PMID: 34641210 DOI: 10.3390/polym13193395
    Scaffolds support and promote the formation of new functional tissues through cellular interactions with living cells. Various types of scaffolds have found their way into biomedical science, particularly in tissue engineering. Scaffolds with a superior tissue regenerative capacity must be biocompatible and biodegradable, and must possess excellent functionality and bioactivity. The different polymers that are used in fabricating scaffolds can influence these parameters. Polysaccharide-based polymers, such as collagen and chitosan, exhibit exceptional biocompatibility and biodegradability, while the degradability of synthetic polymers can be improved using chemical modifications. However, these modifications require multiple steps of chemical reactions to be carried out, which could potentially compromise the end product's biosafety. At present, conducting polymers, such as poly(3,4-ethylenedioxythiophene) poly(4-styrenesulfonate) (PEDOT: PSS), polyaniline, and polypyrrole, are often incorporated into matrix scaffolds to produce electrically conductive scaffold composites. However, this will reduce the biodegradability rate of scaffolds and, therefore, agitate their biocompatibility. This article discusses the current trends in fabricating electrically conductive scaffolds, and provides some insight regarding how their immunogenicity performance can be interlinked with their physical and biodegradability properties.
  10. An alternative method for calculation of half-value layers without the knowledge of attenuation coefficient
    Hassanpour M, Hassanpour M, Uddin Khandaker M, Rashed Iqbal Faruque M, Alshahrani B, Osman H
    Appl Radiat Isot, 2023 Sep;199:110910.
    PMID: 37379789 DOI: 10.1016/j.apradiso.2023.110910
    Radiation protection is crucial for the safe utilization of ionizing radiation and minimizing the harmful effect upon exposure, hence some standards have been defined by some relevant organizations for the safe uses of radiation. One of the parameters relevant to the calculation of gamma ray shielding is the half-value layer (HVL), which is normally calculated using the knowledge of linear attenuation coefficient (μ). In this research, an attempt has been made to directly calculate HVL without the knowledge of μ via Monte Carlo simulation technique. For this purpose, in the Monte Carlo N-Particle eXtended (MCNPX) code, F1, F5 and Mesh Popul sequences tallies were defined and the optimal structure for the least measurement error was introduced. The MCNPX calculated values showed reasonable agreement with the experimental findings. According to the obtained results, it is suggested that in order to reduce the error of HVL calculations, in exchange for the MCNPX code, the values of the R parameter and the radiation angle of the source should be considered according to the calculations introduced in this plan. Because the results show that by considering the measurement error between 6 and 20%, the code output can be cited in different energy ranges.
  11. An efficient ionic liquid mediated synthesis, cholinesterase inhibitory activity and molecular modeling study of novel piperidone embedded α,β-unsaturated ketones
    Kia Y, Osman H, Kumar RS, Murugaiyah V, Basiri A, Khaw KY, et al.
    Med Chem, 2014;10(5):512-20.
    PMID: 24138113
    A series of hitherto unreported piperidone embedded α,β-unsaturated ketones were synthesized efficiently in ionic solvent and evaluated for cholinesterase inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Most of the synthesized compounds displayed good enzyme inhibition; therein compounds 7i and 7f displayed significant activity against AChE with IC50 values of 1.47 and 1.74 µM, respectively. Compound 6g showed the highest BChE inhibitory potency with IC50 value of 3.41 µM, being 5 times more potent than galanthamine. Molecular modeling simulation was performed using AChE and BChE receptors extracted from crystal structure of human AChE and human BChE to determine the amino acid residues involved in the binding interaction of synthesized compounds and their relevant receptors.
  12. An expedient, ionic liquid mediated multi-component synthesis of novel piperidone grafted cholinesterase enzymes inhibitors and their molecular modeling study
    Basiri A, Murugaiyah V, Osman H, Kumar RS, Kia Y, Awang KB, et al.
    Eur J Med Chem, 2013 Sep;67:221-9.
    PMID: 23871902 DOI: 10.1016/j.ejmech.2013.06.054
    Series of hitherto unreported piperidone grafted pyridopyrimidines synthesized through ionic liquid mediated multi-component reaction. These compounds were evaluated for their inhibitory activities against AChE and BChE enzymes. All the compounds displayed considerable potency against AChE with IC50 values ranging from 0.92 to 9.11 μM, therein compounds 6a, 6h and 6i displayed superior enzyme inhibitory activities compared to standard drug with IC50 values of 0.92, 1.29 and 2.07 μM. Remarkably, all the compounds displayed higher BChE inhibitory activity compared to galantamine with IC50 values of 1.89-8.13 μM. Molecular modeling, performed for the most active compounds using three dimensional crystal structures of TcAChE and hBChE, disclosed binding template of these inhibitors into the active site of their respective enzymes.
  13. Antibiotic resistance and molecular typing among cockle (Anadara granosa) strains of Vibrio parahaemolyticus by polymerase chain reaction (PCR)-based analysis
    Sahilah AM, Laila RA, Sallehuddin HM, Osman H, Aminah A, Ahmad Azuhairi A
    World J Microbiol Biotechnol, 2014 Feb;30(2):649-59.
    PMID: 24068534 DOI: 10.1007/s11274-013-1494-y
    Genomic DNA of Vibrio parahaemolyticus were characterized by antibiotic resistance, enterobacterial repetitive intergenic consensus-polymerase chain reaction (ERIC-PCR) and random amplified polymorphic DNA-polymerase chain reaction (RAPD-PCR) analysis. These isolates originated from 3 distantly locations of Selangor, Negeri Sembilan and Melaka (East coastal areas), Malaysia. A total of 44 (n = 44) of tentatively V. parahaemolyticus were also examined for the presence of toxR, tdh and trh gene. Of 44 isolates, 37 were positive towards toxR gene; while, none were positive to tdh and trh gene. Antibiotic resistance analysis showed the V. parahaemolyticus isolates were highly resistant to bacitracin (92%, 34/37) and penicillin (89%, 33/37) followed by resistance towards ampicillin (68%, 25/37), cefuroxime (38%, 14/37), amikacin (6%, 2/37) and ceftazidime (14%, 5/37). None of the V. parahaemolyticus isolates were resistant towards chloramphenicol, ciprofloxacin, ceftriaxone, enrofloxacin, norfloxacin, streptomycin and vancomycin. Antibiogram patterns exhibited, 9 patterns and phenotypically less heterogenous when compared to PCR-based techniques using ERIC- and RAPD-PCR. The results of the ERIC- and RAPD-PCR were analyzed using GelCompare software. ERIC-PCR with primers ERIC1R and ERIC2 discriminated the V. parahaemolyticus isolates into 6 clusters and 21 single isolates at a similarity level of 80%. While, RAPD-PCR with primer Gen8 discriminated the V. parahaemolyticus isolates into 11 clusters and 10 single isolates and Gen9 into 8 clusters and 16 single isolates at the same similarity level examined. Results in the presence study demonstrated combination of phenotypically and genotypically methods show a wide heterogeneity among cockle isolates of V. parahaemolyticus.
  14. Fulltext Anticonvulsant activity of α-terpineol isolated from myristica fragrans in GAERS model of absence epilepsy
    Islam, M.R., Muthuraju, S., Tarmizi, C.H., Zulkifli, M.M., Osman, H., Mohamad, H., et al.
    ASM Science Journal, 2012;6(2):95-102.
    MyJurnal
    Epilepsy is a neurological disorder characterized by recurrent seizures resulting from excessive abnormal electrical discharges in the brain. Medicinal plants may play an invaluable role to discover the new antiepileptic drugs. The aim of the present study was to investigate the anticonvulsant activity of α-terpineol isolated from Myristica fragrans Hountt. The α-terpineol showed a significant inhibition of the seizure episodes and spikes in absence seizures model of Genetic Absence Epilepsy Rats from Strasbourg (GAERS) rats by using electroencephalography records. It showed dose-dependent anticonvulsant activity that was comparable to the known antiepileptic drug of diazepam. It showed a rapid onset and relatively short duration of anticonvulsant effects. The present findings suggest that α-terpineol might possess antiepileptic activities against the partial seizures of human because it prevented seizures in well-established genetic absence seizure animal model of GAERS rats.
  15. Antimicrobial activity of Cassia alata from Malaysia
    Ibrahim D, Osman H
    J Ethnopharmacol, 1995 Mar;45(3):151-6.
    PMID: 7623478
    Ethanolic extract of Cassia alata leaves was investigated for its antimicrobial activities on several microorganisms including bacteria, yeast, dermatophytic fungi and non-dermatophytic fungi. In vitro, the extract exhibited high activity against various species of dermatophytic fungi but low activity against non-dermatophytic fungi. However, bacterial and yeast species showed resistance against in vitro treatment with the extract. The minimum inhibitory concentration (MIC) values of the extract revealed that Trichophyton mentagorphytes var. interdigitale, Trichophyton mentagrophytes var. mentagorophytes, Trichophyton rubrum and Microsporum gypseum had the MIC of 125 mg/ml, whereas Microsporum canis had the MIC of 62.5 mg/ml. The inhibition can be observed on the macroconidia of Microsporum gypseum which resulted in structural degeneration beyond repair. The mechanism of inhibition can be related to the cell leakage as observed by irregular, wrinkle shape and loss in rigidity of the macroconidia.
  16. Antimycobacterial activity: a facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines
    Wei AC, Ali MA, Yoon YK, Ismail R, Choon TS, Kumar RS, et al.
    Bioorg Med Chem Lett, 2012 Aug 1;22(15):4930-3.
    PMID: 22749825 DOI: 10.1016/j.bmcl.2012.06.047
    A series of twelve dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H(37)Rv and INH resistant M. tuberculosis strains using agar dilution method, four of them showed good activity with MIC of less than 1 μM. Compound 4'-[5-(4-fluorophenyl)pyridin-3-yl]-1'-methyldispiro[indan-2,2' pyrrolidine-3',2″-indan]-1,3,1″-trione (4b) was found to be the most active with MIC of 0.1215 and 5.121 μM, respectively.
  17. Fulltext Antioxidant activity and phenolic content of Paederia foetida and Syzygium aqueum
    Osman H, Rahim AA, Isa NM, Bakhir NM
    Molecules, 2009;14(3):970-8.
    PMID: 19305354 DOI: 10.3390/molecules14030970
    The antioxidant activity of fresh and dried plant extracts of Paederia foetida and Syzygium aqueum were studied using beta-carotene bleaching and the 2,2'-azinobis(3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) radical cation assay. The percentage of antioxidant activity for all extract samples using both assays was between 58 and 80%. The fresh samples of both plants had higher antioxidant activity than the dried samples. The results of the beta-carotene bleaching assay were correlated (R(2) = 0.9849) with those of the ABTS assay.
  18. Fulltext Antituberculosis activity, phytochemical identification of Costus speciosus (J. Koenig) Sm., Cymbopogon citratus (DC. Ex Nees) Stapf., and Tabernaemontana coronaria (L.) Willd. and their effects on the growth kinetics and cellular integrity of Mycobacterium tuberculosis H37Rv
    Mohamad S, Ismail NN, Parumasivam T, Ibrahim P, Osman H, A Wahab H
    BMC Complement Altern Med, 2018 Jan 08;18(1):5.
    PMID: 29310671 DOI: 10.1186/s12906-017-2077-5
    BACKGROUND: Costus speciosus, Cymbopogon citratus, and Tabernaemontana coronaria are herbal plants traditionally used as remedies for symptoms of tuberculosis (TB) including cough. The aims of the present study were to evaluate the in vitro anti-TB activity of different solvent partitions of these plants, to identify the phytochemical compounds, and to assess the effects of the most active partitions on the growth kinetics and cellular integrity of the tubercle organism.

    METHODS: The in vitro anti-TB activity of different solvent partitions of the plant materials was determined against M. tuberculosis H37Rv using a tetrazolium colorimetric microdilution assay. The phytochemical compounds in the most active partition of each plant were identified using gas chromatography-mass spectrometry (GC-MS) analysis. The effects of these partitions on the growth kinetics of the mycobacteria were evaluated over 7-day treatment period in a batch culture system. Their effects on the mycobacterial cellular integrity were observed under a scanning electron microscope (SEM).

    RESULTS: The respective n-hexane partition of C. speciosus, C. citratus, and T. coronaria exhibited the highest anti-TB activity with minimum inhibitory concentrations (MICs) of 100-200 μg/mL and minimum bactericidal concentration (MBC) of 200 μg/mL. GC-MS phytochemical analysis of these active partitions revealed that majority of the identified compounds belonged to lipophilic fatty acid groups. The active partitions of C. speciosus and T. coronaria exhibited high cidal activity in relation to time, killing more than 99% of the cell population. SEM observations showed that these active plant partitions caused multiple structural changes indicating massive cellular damages.

    CONCLUSIONS: The n-hexane partition of the plant materials exhibited promising in vitro anti-TB activity against M. tuberculosis H37Rv. Their anti-TB activity was supported by their destructive effects on the integrity of the mycobacterial cellular structure.

  19. Fulltext Antituberculosis: synthesis and antimycobacterial activity of novel benzimidazole derivatives
    Keng Yoon Y, Ashraf Ali M, Choon TS, Ismail R, Chee Wei A, Suresh Kumar R, et al.
    Biomed Res Int, 2013;2013:926309.
    PMID: 24381946 DOI: 10.1155/2013/926309
    A total of seven novel benzimidazoles were synthesized by a 4-step reaction starting from 4-fluoro-3-nitrobenzoic acid under relatively mild reaction conditions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H₃₇Rv (MTB-H₃₇Rv) and INH-resistant M. tuberculosis (INHR-MTB) strains using agar dilution method. Three of them displayed good activity with MIC of less than 0.2 μM. Compound ethyl 1-(2-(4-(4-(ethoxycarbonyl)-2-aminophenyl)piperazin-1-yl)ethyl)-2-(4-(5-(4-fluorophenyl)pyridin-3-ylphenyl-1H-benzo[d]imidazole-5-carboxylate (5 g) was found to be the most active with MIC of 0.112 μM against MTB-H₃₇Rv and 6.12 μM against INHR-MTB, respectively.
  20. Assessment of radioactivity level and associated radiological hazard in fertilizer from Dhaka
    Siraz MMM, Al Mahmud J, Alam MS, Rashid MB, Hossain Z, Osman H, et al.
    Environ Monit Assess, 2024 Jan 23;196(2):192.
    PMID: 38263472 DOI: 10.1007/s10661-024-12328-4
    Miners, factory workers, traders, end-users, and foodstuff consumers all run the risk of encountering health hazards derived from the presence of elevated levels of radiation in fertilizers, as these groups often come into direct or indirect contact with fertilizers as well as raw materials throughout various linked processes such as mineral extractions, fertilizer production, agricultural practices. A total of 30 samples of various kinds of fertilizer produced in different factories in Dhaka megacity were analyzed to quantify the concentrations of primordial radionuclides using HPGe detector. Among the analyzed samples, average (range) concentration of 40K was found to be 9920 ± 1091 (8700 ± 957-11,500 ± 1265), 9100 ± 1001 (8600 ± 946-9600 ± 1056), 2565 ± 282 (2540 ± 279-2590 ± 285), and 3560 ± 392 (2620 ± 288-4500 ± 495) Bq/kg in the samples of Muriate of Potash Fertilizer, Sulphate of Potash Fertilizer, Humic Acid Fertilizer, and NPKS Fertilizer, respectively. Elevated concentration of 226Ra was found in Triple Super Phosphate Fertilizer with a mean (range) of 335 ± 37 (290 ± 32-380 ± 42) Bq/kg. The higher activity of 40K can be linked to the greater levels of elemental potassium in phosphate fertilizer. Elevated concentrations of radionuclides may also result from variations in chemical processes as well as the local geology of the mining areas where the raw materials were extracted for fertilizer production. Numerous fertilizer brands surpass prescribed limits for various hazardous parameters, presenting significant health risks to factory workers, farmers, and consumers of agricultural products. This study provides baseline information on the radioactivity of fertilizers, which could be used to develop mitigation methods, establish national fertilizer usage limits, justify regulatory frameworks, and raise public awareness of fertilizer overuse. The findings of the study could potentially help to explore the impact of fertilizer on the food chain.
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