Chemical Biology Letters http://pubs.thesciencein.org/journal/index.php/cbl <p>Chemical Biology Letters is an interdisciplinary international research journal for publication of research advances in Medicinal Chemistry, Biochemistry, Biotechnology, Chemical Biology, Drug Discovery, Drug Delivery, and related fields for understanding biological phenomenon at molecular level.</p> en-US pubs@thesciencein.org (Editorial Manager) pubs@thesciencein.org (Technical Team) Mon, 14 Oct 2019 00:00:00 +0530 OJS 3.1.1.4 http://blogs.law.harvard.edu/tech/rss 60 Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors http://pubs.thesciencein.org/journal/index.php/cbl/article/view/111 <p>In this paper, we report the design, synthesis, <em>in-silico</em>, and <em>in-vitro</em> evaluations of a series of coumarin-phenylthiazole conjugates to inhibit cholinesterase enzymes. The coumarin and phenylthiazole derivatives have been synthesized separately, and further combined through covalent amine bond linkage. The synthesized compounds showed more inhibition towards BuChE than AChE, where 4-(3-bromophenyl)-1,3-thiazol-2-amine (<strong>7i</strong>) exhibited the strongest inhibition against BuChE with an IC<sub>50</sub> value of 3.54 μM. For the conjugates, 3-{2-[4-(3-nitrophenyl)thiazol-2-ylamino]acetyl}chromen-2-one (<strong>8j</strong>) exhibited strongest inhibition with an IC50 value of 46.47 μM.&nbsp; The better inhibition activities towards BuChE are also shown by 3-bromo and 2-fluoro derivatives. It was also observed that the substitution at 3-position, on phenylthiazole moiety produced better results against BuChE than 4-substituted counterparts.</p> Deepak Mishra, Atiya Fatima, Ram Singh, Nupur S Munjal, Vineet Mehta, Udayabanu Malairaman ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/111 Mon, 14 Oct 2019 00:00:00 +0530 Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3 http://pubs.thesciencein.org/journal/index.php/cbl/article/view/113 <p>Coumarin, triazoles and thiazolidinones are one of the most preferred and high valued scaffolds frequently used in medicinal chemistry. The synthesis of newly designed coumarin based triazolyl-thiazolidinones was performed and new compounds were obtained in good yields. The listed compounds were evaluated for their apoptotic activity and determined the minimal inhibitory concentrations for each of the compound on SCC-4 cells using MTT viability test. Furthermore, apoptotic inducer activity was assayed by detecting the expression of caspase-3, a key apoptotic enzyme.</p> Pooja FNU, Nimisha Sinha, Sonu Kumar, Atul FNU, Sumit Kumar, Prashant Kumar, Abhishek Pandey, Pragya Sharma, Vithika Aggarwal, Poonam FNU, Poonam Mothsra, Brajendra Kumar Singh, Rishi Pal Singh, Yogesh Kumar ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/113 Mon, 11 Nov 2019 00:00:00 +0530 Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity http://pubs.thesciencein.org/journal/index.php/cbl/article/view/107 <p>Selected novel β-lactam and thiazolidinone derivatives have been synthesized by the reaction of 4-methyl-1H-isochromen-1-one with 1,1-biphenyl-4,4-diamine, followed by the reaction with substituted benzaldehyde and further by the reaction with chloroacetyl chloride (for β-lactam type) and with thioglycolic acid (for thiazolidinone type) respectively . All the compounds were characterised by <sup>1</sup>H NMR, IR and mass spectroscopy. These compounds were screened for in-vitro antimicrobial activity against <em>Staphylococus aureus</em>, <em>E. coli</em>, <em>Pseudomonas aeruginosa</em> strain. Some compounds have shown very good efficacy against antibacterial strain</p> Ashish Bhatt, Krishna Srivastava, Ravi Kant, Deepa Lakhmani ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/107 Tue, 12 Nov 2019 00:00:00 +0530 Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice http://pubs.thesciencein.org/journal/index.php/cbl/article/view/115 <p>The present study investigated the effect of monocrotophos, a commonly used organophosphate pesticide exposure in the kidney tissues of the swiss albino mice. Monocrotophos was administered at the sub-lethal doses of 1.25mg/kg, 2.5 mg/kg and 5.0 mg/kg body weight for 24 hr. Monocrotophos toxicity generated oxidative stress in the mice as evidenced by significant decrease in the activities of glutathione, superoxide dismutase and catalase enzymes. The exposure increased the lipid peroxidation and protein oxidation in a dose dependent manner. Oxidative stress generation also elicited cytotoxic effects on the mice kidney which were supported by the histopathological changes like degeneration in glomerulus, bowmen’s capsule and tubules, hemorrhage, mononuclear cell infiltration, tubular cast and congested blood vessels in a dose-dependent manner. In conclusion, the study indicated that monocrotophos exposure at various doses induces significant deleterious health effects in mice kidney tissues via oxidative stress generation.</p> Suman Devi, Jagjeet Singh, Vijay Kumar, Vinay Malik ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/115 Mon, 14 Oct 2019 00:00:00 +0530 Synthesis and toxicological screening of novel organobismuth compounds http://pubs.thesciencein.org/journal/index.php/cbl/article/view/104 <p>Perfluoroorganobismuth compounds scanned first time for biological and toxicological activity. They exhibit significant antibacterial activity against pathogenic bacteria viz., <em>Pseudomonas aeruginosa</em>, <em>Staphylococcus aureus</em>, <em>Klebsiela pneumonia</em> and remarkable antifungal activity against <em>Aspergillus flavus</em> and <em>Aspergillus nigar</em> along with insecticidal activity against <em>Periplanata americana,</em> <em>Musca domestica</em> and <em>Spodoptera litura</em> and <em>Tetranychus</em> species of mites. The compounds were found highly active against <em>Spodoptera litura</em>. The studies suggest that these compounds are better biocidal as compared to corresponding phenyl analogues.</p> Ashish Bhatt, Ravi Kant, Krishna Srivastava ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/104 Mon, 25 Nov 2019 00:00:00 +0530