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) Tue, 04 Jun 2019 17:40:26 +0530 OJS 3.1.1.4 http://blogs.law.harvard.edu/tech/rss 60 Chemical libraries targeting Liver Stage Malarial infection http://pubs.thesciencein.org/journal/index.php/cbl/article/view/96 <p>Despite the noteworthy advances in the use of chemotherapy for malaria, it continues to constantly affect large number of individuals. New molecules capable of blocking life-cycle of the parasite, preferably through targeting novel pathways and various modes of action, are increasingly becoming area of interest. Phenotypic screening of large chemical libraries is certainly one of the important criteria for the discovery of new and effective drugs. In recent years, diverse research groups including pharmaceutical industries have performed this large-scale phenotypic screening to identify the potential drug molecules. Most of the antimalarial drugs target blood-stage malarial infection and remain either less potent or ineffective against other life stages i.e. liver-stage, and the gametocyte stages of the parasite. Although, liver stage is considered as a crucial drug target, limited clinical options have significantly hampered the discovery of effective treatments. This short review presents the collection of selective molecules targeting specifically liver stage malaria parasites.</p> Neha Sharma, Abhishek Verma, Poonam FNU, Prakasha Kempaiah, Brijesh Rathi ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/96 Sun, 30 Jun 2019 00:00:00 +0530 Formulation optimization of multicomponent aqueous coground mixtures of Meloxicam for dissolution enhancement http://pubs.thesciencein.org/journal/index.php/cbl/article/view/93 <p>In present work, the role of various formulation excipients for dissolution enhancement of a BCS Class II drug, meloxicam was studied by formulating multicomponent aqueous coground mixtures using lactose, microcrystalline cellulose and three solubilizers; polyethylene glycol 400, propylene glycol and polyvinyl pyrrolidone. A 3<sup>3</sup> full factorial design was employed using solubilizers’ concentrations as independent variables whereas angle of repose and <em>in vitro</em> drug dissolution as dependent variables in order to optimize the amounts of solubilizers. The results revealed more than fivefold increase in drug dissolution in some experimental batches compared to that of pure drug powder. Full and reduced models were evolved for the dependent variables and the reduced models were further validated using extra design check points. The studies suggested that the incorporation of optimized amounts of solubilizers could be successfully employed for achieving desired flow properties and enhanced drug dissolution of poorly water soluble meloxicam. The method emerged as a simple, cost-effective, and organic solvent-free green approach toward formulation development of meloxicam and may also be applied to other limited water-soluble drugs.</p> Sunita Dahiya, Atul Kaushik, Kamla Pathak ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/93 Tue, 04 Jun 2019 17:42:11 +0530 Synthesis, DNA photocleavage, molecular docking and anticancer studies of 2-methyl-1,2,3,4-tetrahydroquinolines http://pubs.thesciencein.org/journal/index.php/cbl/article/view/97 <p>2-Methyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-ones (<strong>3a−g</strong>) were synthesized by one pot multicomponent aza Diels-alder reaction between <em>N</em>-arylimines with two molecules of <em>N</em>-vinyl-2-pyrrolidinone in presence of Sm(III)nitrate as catalyst in acetonitrile solvent at room temperature stirring. The photocleavage studies with 2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-ones (<strong>3a−g</strong>) revealed that almost all derivatives exhibited effective photocleavage of pUC−19 DNA at 365 nm, The The anticancer activities of newly synthesized compounds (3a−g) were more potent than doxorubicin on MCF−7 cells. The docking of PBR receptor (1EQ1) protein with newly synthesized THQ’s (<strong>3a-g</strong>) exhibited well established bonds with one or more amino acids in the receptor active pocket.</p> P.J. Bindu, T. R. Ravikumar Naik, K.M. Mahadevan, G. Krishnamurthy ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/97 Tue, 04 Jun 2019 00:00:00 +0530