http://pubs.thesciencein.org/journal/index.php/cbl/issue/feed Chemical Biology Letters 2019-06-26T16:41:10+0530 Editorial Manager pubs@thesciencein.org Open Journal Systems <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> http://pubs.thesciencein.org/journal/index.php/cbl/article/view/93 Formulation optimization of multicomponent aqueous coground mixtures of Meloxicam for dissolution enhancement 2019-06-04T17:49:20+0530 Sunita Dahiya sunita.dahiya@upr.edu Atul Kaushik abhi_atul2008@rediffmail.com Kamla Pathak kamlapathak5@gmail.com <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> 2019-06-04T17:42:11+0530 ##submission.copyrightStatement## http://pubs.thesciencein.org/journal/index.php/cbl/article/view/97 Synthesis, DNA photocleavage, molecular docking and anticancer studies of 2-methyl-1,2,3,4-tetrahydroquinolines 2019-06-26T16:41:10+0530 P.J. Bindu bindu12_naik@rediffmail.com T. R. Ravikumar Naik naikravi7@gmail.com K.M. Mahadevan kmmahadevan@gmail.com G. Krishnamurthy gkmnaiksahyadri@gmail.com <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> 2019-06-04T00:00:00+0530 ##submission.copyrightStatement##