SYNTHESIS AND ANTIBACTERIAL EVALUATION OF NOVEL HETEROCYCLIC COMPOUNDS
Journal: Indian Journal of Medical Research and Pharmaceutical Sciences (Vol.7, No. 1)Publication Date: 2020-01-30
Authors : Kpail Tiwari; Pramod Kumar Saxena;
Page : 32-43
Keywords : cyanoacetylhydrazide; QSAR; sulfonamide; pyridazines; pyrazoles; oxazole; pyrimidines.;
Abstract
The work describes QSAR and SAR studies on the reserve transcriptase inhibitor by using the 2D-topological, physicochemical and hydrophobic parameters along with the indicator parameters. For the synthesis of new heterocyclic compounds containing a sulfonamido moiety suitable for use as antibacterial agents, the precursor ethyl {[4- N-(4,6- dimethylpyrimidin-2-yl)sulfamoyl] phenylazo}cyanoacetate was reacted with a variety of active methylene compounds producing pyran, pyridine and pyridazine derivatives. Also, the reactivity of the precursor hydrazone towards hydrazine derivatives to give pyrazole and oxazole derivatives was studied. On the other hand, treatment of the same precursor with urea, thiourea and/or guanidine hydrochloride furnished pyrimidine and thiazine derivatives, respectively. The newly synthesized compounds were tested for antibacterial activity, whereby eight compounds were found to have highactivities
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Last modified: 2020-01-20 21:39:37