Implications of N-capped urea/thiourea and C-capped 3-(1-piperazinyl)-1,2-benzisothiazole with bridging Gly-Val/Phe-Gly-Val-Pro as therapeutic targets

Sharma, A. and Suhas, R. and Banu, S. H. and Chandrashekar, S. and Channe Gowda, D. (2014) Implications of N-capped urea/thiourea and C-capped 3-(1-piperazinyl)-1,2-benzisothiazole with bridging Gly-Val/Phe-Gly-Val-Pro as therapeutic targets. European Journal of Medicinal Chemistry, 87. pp. 657-661. ISSN 0223-5234

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Abstract

A series of urea/thiourea derivatives were synthesized by using peptides conjugated to 3-(1-piperazinyl)-1,2-benzisothiazole and their structure was characterized by analytical and spectral (1H, 13C NMR and Mass) methods. These compounds were screened for antimicrobial and antiglycating activity as well as urease and H+/K+-ATPase inhibition. Preliminary structure-activity relationship studies revealed that the compounds possessing fluoro moiety were excellent antimicrobial agents. Furthermore, for other biological activities methoxy substituent was found to be the most active particularly upon substitution at para position.

Item Type:	Article
Uncontrolled Keywords:	Article, carbon nuclear magnetic resonance, drug synthesis, IC50, mass spectrometry, nonhuman, proton nuclear magnetic resonance, structure activity relation, unclassified drug, drug structure, antibacterial activity, antifungal activity, antifungal agent, antiinfective agent, Aspergillus niger, Escherichia coli, Fusarium oxysporum, Klebsiella pneumoniae, scanning electron microscopy, enzyme activity, proton pump inhibitor, 1, enzyme inhibition, hydrogen bond, minimum inhibitory concentration, biological activity, carbendazim, streptomycin, drug activity, Aspergillus flavus, phenylalanine, thiourea derivative, urea derivative, thiourea, 2 benzisothiazole, 2 benzisothiazole derivative, 3 (1 piperazinyl) 1, antiglycating activity, coagulase positive Staphylococcus, conjugate, derivatization, fungus growth, Fusarium moniliforme, glycine, omeprazole, plasma protein binding, proline, rutoside, urease inhibitor, valine, Xanthomonas oryzae
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Arshiya Kousar Library Assistant
Date Deposited:	31 Aug 2019 10:01
Last Modified:	31 Aug 2019 10:01
URI:	http://eprints.uni-mysore.ac.in/id/eprint/4281

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