Novel 1,3,5-triphenyl-2-pyrazolines as anti-infective agents

Sivakumar, P M and Prabhu Srinivasan, S and Kumar, Vanaja and Doble, Mukesh (2010) Novel 1,3,5-triphenyl-2-pyrazolines as anti-infective agents. Bioorganic and Medicinal Chemistry Letters, 2010. pp. 3160-3172. ISSN 0960-894X

Archive 201029.pdf - Published Version Restricted to Repository staff only Download (219kB) | Request a copy

Abstract

Sixteen 1,3,5-triphenyl-2-pyrazolines were synthesized and their anti-infective activities (against Mycobacterium tuberculosis H37Rv, six bacterial and four fungal strains) were tested. Only compound with SO2CH3 in the para position of the A-ring was active against the tubercular strain at 100 lg/ml concentration. All compounds showed good anti infective activity against Escherichia coli and poor activity against Staphylococcus aureus. Compounds 4, 12, 13 and 14 exhibited reasonable activity against all the organisms tested (<0.309 lM except against S. aureus. The activity of these compounds correlated with their lipophilic/hydrophilic nature. Compounds 4, 10 and 16 showed very good activity (>88% reduction) against four fungi studied at 2 mg/ml. All these compounds possess halogen substitutions. Compound 11 showed very high activity (>90%) against three fungi. Majority of the compounds showed more than 90% inhibition against one or two fungi. Since pyrazolines are reported to inhibit the activity of p-glycoprotein, they may prevent drug resistance developed by microorganism.

Affiliation:	ICMR-National Institute for Research in Tuberculosis
Item Type:	Article
Uncontrolled Keywords:	1,3,5-Triphenyl-2-pyrazolines Alog P Mycobacterium tuberculosis H37Rv High resolution mass spectrum (HR-MS)
Subjects:	Tuberculosis > Laboratory Research > Bacteriological
Divisions:	Basic Science Research > Bacteriology
Depositing User:	Dr. Rathinasabapati R
Date Deposited:	13 May 2022 09:15
Last Modified:	25 May 2022 10:56
URI:	http://eprints.nirt.res.in/id/eprint/1045

Actions (login required)

View Item