2-(4-Pyridyl)-delta 2-1,3,4-oxadiazolines from isonicotinoylhydrazones and diazomethane as potential antimycobacterial and anti-HIV agents. V. NLM AIDSLINE Important note: Information in this article was accurate in 1996. The state of the art may have changed since the publication date.

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2-(4-Pyridyl)-delta 2-1,3,4-oxadiazolines from isonicotinoylhydrazones and diazomethane as potential antimycobacterial and anti-HIV agents. V.

Farmaco. 1995 Nov;50(11):783-6. Unique Identifier : AIDSLINE MED/96153906
Vigorita MG; Ottana R; Zappala C; Maccari R; Pizzimenti FC; Gabbrielli G; Dipartimenti Farmaco-chimico, Universita di Messina, Italy.

Abstract: The 5-aryl-4-methyl-2-(4-pyridyl)-delta 2-1,3,4-oxadiazolines 3, previously synthesized along with isomer 4-aryl-1-methoxy-1-(4-pyridyl)-2,3-diaza-1,3-butadienes 2 from benzaldehyde isonicotinoylhydrazones and diazomethane, were tested for in vitro activity against both M. tuberculosis and some atypical mycobacterial strains as well as against human immunodeficiency virus (HIV-1). Some halophenyl derivatives, 3e, 3g, 3i, 3j, were found to display MIC ranges from 1 to 10 (micrograms/ml against H 37 Rv and a clinical isolate tubercular strain, whereas against M. avium (MAC) the MICs were higher than 20 micrograms/ml. When the combinations of oxadiazolines with ethambutol, acting as inhibitor of cell wall synthesis, were assayed on MAC strain a synergistic effect was demonstrated for 3g and 3h trifluoromethyl derivatives. The antimycobacterial profiles of 2 and 3 analogues are compared and discussed. As shown by compounds 2, no substantial anti-HIV in vitro activity was found in selected delta 2-oxadiazolines; a moderate cytotoxicity, however, appears to be a common property.
Keywords: Anti-Infective Agents/*CHEMICAL SYNTHESIS/PHARMACOLOGY Antiviral Agents/*CHEMICAL SYNTHESIS/PHARMACOLOGY Cell Wall/DRUG EFFECTS/METABOLISM Human HIV-1/*DRUG EFFECTS Mycobacterium/*DRUG EFFECTS Support, Non-U.S. Gov't JOURNAL ARTICLE

KWDanti-infectiveagents/KWDchemicalsynthesis/pharmacologyantiviralagents/KWDchemicalsynthesis/pharmacologycellwall/drugeffects/metabolismhumanhiv-1/KWDdrugeffectsmycobacterium/KWDdrugeffectssupport,non-uKWDsKWDgov'tjournalarticle
960630
M9660728

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