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Novel 2-hydrazino-pyrimidin-4(3H)-one derivatives as potential dihydrofolate reductase inhibitors

✍ Scribed by Mariam S. Degani; Seema Bag; Ranjeet Bairwa; Nilesh R. Tawari; Sherry F. Queener

Book ID: 102342041
Publisher: Journal of Heterocyclic Chemistry
Year: 2010
Tongue: English
Weight: 101 KB
Volume: 47
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.216

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✦ Synopsis

Abstract

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Novel substituted 2‐hydrazino‐pyrimidin‐4(3__H__)‐one derivatives were synthesized and examined for their antifolate activity against DHFR from Pneumocystis carinii (pc), Toxoplasma gondii (tg), Mycobacterium avium (ma), and rat liver (rl). A novel, simple, and feasible methodology was developed for the synthesis of the titled compounds. Amongst these, compound 8 6‐phenyl‐2‐(2‐(1‐(thiophen‐2‐yl) ethylidene)hydrazinyl) pyrimidin‐4(3__H__)‐one exhibited 17.74 μ__M__ activity against pcDHFR. J. Heterocyclic Chem., (2010).

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