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Synthesis of 1,3-diamino-7,8,9,10-tetrahydropyrido[3,2-f]-quinazolines. Inhibitors of Candida albicans dihydrofolate reductase as potential antifungal agents

✍ Scribed by Joseph H. Chan; David P. Baccanari; Robert L. Tansik; Christine M. Boytos; Sharon K. Rudolph; Andrew D. Brown; Jean S. Hong; Lee F. Kuyper; Michael L. Jones

Book ID: 102892166
Publisher: Journal of Heterocyclic Chemistry
Year: 1997
Tongue: English
Weight: 637 KB
Volume: 34
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.5570340123

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✦ Synopsis

Abstract

A series of novel 1,3‐diamino‐7,8,9,10‐tetrahydropyrido[3,2‐f]quinazolines were synthesized starting from 6‐amino‐5‐cyanoquinoline (4). These compounds inhibited Candida albicans dihydrofolate reductase with K~i~ values of ≤0.60 a__M.__ One analogue exhibited moderate in vivo efficacy in a C. albicans‐infected mouse model.

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