Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 47, Issue 14, Pages 3689-3692Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0306327
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Funding
- NIAID NIH HHS [AI 47759, AI 44661, AI 41743] Funding Source: Medline
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2,4-Diamino-5-methyl-6-(substituted-phenyl)thiopyrrolo[2,3-d]pyrimidines 4-11 were synthesized as dihydrofolate reductase (DHFR) inhibitors against opportunistic pathogens that afflict patients with AIDS. Synthesis was achieved from 2,4-diamino-5-methypyrrolo[2,3-d]pyrimidine and substituted phenylthiols under modified conditions reported by Gangjee et al. Some of these compounds were potent and selective against DHFR from both Toxoplasma gondii and Mycobacterium avium compared to mammalian DHFR. Compound 11 with a 1-naphthyl substituent is 16-fold more potent and equally selective against Toxoplasma gondii DHFR as the clinically used trimethoprim.
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