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N-(2,4-diaminopteridin-6-yl)-methyl-dibenz[b,f]azepine

Development stage: Discontinued
Modality: Small Molecules

Overview

N-(2,4-diaminopteridin-6-yl)-methyl-dibenz[b,f]azepine is an experimental small molecule inhibitor designed as a selective antifolate. It acts by inhibiting dihydrofolate reductase (DHFR), with high selectivity for the DHFR enzymes of Pneumocystis carinii and Toxoplasma gondii over mammalian DHFR. This selectivity is attributed to its bulky dibenzoazepine moiety fitting into unique regions of the microbial enzyme active sites not present in mammalian counterparts. The compound has been studied as a potential lead for developing antiparasitic agents targeting opportunistic infections in immunocompromised patients[7][8].

Other names: [N-(2,4-DIAMINOPTERIDIN-6-YL)-METHYL]-DIBENZ[B,F]AZEPINEN-((2,4-diaminopteridin-6-yl)methyl)dibenz(b,f)azepine6-(5H-dibenz[b,f]azepin-5-ylmethyl)-2,4-pteridinediamine6-(benzo[b][1]benzazepin-11-ylmethyl)pteridine-2,4-diamine

Targets

DHFR (Dihydrofolate reductase)

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