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N-[(1S)-2-methyl-1-(pyridin-4-ylcarbamoyl)propyl]cyclohexanecarboxamide

Development stage
Preclinical
Lead developer
University of California, San Francisco
Modality
Small Molecules
01

Overview

N-[(1S)-2-methyl-1-(pyridin-4-ylcarbamoyl)propyl]cyclohexanecarboxamide is a synthetic small molecule belonging to the class of n-acyl-alpha amino acid derivatives. It was identified as an inhibitor of sterol 14alpha-demethylase (CYP51), a cytochrome P450 enzyme involved in sterol biosynthesis. The compound was discovered through screening efforts targeting Mycobacterium tuberculosis CYP51 and later shown to inhibit the orthologous enzyme in Trypanosoma cruzi, the causative agent of Chagas disease. In vitro studies demonstrated potent and selective anti-T. cruzi activity, suggesting its potential as a lead compound for antiparasitic drug development[7][8]. Its mechanism involves binding to and inhibiting CYP51, thereby disrupting membrane sterol biosynthesis essential for parasite survival.

Other names
(2S)-2-(cyclohexylformamido)-3-methyl-N-(pyridin-4-yl)butanamideN-[(2S)-3-Methyl-1-oxo-1-(4-pyridinylamino)-2-butanyl]cyclohexanecarboxamide
02

Targets

CYP51A1 (Sterol 14α-demethylase)

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