Design and Synthesis of Novel Imidazole-Substituted Dipeptide Amides as Potent and Selective Inhibitors of Candida albicans MyristoylCoA:Protein N-Myristoyltransferase and Identification of Related Tripeptide Inhibitors with Mechanism-Based Antifungal Activity

A new class of antifungal agents has been discovered which exert their activity by blockade of myristoylCoA:protein N-myristoyltransferase (NMT; EC 2.1.3.97). Genetic experiments have established that NMT is needed to maintain the viability of Candida albicans and Cryptococcus neoformans, the two pr...

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Veröffentlicht in:	Journal of medicinal chemistry 1997-08, Vol.40 (16), p.2609-2625
Hauptverfasser:	Devadas, Balekudru, Freeman, Sandra K, Zupec, Mark E, Lu, Hwang-Fun, Nagarajan, Srinivasan R, Kishore, Nandini S, Lodge, Jennifer K, Kuneman, David W, McWherter, Charles A, Vinjamoori, Dutt V, Getman, Daniel P, Gordon, Jeffrey I, Sikorski, James A
Format:	Artikel
Sprache:	eng
Schlagworte:	Acyltransferases - antagonists & inhibitors Acyltransferases - genetics Amides - chemical synthesis Amides - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Antifungal Agents - chemical synthesis Antifungal Agents - pharmacology Biological and medical sciences Candida albicans - enzymology Chromatography, High Pressure Liquid Dipeptides - chemical synthesis Dipeptides - pharmacology Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Humans Imidazoles - chemical synthesis Imidazoles - pharmacology Kinetics Medical sciences Models, Chemical Molecular Mimicry Pharmacology. Drug treatments Stereoisomerism Structure-Activity Relationship
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