Fenech; Tommasini, Atti della Societa Peloritana di Scienze Fisiche, Matematiche e Naturali, 1957, vol. 3, p. 279,291
作者:Fenech、Tommasini
DOI:——
日期:——
Optimization of Potent and Specific Trypanothione Reductase Inhibitors: A Structure-Based Drug Discovery Approach
作者:Theo Battista、Stefano Federico、Simone Brogi、Luca Pozzetti、Tuhina Khan、Stefania Butini、Anna Ramunno、Eleonora Fiorentino、Stefania Orsini、Trentina Di Muccio、Annarita Fiorillo、Cécile Exertier、Daniel Di Risola、Gianni Colotti、Sandra Gemma、Andrea Ilari、Giuseppe Campiani
DOI:10.1021/acsinfecdis.2c00325
日期:2022.8.12
inadequate, and there is an urgent need for better drugs. Trypanothionereductase (TR) represents a druggable target since it is essential for the parasite and not shared by the human host. Here, we report the optimization of a novel class of potent and selective LiTR inhibitors realized through a concerted effort involving X-ray crystallography, synthesis, structure–activity relationship (SAR) investigation