Molecular Design, Synthesis and Trypanocidal Activity of Dipeptidyl Nitriles as Cruzain Inhibitors.

• Main Authors: Leandro A A Avelar (Author), Cristian D Camilo (Author), Sérgio de Albuquerque (Author), William B Fernandes (Author), Cristiana Gonçalez (Author), Peter W Kenny (Author), Andrei Leitão (Author), James H McKerrow (Author), Carlos A Montanari (Author), Erika V Meñaca Orozco (Author), Jean F R Ribeiro (Author), Josmar R Rocha (Author), Fabiana Rosini (Author), Marta E Saidel (Author)
• Format: Book
• Published: Public Library of Science (PLoS), 2015-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

A series of compounds based on the dipeptidyl nitrile scaffold were synthesized and assayed for their inhibitory activity against the T. cruzi cysteine protease cruzain. Structure activity relationships (SARs) were established using three, eleven and twelve variations respectively at the P1, P2 and...