The synthesis of 2, 5-bis (4-amidinophenyl) thiophene derivatives providing submicromolar-range inhibition of the botulinum neurotoxin serotype A metalloprotease

…, LM Gomba, D Opsenica, JC Burnett, R Gussio…

Index: Opsenica, Igor; Filipovic, Vuk; Nuss, Jon E.; Gomba, Laura M.; Opsenica, Dejan; Burnett, James C.; Gussio, Rick; Solaja, Bogdan A.; Bavari, Sina European Journal of Medicinal Chemistry, 2012 , vol. 53, p. 374 - 379

Full Text: HTML

Citation Number: 11

Abstract

Botulinum neurotoxins (BoNTs), composed of a family of seven serotypes (categorized A– G), are the deadliest of known biological toxins. The activity of the metalloprotease, light chain (LC) component of the toxins is responsible for causing the life-threatening paralysis associated with the disease botulism. Herein we report significantly more potent analogs of novel, lead BoNT serotype A LC inhibitor 2, 5-bis (4-amidinophenyl) thiophene (Ki= 10.88 ...