150869-41-3Relevant articles and documents
Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors
Capkova, Katerina,Yoneda, Yoshiyuki,Dickerson, Tobin J.,Janda, Kim D.
, p. 6463 - 6466 (2008/04/02)
Botulinum neurotoxins are the most toxic proteins currently known. Based on a recently identified potent lead structure, 2,4-dichlorocinnamic acid hydroxamate, herein we report on the structure-activity relationship of a series of hydroxamate BoNT/A inhibitors. Among them, 2-bromo-4-chlorocinnamic acid hydroxamate, 2-methyl-4-chlorocinnamic acid hydroxamate, and 2-trifluoromethyl-4-chlorocinnamic acid hydroxamate displayed comparable inhibitory activity to that of the lead structure.
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists
Xie, Yun Feng,Lake, Kirk,Ligsay, Kathleen,Komandla, Mallareddy,Sircar, Ila,Nagarajan, Gobi,Li, Jian,Xu, Kui,Parise, Jason,Schneider, Lisa,Huang, Ding,Liu, Juping,Dines, Kevin,Sakurai, Naoki,Barbosa, Miguel,Jack, Rick
, p. 3367 - 3372 (2008/02/07)
Design and synthesis of a series of 3-amino-4-(2-(2-(4-benzylpiperazin-1-yl)-2-oxoethoxy)phenylamino)cyclobutenedione derivatives as novel CCR1 antagonists are described. Structure-activity relationship studies led to the identification of compound 22, which demonstrated potent binding activity, functional antagonism of CCR1 as well as good species cross-reactivity. In addition, compound 22 also showed desirable pharmacokinetic profiles and was selected for in vivo studies in the mouse collagen-induced arthritis model.