Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes
التفاصيل البيبلوغرافية
العنوان:
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes
Screening of the Merck sample collection for compounds with CCR5 receptor binding afforded (2 S )-2-(3,4-dichlorophenyl)-1-[ N -(methyl)- N -(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4′-piperidin-1′-yl)]butane S -oxide ( 4 ) as a potent lead structure having an IC 50 binding affinity of 35 nM. Herein, we describe the discovery of this lead structure and our initial structure–activity relationship studies directed toward the requirement for and optimization of the 1-amino fragment.