title: Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.
abstract: A novel series of CCR5 antagonists has been identified, utilizing the lead, nifeviroc, which were further modified based on bioisosteric principles. Lead optimization was pursued by balancing potential toxicity and potency. Potent analogues with low toxic properties were successfully developed by formation of urea and amide bonds at the nitrogen at position 4- of the pyrrolidine ring.
authors.affiliation: Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 319 Yueyang Lu, Shanghai 200031, China.
authors.forename: Li
authors.initials: L
authors.lastname: Ben
authors.forename: Eric Dale
authors.initials: ED
authors.lastname: Jones
authors.forename: Enkun
authors.initials: E
authors.lastname: Zhou
authors.forename: Chen
authors.initials: C
authors.lastname: Li
authors.forename: Dean Cameron
authors.initials: DC
authors.lastname: Baylis
authors.forename: Shanghai
authors.initials: S
authors.lastname: Yu
authors.forename: Miao
authors.initials: M
authors.lastname: Wang
authors.forename: Xing
authors.initials: X
authors.lastname: He
authors.forename: Jonathan Alan Victor
authors.initials: JA
authors.lastname: Coates
authors.forename: David Ian
authors.initials: DI
authors.lastname: Rhodes
authors.forename: Gang
authors.initials: G
authors.lastname: Pei
authors.forename: John Joseph
authors.initials: JJ
authors.lastname: Deadman
authors.forename: Xin
authors.initials: X
authors.lastname: Xie
authors.forename: Dawei
authors.initials: D
authors.lastname: Ma
mesh_terms: D000818:Animals; D065100:CCR5 Receptor Antagonists; D016466:CHO Cells; D018938:Caco-2 Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D011759:Pyrrolidines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D065100:CCR5 Receptor Antagonists; D011759:Pyrrolidines