title: Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
abstract: A series of highly sterically hindered secondary amine analogues of pyridylmethylamine (7a-f, 8a-c) and positional isomeric analogues of ABT-594 (9a-c) were synthesized and evaluated for their in vivo analgesic activity. The compounds 7a and 7d show potent analgesic activity and lower toxicity. Some interesting structure-activity relationships have been revealed.
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100083, PR China.
authors.forename: Chuan-Xin
authors.initials: CX
authors.lastname: Zhang
authors.forename: Ze-Mei
authors.initials: ZM
authors.lastname: Ge
authors.forename: Tie-Ming
authors.initials: TM
authors.lastname: Cheng
authors.forename: Run-Tao
authors.initials: RT
authors.lastname: Li
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001384:Azetidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007536:Isomerism; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: C109763:5-(2-azetidinylmethoxy)-2-chloropyridine; D000700:Analgesics; D001384:Azetidines; D011725:Pyridines