title: A class of novel conjugates of substituted purine and Gly-AA-OBzl: synthesis and evaluation of orally analgesic activity.
abstract: Aimed at the chemotherapy of chronic pain two kinds of analgesic pharmacophores, substituted purine and Gly-AA-OBzl, were coupled via a five-step-reaction procedure and 19 novel conjugates N-[2-chloro-9-(tetrahydropyran-2-yl)-9H-purin-6-yl]-N-cyclopropylglycylamino acid benzylesters were provided. On mouse-tail flick model their in vivo analgesic activities were assayed. The results indicate that introducing Gly-OC(2)H(5) into the 6-position of the substituted purine leads to ambiguous increase of the analgesic activity, while introducing Gly-AA-OBzl into this position leads to significant increase of the analgesic activity.
authors.affiliation: College of Pharmaceutical Sciences, Peking University, Beijing, PR China.
authors.forename: Guifeng
authors.initials: G
authors.lastname: Kang
authors.forename: Ming
authors.initials: M
authors.lastname: Zhao
authors.forename: Xiaoyi
authors.initials: X
authors.lastname: Zhang
authors.forename: Li
authors.initials: L
authors.lastname: Peng
authors.forename: Chunbo
authors.initials: C
authors.lastname: Li
authors.forename: Wei
authors.initials: W
authors.lastname: Mao
authors.forename: Weidong
authors.initials: W
authors.lastname: Ye
authors.forename: Shiqi
authors.initials: S
authors.lastname: Peng
mesh_terms: D000284:Administration, Oral; D000700:Analgesics / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D000818:Animals; D002908:Chronic Disease; D005998:Glycine / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D008297:Male; D051379:Mice; D010146:Pain / Q000188:drug therapy*; D011687:Purines / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D021281:Quantitative Structure-Activity Relationship
chemical_list: D000700:Analgesics; D011687:Purines; D005998:Glycine