title: 5,6,7-trisubstituted 4-aminopyrido[2,3-d]pyrimidines as novel inhibitors of adenosine kinase.
abstract: The synthesis and structure-activity relationship of a series of 5,6,7-trisubstituted 4-aminopyrido[2,3-d]pyrimidines as novel nonnucleoside adenosine kinase inhibitors is described. A variety of alkyl, aryl, and heteroaryl substituents were found to be tolerated at the C5, C6, and C7 positions of the pyridopyrimidine core. These studies have led to the identification of analogues that are potent inhibitors of adenosine kinase with in vivo analgesic activity.
authors: Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064-6115, USA. richard.j.perner@abbott.com
authors: Richard J
authors: RJ
authors: Perner
authors: Yu-Gui
authors: YG
authors: Gu
authors: Chih-Hung
authors: CH
authors: Lee
authors: Erol K
authors: EK
authors: Bayburt
authors: Jeffery
authors: J
authors: McKie
authors: Karen M
authors: KM
authors: Alexander
authors: Kathy L
authors: KL
authors: Kohlhaas
authors: Carol T
authors: CT
authors: Wismer
authors: Joe
authors: J
authors: Mikusa
authors: Michael F
authors: MF
authors: Jarvis
authors: Elizabeth A
authors: EA
authors: Kowaluk
authors: Shripad S
authors: SS
authors: Bhagwat
mesh_terms: D000248:Adenosine Kinase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D045744:Cell Line, Tumor; D006801:Humans; D051379:Mice; D010147:Pain Measurement; D010766:Phosphorylation; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D011725:Pyridines; D011743:Pyrimidines; D000248:Adenosine Kinase