title: Novel pyrimidines as acid pump antagonists (APAs).
abstract: A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H(+)/K(+) ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a potent APA with H(+)/K(+) ATPase, IC(50) = 52 nM.
authors.affiliation: Yuhan Research Institute, 416-1 Gongse-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-902, Republic of Korea.
authors.forename: Young Ae
authors.initials: YA
authors.lastname: Yoon
authors.forename: Chan Sun
authors.initials: CS
authors.lastname: Park
authors.forename: Myung Hun
authors.initials: MH
authors.lastname: Cha
authors.forename: Hyunho
authors.initials: H
authors.lastname: Choi
authors.forename: Jae Young
authors.initials: JY
authors.lastname: Sim
authors.forename: Jae Gyu
authors.initials: JG
authors.lastname: Kim
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005753:Gastric Mucosa / Q000201:enzymology; D017506:H(+)-K(+)-Exchanging ATPase / Q000378:metabolism; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007700:Kinetics; D054328:Proton Pump Inhibitors; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D004791:Enzyme Inhibitors; D007546:Isoquinolines; D054328:Proton Pump Inhibitors; D011743:Pyrimidines; D017506:H(+)-K(+)-Exchanging ATPase; C030986:pyrimidine