Novel pyrimidines as acid pump antagonists (APAs).
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.
Yoon
Young Ae
YA
Yuhan Research Institute, 416-1 Gongse-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-902, Republic of Korea.
Park
Chan Sun
CS
Cha
Myung Hun
MH
Choi
Hyunho
H
Sim
Jae Young
JY
Kim
Jae Gyu
JG
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
D004791:Enzyme Inhibitors; D007546:Isoquinolines; D054328:Proton Pump Inhibitors; D011743:Pyrimidines; D017506:H(+)-K(+)-Exchanging ATPase; C030986:pyrimidine