Novel pyrimidines as acid pump antagonists (APAs)

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 19, 2010, Pages 5735-5738

  Yoon, Young Ae ^a   Park, Chan Sun ^a   Cha, Myung Hun ^a   Choi, Hyunho ^a   Sim, Jae Young ^a   Kim, Jae Gyu ^a  

^a Yuhan Research Institute   (South Korea)

Author keywords

Acid pump antagonist (APA); Gastroesophageal reflux disease; H+ K+ ATPase; Ulcer

Indexed keywords

1 METHYL 1,2,3,4 TETRAHYDROISOQUINOLINE; 1,6 DIMETHYL 1,2,3,4 TETRAHYDROISOQUINOLINE; 2 METHYL 2 (4 FLUOROPHENYL)ETHYL; 4 FLUOROPHENYLCYCLOPROPYL; 7 METHOXY 1 METHYL 1,2,3,4 TETRAHYDROISOQUINOLINE; CARBON; HYDROGEN POTASSIUM ADENOSINE TRIPHOSPHATASE; PROTON PUMP INHIBITOR; PYRIMIDINE DERIVATIVE; REVAPRAZAN; UNCLASSIFIED DRUG;

ARTICLE; DRUG SYNTHESIS; IC 50; NONHUMAN; STOMACH MUCOSA; SWINE;

ANIMALS; ENZYME INHIBITORS; GASTRIC MUCOSA; H(+)-K(+)-EXCHANGING ATPASE; ISOQUINOLINES; KINETICS; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; SWINE;

EID: 77957577802     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.08.007     Document Type: Article

References (20)

1. J. Dent, H.B. El-Serag, M.A. Wallander, and S. Johansson Gut 54 2005 710
2. N. Bell, D. Burget, C. Howden, J. Wilkinson, and R. Hunt Digestion 51 1992 59
3. M. Robinson Eur. J. Gastroenterol. Hepatol. 13 2001 S43
4. G.N. Tytgat Eur. J. Gastroenterol. Hepatol. 13 2001 S29
5. G. Sachs, J.M. Shin, C. Briving, B. Wallmark, and S. Hersey Annu. Rev. Pharmacol. Toxicol. 35 1995 277
6. J.G. Hatlebakk, P.O. Katz, B. Kuo, and D.O. Castell Aliment. Pharmacol. Ther. 12 1998 1235
7. P.O. Katz, J.G. Hatlebakk, and D.O. Castell Aliment. Pharmacol. Ther. 14 2000 709
8. P.O. Katz, C. Anderson, R. Khoury, and D.O. Castell Aliment. Pharmacol. Ther. 12 1998 1231
9. K. Andersson, and E. Carlsson Pharmacol. Ther. 108 2005 294
10. Park, S.; Ahn, B.; Lee, B.; Kang, H.; Song, K. Gut, 2003, 52, Abstr. MON-G-008.
11. Park, S.; Song, K.; Moon, B. S.; Joo, S.; Choi, M.; Chung, I.; Sun, H. Gut, 2002, 51, Abstr. TUE-G-312.
12. K.S. Yu, K.S. Bae, J.H. Shon, J.Y. Cho, S.Y. Yi, J.Y. Chung, H.S. Lim, I.J. Jang, S.G. Shin, K.S. Song, and B.S. Moon J. Clin. Pharmacol. 44 2004 73
13. Park, S.; Lee, S.; Song, K.; Lee, B.; Kang, H.; Kang, J. Gut, 2003, 52, Gut, 2003, 52, Abstr. MON-G-009.
14. R.A. Moss, M. Wei, D.C. Merrer, and X. Song Tetrahedron Lett. 36 1995 8761
15. R.D. Larsen, R.A. Reamer, E.G. Corley, P. Davis, E.J.J. Grabowski, P.J. Reider, and I. Shinkai J. Org. Chem. 56 1991 6034
16. Hong, Y. W.; Lee, Y. N.; Kim, H. B. PCT Int. Appl., WO 1997042186A1, 1997.
17. Hong, Y. W.; Lee, Y. N.; Kim, H. B. PCT Int. Appl., WO 1998018784A1, 1998.
18. J. Sandosham, and K. Undheim Tetrahedron 50 1994 275
19. 50s of test compounds were calculated from each % inhibition value of compounds using the method described by Litchfield-Wilcoxon (Litchfield, J. T.; Wilcoxon, F. J. Pharmacol. Exp. Ther. 1949, 95).
20. +-ATPase activities were analyzed by Lineweaver-Burk plot.