Ife, Robert J.; Brown, Thomas H.; Blurton, Peter; Keeling, David J.; Leach, Colin A.; Meeson, Malcolm L.; Parsons, Michael E.; Theobald, Colin J. published the artcile< Reversible Inhibitors of the Gastric (H+/K+)-ATPase. 5. Substituted 2,4-Diaminoquinazolines and Thienopyrimidines>, Related Products of 18740-39-1, the main research area is quinazolinamine thienopyrimidinamine quinazolinediamine.
Quinazolines bearing a secondary [4-(arylamino)] substituent demonstrate a structure-activity relationship for inhibition of the gastric (H+/K+)-ATPase different from the previously described 3-acylquinolines, suggesting that, although these compounds are also K+-competitive, they probably bind to the enzyme in a different orientation. Compounds bearing a tertiary 4-(arylamino) substituent, however, in particular 4-(N-methylarylamino), appear to possess an structure-activity relationship quite similar to the 3-acylquinolines. Compounds possessing both a 4-(N-methylarylamino) substituent and a 2-(arylamino) substituent proved to be very potent, K+-competitive inhibitors of K+-stimulated ATPase activity with Ki values down to 12 nM. Some compounds also proved to be effective inhibitors of stimulated acid secretion in both the rat and dog when dosed i.v. However, although a number of these demonstrated activity after oral administration in dogs, the level and variability precluded further evaluation.
Journal of Medicinal Chemistry published new progress about Structure-activity relationship, ATPase-inhibiting. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Related Products of 18740-39-1.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia