Malcolm L. Meeson

TL;DR: Quinazolines bearing a secondary 4-(arylamino) substituent demonstrate an SAR 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.

TL;DR: A weak HTS hit at the CCR2B receptor has been converted into a potent antagonist by array SAR studies and selectivity over the closely related CCR5 receptor is achieved.

TL;DR: It is shown that, for compounds bearing such a substituent, only a particular combination of properties provides high activity, both in vitro and as inhibitors of gastric acid secretion in vivo.

TL;DR: It is shown that by utilizing the powerful electron-donating effect of a 4-amino substituent on the pyridine, moderated by the electron-withdrawingeffect of a 3- or 5-halogen substituents, a combination of high potency and good stability under physiological conditions can be obtained.

TL;DR: A new structural type of antagonist is shown which represents an important departure from the conventional view of antihistamines as strongly basic amines which are predominantly protonated under physiological conditions and believed to interact with the receptor in the cationic form.