SAR studies on H 2 antagonists containing alkylamino substituted 1, 2, 5-thiadiazole 1-oxide moieties

…, A Gasco, G Bertaccini, C Pozzoli, M Adami, G Coruzzi

Index: Di Stilo, Antonella; Cena, Clara; Lolli, Marco; Sorba, Giovanni; Gasco, Alberto; Bertaccini, Giulio; Pozzoli, Cristina; Adami, Maristella; Coruzzi, Gabriella Farmaco, 1998 , vol. 53, # 8-9 p. 536 - 540

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Citation Number: 2

Abstract

A number of ranitidine analogues in which the diamino-1, 2, 5-thiadiazole 1-oxide substructure bearing alkyl chains of different length is present as the urea equivalent group, were synthesised and studied for their lipophilic and H2 antagonist properties. Derivatives which displayed a logP≤ 3 behaved as competitive antagonists of histamine at H2 receptors present on guinea pig right atrium. The remaining more lipophilic members of ...