Synthesis and H2-antagonist properties of some 1,2,5-thiadiazole-1-oxide derivatives.
A series of 1,2,5-thiadiazole-1-oxide derivatives has been synthesized and studied for its H2-antagonist properties. These derivatives can be considered derived from classical H2-antagonists in which the structure was deeply modified in order to evidence the minimal structural requirements for the activity. It was found that it is sufficient to have the 1,2,5-thiadiazole-1-oxide ring substituted with an alkylamino moiety and with an aliphatic chain linked to the hydroxy or ether group to achieve compounds as active as cimetidine. A few considerations on the binding on guinea-pig cerebral cortex of a series of H2-antagonists with more and more simplified structures are also reported.
Sorba
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G
Dipartimento di Scienza e Technologia del Farmaco, Torino.
Di Stilo
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A
Gasco
A M
AM
Gili
M
M
Gasco
A
A
Orsetti
M
M
D000818:Animals; D002217:Carbachol / Q000494:pharmacology; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D006632:Histamine / Q000494:pharmacology; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D009130:Muscle, Smooth / Q000187:drug effects; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D006635:Histamine H2 Antagonists; D013830:Thiadiazoles; D006632:Histamine; D002217:Carbachol; D007545:Isoproterenol