Potential histamine H2-receptor antagonists. Synthesis, structure and activity of a few open models related to classical H2-antagonists.
A few ethers and oximes structurally related to classical H2-antagonists have been synthetized and tested for their in vitro H2-antagonist activity. The compounds in which cyclic "urea equivalent" groups are joined to a cyclohexylmethyl moiety showed a high increase of activity in comparison with the unsubstituted analogues. This finding supports the hypothesis of the existence of an accessorial binding area on H2-receptor near the site fitted by cyclic "urea equivalent" groups.
Sorba
G
G
Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Turin.
Fruttero
R
R
Gasco
A
A
Orsetti
M
M
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D008954:Models, Biological; D011899:Ranitidine / Q000031:analogs & derivatives / Q000494:pharmacology; D013329:Structure-Activity Relationship
D006635:Histamine H2 Antagonists; D011899:Ranitidine