Theophylline derivatives as potential histamine H3-receptor antagonists.
Previous results of histamine H3-receptors investigations allowed to formulate a general structure of H3-receptor antagonists. According to this model a series of compounds were obtained. As heterocycles they contained a theophylline moiety connected with a polar group (amine, ester, amide, and thiourea function) via an alkyl chain linked by a spacer to a lipophilic residue. The common distance between xanthine moiety and lipophilic rest was a six-link-chain. Selected compounds did not show significant H3-receptor antagonist activity and were weak antagonists at histamine H1-receptors.
Kieć-Kononowicz
K
K
Department of Chemical Technology of Drugs, Collegium Medicum, Jagiellonian University, Kraków, Poland.
Cegła
M T
MT
D000818:Animals; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013806:Theophylline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*
D006633:Histamine Antagonists; D018100:Receptors, Histamine H3; D013806:Theophylline