Design, synthesis and pharmacological screening of a series of N1-(substituted)aryl-5,7-dimethyl-2-(substituted)pyrido(2,3-d)pyrimidin-4(3H)-ones as potential histamine H1-receptor antagonists

A series of N1-(substituted)aryl-5,7-dimethyl-2-(substituted)pyrido(2,3-d)pyrimidin-4(3H)-one was designed on the basis of the triangular pharmacophoric requirement of histamine H1-receptor antagonists. The designed series was synthesized by cyclo-condensation of monoaryl thiourea with ethyl cyanoac...

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Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2006-01, Vol.21 (6), p.681-691
Hauptverfasser:	Suhagia, Bhanubhai N., Chhabria, Mahesh T., Makwana, Ashlesha G.
Format:	Artikel
Sprache:	eng
Schlagworte:	allergy Animals Cetirizine - pharmacology Guinea Pigs Histamine Histamine H1 Antagonists - chemical synthesis Histamine H1 Antagonists - chemistry Histamine H1 Antagonists - pharmacology Histamine H1 Antagonists, Non-Sedating - pharmacology Ileum - drug effects Ileum - metabolism Mice Mice, Inbred Strains pyrido (2,3-d)pyrimidin-4(3H)-ones Pyrimidinones - chemical synthesis Pyrimidinones - chemistry Pyrimidinones - pharmacology Rats receptor antagonist Receptors, Histamine H1 - metabolism
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