88939-84-8Relevant academic research and scientific papers
A Palladium-Catalyzed Carbonyl Insertion Route to Pyridoquinazoline Derivatives
Tilley, Jefferson W.,Coffen, David L.,Schaer, Beatrice H.,Lind, Joan
, p. 2469 - 2474 (2007/10/02)
A synthesis of 8-substituted pyridoquinazoline derivatives is described involving as the key step the palladium-catalyzed carbonyl insertion reaction of 5-substituted 2-(2-bromoanilino)pyridines.This methodology provides a new and flexible route to
N-(Heterocyclic alkyl)pyridoquinazoline-8-carboxamides as Orally Active Antiallergy Agents
Tilley, Jefferson W.,Levitan, Paul,Lind, Joan,Welton, Ann F.,Crowley, Herman J.,et al.
, p. 185 - 193 (2007/10/02)
A series of N-(heterocyclic alkyl)pyridoquinazoline-8-carboxamides were evaluated for their ability to antagonize slow-reacting substance of anaphylaxis (SRS-A) induced contractions of guinea pig ilea and to inhibit thromboxane synthase in vitro.The results indicated that those pyridoquinazoline-8-carboxamides bearing a branched-chain alkyl moiety in the 2-position and a four to six atom linear chain between a 3- or 4-substituted pyridine or a 1-substituted imidazole ring and the carboxamide nitrogen atom showed the best combination of potencies in the two assays.Several of these compounds were found to be orally active inhibitors of LTE4-induced bronchoconstriction in the guinea pig and LTE4-induced skin wheal formation in the rat.One of the most potent analogues, 2-(1-methylethyl)-N-(1H-imidazol-1-ylbutyl)-11-oxo-11H-pyridoquinazoline-8-carboxamide (36), was selected for extensive pharmacological investigation.It was found that this compound was not a specific inhibitor of LTE4-induced symptomatology, but exhibited more general activity by inhibiting bronchospasm in guinea pigs induced by LTC4, LTD4, PAF, and histamine and skin wheal formation in rats and guinea pigs induced by LTC4, LTD4, and PAF.In addition, 36 was orally active in the passive cutaneous anaphylaxis assay, suggesting that it also exhibits mediator release inhibitory activity.On the basis of the overall pharmacological profile of 36 and its closely related analogues, it was concluded that these compounds may be useful for the treatment of asthma.
Pyrido[2,1-b]quinazoline derivatives useful as agents for treatment of allergic conditions and vascular disorders involving thrombosis
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, (2008/06/13)
Pyrido[2,1-b]quinazoline derivatives of the formulas STR1 wherein R1, R2 and R3 are as hereinafter set forth, are described. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions
