Novel bronchodilatory quinazolines and quinoxalines: Synthesis and biological evaluation

Abstrakt

A series of heterocyclic derivatives analogous to (-)vasicinone, in which the vasicinone C-ring was replaced with alkyl chain terminated by tertiary amine was prepared. N3, C4-O, C4-S or C4-N were used as the sites of attachment.

The 4-[3-(1-piperidyl)propylsulfanyl]derivatives displayed bronchodilatory effect at low micromolar concentrations on isolated rat trachea, and low toxicity both on Balb/c 3T3 mouse fibroblast cells and in mice.

Klíčová slova

• Vasicinone
• Quinazoline
• Synthesis
• Bronchodilator
• Toxicity