Studies on Pyridinol Derivatives. II. Synthesis and Pharmacological Activity of 2H-Pyrido [3, 2-b]-1, 4-oxazin-3-one Derivatives. (1)

Abstract

Twenty kinds of derivatives of 2H-pyrido [3, 2-b]-1, 4-oxazin-3-one (8a-12d) having β-dialkylaminoethyl groups were synthesized by the ring closure of 2-amino-3-hydroxypyridine (1) with α-halogeno acid ester in the presence of sodium hydride in DMF. The following results were obtained from the preliminary investigation on the local anesthetic and the analgesic activities (mouse writhing test) of these synthesized compounds. It was proved that the duration time of the local anesthetic activities of almost all these compounds is inferior to that of cocaine or lidocaine, but the duration of these activities, in quite few cases, superior to that of cocaine or lidocaine ; the analgesic action of some of them are apporoximately equivalent to that of pyrabital.