Ogawa, Nobuo; Yoshida, Toshihiko; Aratani, Takayuki; Koshinaka, Eiichi; Kato, Hideo; Ito, Yasuo published the artcile< Synthesis and histamine H2-antagonist activity of 4-quinazolinone derivatives>, Quality Control of 5004-88-6, the main research area is piperidinylmethylphenoxypropylaminoquinazolinone preparation antiulcer histamine antagonist; quinazolinone piperidinylmethylphenoxypropylamino preparation histamine antagonist; structure activity aminomethylphenoxyalkylaminoquinazolinone histamine antagonist.
With the aim of developing new antiulcer agents, a series of 4-quinazolinone derivatives e.g., I (R = piperidino, pyrrolidino, morpholino, R1 = H, OMe, R2 = H, Me; n = 2, 3, 4) was synthesized and tested for histamine H2-antagonist activity and gastric antisecretory activity. Thus, 2-alkylamino-, 2-alkylthio-, and 2-alkyl-4-quinazolinones were prepared by the condensation of alkylamines with 2-chloro- or 2-methylthio-4-quinazolinones, the condensation of alkyl bromides with 2-mercapto-4-quinazolinones, and the condensation of alkylcarboxylic acids with anthranilamides, resp. Several of the 4-quinazolinone derivatives showed potent H2-antagonist activity, and one of them, I (R = piperidino, R1 = R2 = H, n = 3), showed the most potent antisecretory activity. The structure-activity relationships are discussed.
Chemical & Pharmaceutical Bulletin published new progress about Histamine H2 receptor antagonists. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Quality Control of 5004-88-6.
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