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Glucuronidation of Two Novel Metabolites of Benproperine with Trichloroacetimidate Donor

Chemical Research in Chinese Universities 2006年第4期22卷 455-458页

作者： LI Yan HARA Osamu maeba isamu ZHONG Da-fang School of Pharmacy School of Pharmaceutical Engineering Shenyang Pharmaceutical UniversityShenyang 110016 P. R. China Faculty of Pharmacy Meijo University Nagoya 460-8503 Japan

The glucuronide metabolites of benproperine were synthesized from mono-hydroxylate metabolites of benproperine that were treated with methyl （2,3,4-tri-O-acetyl-1-O-tfichloroacetimidoyl ） -α-D-glucopyranuronate with BF3 · Eh O as the promoter followed by basic hydrolyzation with Na2 CO3. The form of basic acceptors, the order of addition, and the promoter are all important variables in this glucuronidation. The salt form of the basic acceptor was found to be better than its free form for glucuronidation with a Lewis acid as the promoter. Two mono-hydroxylated benproperines were synthesized from 2-benzylphenol in three steps.

关键词： Glucuronidation Benproperine Metabolite Trichloroacetimidate

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Identification of some benproperine metabolites in humans and investigation of their antitussive effect

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Acta Pharmacologica Sinica 2005年第12期26卷 1519-1526页

作者： isamu maeba Faculty of Pharmacy Meijo University Japan Nagoya 460-8503

Aim:To identify 4 unknown metabolites of benproperine(BPP,1)in human urineafter a po dose,and to investigate the antitussive effect of ***:The putative metabolite references were prepared usingchemical *** structures were identified using ~1H and13C nuclearmagnetic resonance,and mass *** metabolites in human urinewere separated and assayed using liquid chromatography-ion trap mass spec-trometry(LC/MS/MS),and further confirmed by comparison of their mass spectraand chromatographic retention times with those of synthesized *** antitussive effects of metabolites were evaluated on coughsinduced by 7.5% citric acid in conscious guinea ***:1-[1-Methyl-2-[2-(phenylmethyl)phenoxy]-ethyl]-4-piperidinol(2),1-[1-methyl-2-[2-(phenylmethyl)phenoxy]ethyl]-3-piperidinol(3)and their glucuronides 4 and 5 were obtainedfrom chemical *** urinary metabolites in human urine showed peakswith the same chromatographic retention times and mass spectra in LC/MS/MS assynthetic substances 2,3,4 and *** of compounds 2 and 3 prolongedthe latency of cough and reduced the number of coughs during the 3 rain testusing citric acid,but did not reduce the number of coughs during the 5 min imme-diately after the test in conscious guinea ***:Compounds 2,3,4,and 5 were identified as the metabolites of BPP in human *** them,compounds 2 and 3 are inactive in the antitussive effect.

关键词： benproperine metabolism antitussive agents hydroxylation glucuronide high performance liquid chromatography mass spectrometry

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