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pubmed-article:12729652pubmed:abstractTextThree series of spirocyclopiperazinium derivatives 5a-d, 6a-f and 17a-d were synthesized and evaluated for their in vivo analgesic activities. Compounds 5a, 17a and 17b exhibited excellent analgesic activity. Two important structure-activity relationships were observed from this study: (1) the quaternary ammonium functionality is a critical pharmacophore for analgesic activity; (2) it is important to adjust the lipophilic property of compounds to improve analgesic activity.lld:pubmed
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pubmed-article:12729652pubmed:dateRevised2010-11-18lld:pubmed
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pubmed-article:12729652pubmed:articleTitleUnique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.lld:pubmed
pubmed-article:12729652pubmed:affiliationSchool of Pharmaceutical Sciences, Peking University, Beijing 100083, PR China.lld:pubmed
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