Synthesis and Matrix Metalloproteinase-12 Inhibitory Activity of Ageladine A Analogs
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- Ando Naoki
- Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd.
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- Terashima Shiro
- Sagami Chemical Research Institute
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Synthesis of the 37 ageladine A analogs was accomplished by employing the total synthetic route of natural ageladine A previously explored by us. From the matrix metalloproteinase-12 (MMP-12) inhibitory activity assay carried out using the novel analogs, it appeared evident that the halogen atom at the 2-position of pyrrole ring was essential for the inhibitory activity and that the introduction of a bromine atom into the 4-position of pyrrole ring is very effective for producing potent activity. In addition, exchange of the pyrrole ring to an imidazole ring was extremely effective in increasing activity, and the analog 29 thus obtained was found to show approximately 4 times more potent activity than natural ageladine A.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 59 (5), 579-596, 2011
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204173347968
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- NII論文ID
- 130000648873
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 11058029
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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