Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors |
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| Authors: | Wallace Michael B Feng Jun Zhang Zhiyuan Skene Robert J Shi Lihong Caster Christopher L Kassel Daniel B Xu Rongda Gwaltney Stephen L |
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| Affiliation: | Takeda San Diego, Drug Discovery, 10410 Science Center Drive, San Diego, CA 92121, USA. michael.wallace@takedasd.com |
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| Abstract: | A novel series of non-covalent, benzimidazole-based inhibitors of DPP-4 has been developed from a small fragment hit using structure-based drug design. A highly versatile synthetic route was created for the development of SAR, which led to the discovery of potent and selective inhibitors with excellent pharmaceutical properties. |
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