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- Title
Bioisosteric Exchange of C.
- Authors
Krautwald, Simon; Nilewski, Christian; Mori, Mihoko; Shiomi, Kazuro; Ōmura, Satoshi; Carreira, Erick M.
- Abstract
Asymmetric synthesis and initial biological studies of two analogues of a naturally occurring chlorinated antifungal agent, atpenin A5, are described. These analogues were selected on the basis of Cl→CH3 or H3C→Cl exchanges in the side-chain of atpenin A5. The interchange of chloro and methyl substituents led to complex II inhibitors with equal IC50 values. This suggests that Cl↔Me bioisosteric exchange can be realized in aliphatic settings.
- Subjects
BIOISOSTERES; PHARMACEUTICAL chemistry; DRUG design; ANTIFUNGAL agents; METHYL groups
- Publication
Angewandte Chemie, 2016, Vol 128, Issue 12, p4117
- ISSN
0044-8249
- Publication type
Article
- DOI
10.1002/ange.201511672