Bioisosteric Exchange of Csp3 -Chloro and Methyl Substituents: Synthesis and Initial Biological Studies of Atpenin A5 Analogues

Autor:	Simon Krautwald, Mihoko Mori, Erick M. Carreira, Kazuro Shiomi, Satoshi Ōmura, Christian Nilewski
Rok vydání:	2016
Předmět:	Antifungal Antifungal Agents Biological studies Molecular Structure Pyridones Stereochemistry medicine.drug_class 010405 organic chemistry Enantioselective synthesis General Chemistry General Medicine 010402 general chemistry 01 natural sciences Catalysis 0104 chemical sciences chemistry.chemical_compound chemistry Ic50 values medicine Molecule Bioisostere Atpenin A5
Zdroj:	Angewandte Chemie. 128:4117-4121
ISSN:	0044-8249
DOI:	10.1002/ange.201511672
Popis:	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 H3 C→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.
Databáze:	OpenAIRE
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