Structure–activity relationship studies of atpenin A5 analogs with chemical modification of the side chain moiety

Autor:	Tohru Nagamitsu, Tohru Hiura, Atsuyoshi Miyao, Satoshi Omura, Masaki Ohtawa, Kouhei Sugiyama, Kiyoshi Kita, Shiho Arima, Keisuke Yano
Rok vydání:	2019
Předmět:	010405 organic chemistry Chemistry Stereochemistry Organic Chemistry Chemical modification 010402 general chemistry 01 natural sciences Biochemistry 0104 chemical sciences chemistry.chemical_compound Drug Discovery Side chain Moiety Structure–activity relationship Atpenin A5 Lead compound
Zdroj:	Tetrahedron Letters. 60:1037-1042
ISSN:	0040-4039
DOI:	10.1016/j.tetlet.2019.03.026
Popis:	We designed and synthesized new atpenin A5 analogs for SAR study. Most of the analogs lacked one or several functional groups in the side chain of atpenin A5, and the stereoisomers proved to be weak nematode complex II inhibitors. However, we determined that 4-epi-atpenin A5 was a potent nematode complex II inhibitor comparable to atpenin A5. Therefore, 4-epi-atpenin A5 is expected to become a new lead compound in nematicide development.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::ab88114e434aacfeb04febfadfd859e8 https://doi.org/10.1016/j.tetlet.2019.03.026 Zobrazit plný text záznamu Full Text from ScienceDirect