Structure-Activity Relationship between Thiol Group-Trapping Ability of Morphinan Compounds with a Michael Acceptor and Anti-Plasmodium falciparum Activities

Autor:	Noriki Kutsumura, Yasuaki Koyama, Tsuyoshi Saitoh, Naoshi Yamamoto, Yasuyuki Nagumo, Yoshiyuki Miyata, Rei Hokari, Aki Ishiyama, Masato Iwatsuki, Kazuhiko Otoguro, Satoshi Ōmura, Hiroshi Nagase
Jazyk:	angličtina
Rok vydání:	2020
Předmět:	morphinan bntx δ opioid receptor antagonist 1h-nmr experiments mechanism elucidation Organic chemistry QD241-441
Zdroj:	Molecules, Vol 25, Iss 5, p 1112 (2020)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules25051112
Popis:	7-Benzylidenenaltrexone (BNTX) and most of its derivatives showed in vitro antimalarial activities against chloroquine-resistant and -sensitive Plasmodium falciparum strains (K1 and FCR3, respectively). In addition, the time-dependent changes of the addition reactions of the BNTX derivatives with 1-propanethiol were examined by 1H-NMR experiments to estimate their thiol group-trapping ability. The relative chemical reactivity of the BNTX derivatives to trap the thiol group of 1-propanethiol was correlated highly with the antimalarial activity. Therefore, the measurements of the thiol group-trapping ability of the BNTX derivatives with a Michael acceptor is expected to become an alternative method for in vitro malarial activity and related assays.
Databáze:	Directory of Open Access Journals
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