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A convenient synthesis of a chlorobenzothiophenyl-indole-based inhibitor of bacterial cystathionine γ-lyase Научная публикация

Журнал Mendeleev Communications
ISSN: 1364-551X , E-ISSN: 0959-9436
Вых. Данные Год: 2024, Том: 34, Номер: 2, Страницы: 255-258 Страниц : 4 DOI: 10.1016/j.mencom.2024.02.030
Авторы Novikov Maxim A. 1,2 , Potapov Konstantin V. 1,2 , Novikov Roman A. 1,3,2 , Solyev Pavel N. 2 , Tomilov Yury V. 1 , Kochetkov Sergey N. 2 , Makarov Alexander A. 2 , Mitkevich Vladimir A. 4,2
Организации
1 N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 119991 Moscow, Russian Federation
2 V. A. Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 119991 Moscow, Russian Federation
3 Sirius University of Science and Technology, 354349 Sochi, Russian Federation
4 Institute of Fundamental Medicine and Biology, Kazan Federal University, 420008 Kazan, Russian Federation

Реферат: A convenient and efficient synthesis of 3-{[6-(7-chloro- benzo[b]thiophen-2-yl)-1H-indol-1-yl]methyl}-1H-pyrazole- 5-carboxylic acid (NL3), which is currently among the most active and promising bacterial cystathionine γ-lyase (bCSE) inhibitors, has been developed. It is based on shifting the key stage of [Pd]-catalyzed cross-coupling of the indole and benzothiophene counterparts to the beginning of the synthetic scheme, with the polarity reversal of the components being coupled, to give 6-(7-chlorobenzo[b]thiophen-2-yl)-1H- indole as the key intermediate. The STD NMR method was used to estimate the NL3 compound obtained in the optimized synthesis as a ligand to saCSE (the main producer of H2S in pathogenic S. aureus).
Библиографическая ссылка: Novikov M.A. , Potapov K.V. , Novikov R.A. , Solyev P.N. , Tomilov Y.V. , Kochetkov S.N. , Makarov A.A. , Mitkevich V.A.
A convenient synthesis of a chlorobenzothiophenyl-indole-based inhibitor of bacterial cystathionine γ-lyase
Mendeleev Communications. 2024. V.34. N2. P.255-258. DOI: 10.1016/j.mencom.2024.02.030 WOS Scopus OpenAlex
Идентификаторы БД:
≡ Web of science: WOS:001223752100001
≡ Scopus: 2-s2.0-85189828191
≡ OpenAlex: W4393856752
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