RSC advances · 2022
Coupling of acceptor-substituted diazo compounds and tertiary thioamides: synthesis of enamino carbonyl compounds and their pharmacological evaluation.
СтатьяНазвание и аннотация: Перевод в очереди
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Secka Jim, Pal Arpan, Acquah Francis A, Mooers Blaine H M, Karki Anand B, Mahjoub Dania, Fakhr Mohamed K, Wallace David R, Okada Takuya, Toyooka Naoki, Kuta Adama, Koduri Naga, Herndon Deacon, Roberts Kenneth P, Wang Zhiguo, Hileman Bethany, Rajagopal Nisha, Hussaini Syed R
Аннотация
This paper describes the synthesis of enamino carbonyl compounds by the copper(i)-catalyzed coupling of acceptor-substituted diazo compounds and tertiary thioamides. We plan to use this method to synthesize indolizidine (-)-237D analogs to find α6-selective antismoking agents. Therefore, we also performed in silico α6-nAchRs binding studies of selected products. Compounds with low root-mean-square deviation values showed more favorable binding free energies. We also report preliminary pharmacokinetic data on indolizidine (-)-237D and found it to have weak activity at CYP3A4. In addition, as enamino carbonyl compounds are also known for antimicrobial properties, we screened previously reported and new enamino carbonyl compounds for antibacterial, antimicrobial, and antifungal properties. Eleven compounds showed significant antimicrobial activities.