GONĚC, Tomáš, Šárka MASCARETTI, Hana MICHNOVÁ, Alois ČÍŽEK and Josef JAMPÍLEK. 2-Hydroxynaphthalene-1-carboxamides possessing antimycobacterial activity. In 50th Conference Synthesis and Analysis of Drugs. 2022. ISBN 978-80-280-0110-0.
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Basic information
Original name 2-Hydroxynaphthalene-1-carboxamides possessing antimycobacterial activity
Name in Czech 2-Hydroxynaftalen-1-karboxamidy vykazující antimykobakteriální aktivitu
Authors GONĚC, Tomáš, Šárka MASCARETTI, Hana MICHNOVÁ, Alois ČÍŽEK and Josef JAMPÍLEK.
Edition 50th Conference Synthesis and Analysis of Drugs, 2022.
Other information
Original language English
Type of outcome Conference abstract
Field of Study 30104 Pharmacology and pharmacy
Country of publisher Czech Republic
Confidentiality degree is not subject to a state or trade secret
WWW URL URL
Organization unit Faculty of Pharmacy
ISBN 978-80-280-0110-0
Keywords (in Czech) hydroxynaftalenkarboxamid; Mycobacterium; MIC; syntéza
Keywords in English hydroxynaphthalene carboxamide; Mycobacterium; MIC; synthesis
Tags International impact
Changed by Changed by: PharmDr. Tomáš Goněc, Ph.D., učo 39112. Changed: 11/5/2023 10:46.
Abstract
The aim of recent work was to synthetize series of N-(phenyl)-2-hydroxynaphthalene-1-carboxamides with multiple substitution on phenyl ring. 30 compounds with halogen, trifluoromethyl, methyl, methoxy and nitro substituted anilide ring were prepared according to well approved microwave-assisted synthetic method. Structure of novel compounds was confirmed by 1H and 13C NMR, HRMS and IR spectroscopy. Primary in vitro screening of the synthesized compounds was performed against Mycobacterium marinum, Mycobacterium kansasii and Mycobacterium smegmatis. Several compounds showed antimycobacterial activity comparable to standards Pyrazinamide and Rifampicine.
Abstract (in Czech)
Cílem práce byla syntéza série N-(fenyl)-2-hydroxynaftalen-1-karboxamidů s vícečetnou substitucí fenylové části. Bylo připraveno 30 látek s halogen, trifluormethyl, methyl, methoxy a nitro substitucí, pomocí osvědčené mikrovlnné syntézy. Struktura nových látek byla potvrzena pomocí 1H, 13C NMR, HRMS a IČ spektrometrie. Primární in vitro skrínink antimykobakteriální aktivity byl proveden u kmenů Mycobacterium marinum, Mycobacterium kansasii a Mykobacterium smegmatis. Několik látek vykázalo srovnatelnou, nebo vyšší antimykobakteriální aktivitu než standardy pyrazinamid a rifampicin.
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