substituted n-phenylpyrazine-2-carboxamides synthesis and antimycobacterial evaluation代替n-phenylpyrazine-2-carboxamides合成和抗评估.pdfVIP

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substituted n-phenylpyrazine-2-carboxamides synthesis and antimycobacterial evaluation代替n-phenylpyrazine-2-carboxamides合成和抗评估.pdf

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substituted n-phenylpyrazine-2-carboxamides synthesis and antimycobacterial evaluation代替n-phenylpyrazine-2-carboxamides合成和抗评估

Molecules 2009, 14, 4180-4189; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Substituted N-Phenylpyrazine-2-carboxamides: Synthesis and Antimycobacterial Evaluation Martin Doležal 1,*, Jan Zitko 1, Diana Kešetovičová 1, Jiří Kuneš 1 and Michaela Svobodová 2 1 Faculty of Pharmacy in Hradec Králové, Charles University in Prague, Heyrovského 1203, Hradec Králové, 500 05, Czech Republic; E-Mails: jan.zitko@faf.cuni.cz (J.Z.); diana.kesetovicova@faf.cuni.cz (D.K.); jiri.kunes@faf.cuni.cz (J.K.) 2 Department of Microbiology, Regional Hospital, Kyjevská 44, Pardubice, 532 03, Czech Republic E-Mail: michaela.svobodova@nemocnice-pardubice.cz (M.S.) * Author to whom correspondence should be addressed; E-Mail: martin.dolezal@faf.cuni.cz. Received: 8 September 2009; in revised form: 1 October 2009 / Accepted: 13 October 2009 / Published: 20 October 2009 Abstract: The condensation of chlorides of substituted pyrazinecarboxylic acids with ring- substituted anilines yielded twelve substituted pyrazinecarboxylic acid amides. The synthetic approach, analytical, and lipophilicity data of the newly synthesized compounds are presented. Two antituberculosis assays were used. Firstly, the antimycobacterial activity against four different Mycobacterium strains in a series of pyrazine derivatives was investigated. Secondly, the antimycobacterial evaluation was performed at the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) program.