synthesis and preliminary antimicrobial activities of new arylideneamino-1,3,4-thiadiazole-(thiodithio)-acetamido cephalosporanic acids合成和初步的抗菌活动新arylideneamino-1 4-thiadiazole 3u2014u2014(thiodithio)-acetamido cephalosporanic酸.pdfVIP
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synthesis and preliminary antimicrobial activities of new arylideneamino-1,3,4-thiadiazole-(thiodithio)-acetamido cephalosporanic acids合成和初步的抗菌活动新arylideneamino-1 4-thiadiazole 3u2014u2014(thiodithio)-acetamido cephalosporanic酸
Molecules 2012, 17, 1025-1038; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Preliminary Antimicrobial Activities of New Arylideneamino-1,3,4-thiadiazole-(thio/dithio)-acetamido Cephalosporanic Acids Shakir Mahmood Alwan Department of Pharmaceutical Chemistry, College of Pharmacy, University of Baghdad, Bab-Al-muadham P.O. Box 14026, 10047, Baghdad, Iraq; E-Mail: shakmawales@yahoo.co.uk; Tel.: +00964-7902-518-888 Received: 9 October 2011; in revised form: 27 December 2011 / Accepted: 4 January 2012 / Published: 19 January2012 Abstract: New derivatives of 7-aminocephalosporanic acid 1–8 were synthesized by acylation of the 7-amino group of the cephem nucleus with various arylidinimino-1,3,4- thiadiazole-thio(or dithio)-acetic acid intermediates 3a–d and 5a–d, respectively, so the acyl side chains of these new cephalosporins contained a sulfide or disulfide bond. This unique combination of a Schiff base with the sulfide or disulfide bonds in the acyl side chain afforded new cephalosporins of reasonable potencies, some of which were found to possess moderate activities against the tested microorganisms. Their chemical structures were characterized by ¹H-NMR, IR spectroscopy and elemental microanalysis. Preliminary in vitro antimicrobial activities of the prepared cephalosporins were investigated using a panel of selected microorganisms. Results in
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