synthesis and bioactivity evaluation of new 6-aryl-5-cyano thiouracils as potential antimicrobial and anticancer agents合成和生物活性评价的新6-aryl-5-cyano硫脲嘧啶作为潜在的抗菌和抗癌剂.pdf

Molecules 2012, 17, 9868-9886; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Bioactivity Evaluation of New 6-Aryl-5-cyano Thiouracils as Potential Antimicrobial and Anticancer Agents Azza Taher Taher 1 and Sahar Mahmoud Abou-Seri 2,* 1 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, P.O. Box, 11562, Egypt; E-Mail: azzataher2005@ 2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, P.O. Box, 11562, Egypt * Author to whom correspondence should be addressed; E-Mail: saharshaarawy_69@; Tel.: +20-2-2559-1683; Fax: +20-2-2362-8426. Received: 16 July 2012; in revised form: 25 July 2012 / Accepted: 10 August 2012 / Published: 17 August 2012 Abstract: Several novel 6-aryl-5-cyano thiouracil derivatives were synthesized and explored for their activities as antibacterial, antifungal and anticancer agents. The antimicrobial evaluation revealed that compounds 7b and 7c possessed superior antibacterial activity against the Gram positive bacteria S. aureus and B. subtilis compared to the reference drug amoxicillin. Moreover, compound 4i was found to be a broad spectrum antimicrobial agent and it also exhibited the highest antifungal activity against C. albicans, even higher than the reference drug amphotericin B (MIC = 2.34, 3.00 μg/mL respectively