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Synthesis and Structural Studies of 4-Thioxopyrimidines with Antimicrobial Activities |
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| Authors: | Silvio Cunha Rodrigo M. Bastos Priscila de O. Silva Giselle A. Nobre Costa Ivo Vencato Carlito Lariucci Hamilton B. Napolitano Cecília M. A. de Oliveira Lucília Kato Cleuza C. da Silva Diego Menezes Marcos A. Vannier-Santos |
| Affiliation: | Instituto de Química, Universidade Federal da Bahia, Campus de Ondina, Salvador-BA, Brazil Instituto de Física, Universidade Federal de Goiás, Goiania-GO, Brazil Ciências Exatas e Tecnológicas, Universidade Estadual de Goiás, Anápolis-GO, Brazil Instituto de Química, Universidade Federal de Goiás, Goiania-GO, Brazil Departamento de Química, Universidade Estadual de Maringá, Maringá-PR, Brazil Laboratório de Biomorfologia Parasitária e Microscopia Eletr?nica, Centro de Pesquisas Gon?alo Moniz, Funda??o Oswaldo Cruz (CPqGM-FIOCRUZ), Candeal, Salvador-BA, Brazil |
| Abstract: | Summary. This work describes a two-step, one-pot synthetic method for the formal aza-[3 + 3] cycloaddition between N-alkyl substituted enaminones and benzoyl isothiocyanate, which afforded 4-thioxopyrimidines in reasonable yields. Reaction of acyclic enaminone with a sterically hindered group attached to the nitrogen atom afforded pyridine-2-thione, yet in low yield. The antibacterial, antifungal, and trypanocidal activities of the thioxopyrimidines were evaluated and five compounds exhibited moderate activity against Candida albicans, Micrococcus luteus, and Trypanosoma cruzi. The solid state structures of a thioxopyrimidine, an organic disulfide, and a 1,2,4-triazole were determined by X-ray diffraction analysis. |
| Keywords: | . Cyclizations Enaminones Heterocycles Pyrimidine-4-thiones X-ray structure determination. |
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