源自森田-贝利斯-希尔曼反应的烯丙基硫氰酸盐的抗菌活性。
Antimicrobial activity of allylic thiocyanates derived from the Morita-Baylis-Hillman reaction.
作者信息
Sá Marcus Mandolesi, Ferreira Misael, Lima Emerson Silva, dos Santos Ivanildes, Orlandi Patrícia Puccinelli, Fernandes Luciano
机构信息
Departamento de Química Universidade Federal de Santa Catarina FlorianópolisSC Brazil Departamento de Química, Universidade Federal de Santa Catarina, Florianópolis, SC, Brazil.
Faculdade de Ciências Farmacêuticas Universidade Federal do Amazonas ManausAM Brazil Faculdade de Ciências Farmacêuticas, Universidade Federal do Amazonas, Manaus, AM, Brazil.
出版信息
Braz J Microbiol. 2014 Oct 9;45(3):807-12. doi: 10.1590/s1517-83822014000300007. eCollection 2014.
Bacterial resistance to commonly used antibiotics has been recognized as a significant global health issue. In this study, we carried out the screening of a family of allylic thiocyanates for their action against a diversity of bacteria and fungi with a view to developing new antimicrobial agents. Allylic thiocyanates bearing halogenated aryl groups, which were readily obtained in two steps from the Morita-Baylis-Hillman adducts, showed moderate-to-high activity against selective pathogens, including a methicillin-resistant S. aureus (MRSA) strain. In particular cases, methyl (Z)-3-(2,4-dichlorophenyl)-2-(thiocyanomethyl)-2-propenoate exhibited antimicrobial activity comparable to the reference antibiotic Imipenem.
细菌对常用抗生素的耐药性已被公认为一个重大的全球健康问题。在本研究中，我们对一系列烯丙基硫氰酸盐进行了筛选，以考察它们对多种细菌和真菌的作用，旨在开发新型抗菌剂。带有卤代芳基的烯丙基硫氰酸盐可通过两步反应从森田-贝利斯-希尔曼加合物轻松制得，对包括耐甲氧西林金黄色葡萄球菌（MRSA）菌株在内的选择性病原体表现出中度至高度活性。在某些特定情况下，(Z)-3-(2,4-二氯苯基)-2-(硫氰基甲基)-2-丙烯酸甲酯表现出与参考抗生素亚胺培南相当的抗菌活性。
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