Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Department of Medical Oncology, VU University Medical Center, Cancer Center Amsterdam, DeBoelelaan 1117, 1081HV, Amsterdam, The Netherlands.
J Med Chem. 2020 Aug 13;63(15):7923-7956. doi: 10.1021/acs.jmedchem.9b01245. Epub 2020 Apr 2.
Thiazoles, their benzofused systems, and thiazolidinone derivatives are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor, and antimicrobial. In particular, in the past decade, many compounds bearing these heterocycles have been studied for their promising antibacterial properties due to their action on different microbial targets. Here we assess the recent development of this class of compounds to address mechanisms underlying antibiotic resistance at both bacterial-cell and community levels (biofilms). We also explore the SAR and the prospective clinical application of thiazole and its benzofused derivatives, which act as inhibitors of mechanisms underlying antibiotic resistance in the treatment of severe drug-resistant infections. In addition, we examined all bacterial targets involved in their antimicrobial activity reporting, when described, their spontaneous frequencies of resistance.
噻唑、苯并稠合系统和噻唑烷酮衍生物被广泛认为是获得具有各种生物活性的分子的有价值的核，包括镇痛、抗炎、抗 HIV、抗糖尿病、抗肿瘤和抗微生物。特别是在过去的十年中，由于这些杂环化合物对不同的微生物靶标起作用，许多含有这些杂环的化合物因其有希望的抗菌特性而被研究。在这里，我们评估了这一类化合物的最新发展，以解决细菌细胞和群落水平（生物膜）的抗生素耐药性的机制。我们还探索了噻唑及其苯并稠合衍生物的 SAR 和潜在的临床应用，它们作为治疗严重耐药感染中抗生素耐药机制的抑制剂。此外，我们检查了所有涉及到它们的抗菌活性的细菌靶标，并报告了当被描述时，它们的自发耐药频率。
