School of New Energy, Yulin University, Yulin 719000, Shaanxi, PR China.
Adichunchanagiri Institute for Molecular Medicine, Adichunchanagiri Institute of Medical Sciences, Adichunchanagiri University, B. G. Nagar 571448, India.
Bioorg Chem. 2024 Apr;145:107241. doi: 10.1016/j.bioorg.2024.107241. Epub 2024 Feb 25.
The discovery of new small molecule-based inhibitors is an attractive field in medicinal chemistry. Structurally diversified heterocyclic derivatives have been investigated to combat multi-drug resistant bacterial infections and they offers several mechanism of action. Methicillin-resistant Staphylococcus aureus (MRSA) is becoming more and more deadly to humans because of its simple method of transmission, quick development of antibiotic resistance, and ability to cause hard-to-treat skin and filmy diseases. The sulfur (S) particularly sulfonyl and sulfonamide based heterocyclic moieties, have found to be good anti-MRSA agents. The development of new nontoxic, economical and highly active sulfur (S) containing derivatives has become hot research topics in drug discovery research. Presently, more than 150 FDA approved Sulfur (S)-based drugs are available in the market, and they are widely used to treat various types of diseases with different therapeutic potential. The present collective data provides the latest advancements in Sulfur (S)-hybrid compounds as antibacterial agents against MRSA. It also examines the outcomes of in-vitro and in-vivo investigations, exploring potential mechanisms of action and offering alternative perspectives on the structure-activity relationship (SAR). Sulfur (S)-hybrids exhibits synergistic effects with existing drugs to provide antibacterial action against MRSA.
新型小分子抑制剂的发现是药物化学领域的一个热门研究方向。具有多样化结构的杂环衍生物已被用于对抗多重耐药菌感染，它们具有多种作用机制。耐甲氧西林金黄色葡萄球菌（MRSA）由于其简单的传播方式、快速产生抗生素耐药性以及导致难以治疗的皮肤和膜状疾病的能力，对人类的威胁越来越大。含硫（S）特别是磺酰基和磺酰胺的杂环部分已被证明是很好的抗 MRSA 药物。开发新型无毒、经济且高效的含硫（S）衍生物已成为药物发现研究的热门课题。目前，市场上有超过 150 种获得 FDA 批准的含硫（S）药物，它们被广泛用于治疗各种具有不同治疗潜力的疾病。本综述提供了最新的关于含硫（S）杂合化合物作为抗 MRSA 抗菌剂的研究进展。它还检查了体外和体内研究的结果，探索了潜在的作用机制，并提供了关于结构-活性关系（SAR）的替代观点。含硫（S）杂合化合物与现有药物具有协同作用，可提供针对 MRSA 的抗菌作用。
