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2-Amino-1,3,4-thiadiazole as a potential scaffold for promising antimicrobial agents

机译:2-氨基-1,3,4-噻二唑用作潜在的抗菌药物的潜在支架

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Pathogenic microorganisms are causative agents for different types of serious and even lethal infectious diseases. Despite advancements in medication, bacterial and fungal infections continue to be a growing problem in health care. As more and more bacteria become resistant to antibiotics used in therapy and an increasing number of invasive fungal species become resistant to current antifungal medications, there is considerable interest in the development of new compounds with antimicrobial activity. The compounds containing a heterocyclic ring play an important role among organic compounds with biological activity used as drugs in human and veterinary medicine or as insecticides and pesticides in agriculture. Thiadiazoles belong to the classes of nitrogen–sulfur heterocycles with extensive application as structural units of biologically active molecules and as useful intermediates in medicinal chemistry. The potency of the thiadiazole nucleus is demonstrated by the drugs currently used. 1,3,4-Thiadiazoles and some of their derivatives are extensively studied because of their broad spectrum of pharmacological activities. The aim of this review was to highlight the main antimicrobial properties exhibited by derivatives possessing 2-amino-1,3,4-thiadiazole moiety. Many of the reported 2-amino-1,3,4-thiadiazole derivatives can be considered as lead compounds for drug synthesis, and several of them have demonstrated higher antimicrobial activity in comparison to standard drugs. Furthermore, taking into account the reactivity of the amine group in the derivatization process, 2-amino-1,3,4-thiadiazole moiety may be a good scaffold for future pharmacologically active 1,3,4-thiadiazole derivatives.
机译:病原微生物是导致各种类型的严重甚至致命的传染病的病原体。尽管药物方面取得了进步,但是细菌和真菌感染仍然是卫生保健中日益严重的问题。随着越来越多的细菌对治疗中使用的抗生素产生抗药性,并且越来越多的侵入性真菌对目前的抗真菌药物产生抗药性,对具有抗菌活性的新化合物的开发产生了极大的兴趣。在具有生物活性的有机化合物中,含有杂环的化合物在用作人和兽药的药物或用于农业的杀虫剂和农药中起着重要的作用。噻二唑属于氮硫杂环类,广泛用作生物活性分子的结构单元和医药化学中的有用中间体。噻二唑核的效力由目前使用的药物证明。 1,3,4-噻二唑及其某些衍生物因其广泛的药理活性而得到了广泛的研究。这篇综述的目的是强调具有2-氨基-1,3,4-噻二唑部分的衍生物所表现出的主要抗菌性能。可以将许多报道的2-氨基-1,3,4-噻二唑衍生物视为药物合成的先导化合物,并且其中一些已证明比标准药物具有更高的抗菌活性。此外,考虑到胺基在衍生化过程中的反应性,对于未来的药理活性的1,3,4-噻二唑衍生物,2-氨基-1,3,4-噻二唑部分可能是很好的支架。

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