Serban Georgeta, Stanasel Oana, Serban Eugenia, Bota Sanda
Pharmaceutical Chemistry Department, Faculty of Medicine and Pharmacy, University of Oradea, Oradea, Romania.
Chemistry Department, Faculty of Sciences, University of Oradea, Oradea, Romania.
Drug Des Devel Ther. 2018 May 31;12:1545-1566. doi: 10.2147/DDDT.S155958. eCollection 2018.
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.
病原微生物是引发各类严重甚至致命传染病的病原体。尽管药物治疗取得了进展，但细菌和真菌感染在医疗保健领域仍是一个日益严重的问题。随着越来越多的细菌对治疗中使用的抗生素产生耐药性，以及越来越多的侵袭性真菌物种对当前的抗真菌药物产生耐药性，人们对开发具有抗菌活性的新化合物产生了浓厚兴趣。含有杂环的化合物在用作人类和兽医学药物或农业杀虫剂和农药的具有生物活性的有机化合物中发挥着重要作用。噻二唑属于氮硫杂环类，作为生物活性分子的结构单元和药物化学中的有用中间体有着广泛应用。目前使用的药物证明了噻二唑核的效力。1,3,4-噻二唑及其一些衍生物因其广泛的药理活性而受到广泛研究。本综述的目的是突出具有2-氨基-1,3,4-噻二唑部分的衍生物所表现出的主要抗菌特性。许多已报道的2-氨基-1,3,4-噻二唑衍生物可被视为药物合成的先导化合物，其中一些与标准药物相比表现出更高的抗菌活性。此外，考虑到胺基在衍生化过程中的反应性，2-氨基-1,3,4-噻二唑部分可能是未来具有药理活性的1,3,4-噻二唑衍生物的良好支架。
