a Department of Chemistry, Faculty of Science , Kuwait University , Safat , Kuwait.
b Department of Chemistry, Faculty of Science , Cairo University , Giza , Egypt.
Expert Opin Ther Pat. 2017 Apr;27(4):477-505. doi: 10.1080/13543776.2017.1272575. Epub 2017 Jan 4.
Four isomeric structures of thiadiazole motifs have outstanding pharmacological inhibitory applications are reported in this review. Thiadiazole nucleus is present in several biologically active natural products and commercial drugs. Most of thiadiazoles reported herein are emphasized to have broad spectrum of medicinal activities. Areas covered: This review represents the recent inhibitory activities of thiadiazole isomeric scaffolds and their broad-spectrum biological applications published as full texts during 2010-2016 as well as the patents published during 2005-2016. The inhibition areas covered included anti-inflammatory, antimicrobial, antitumor, antioxidant, antitubercular, antiviral, antileishmanial, anticonvulsant, herbicidal and algicidal activities in addition to enzymes, human platelet aggregation and neuroprotective inhibitors. Expert opinion: This survey revealed very interesting data about the applications of thiadiazoles, where some synthetic or natural thiadiazole derivatives were components of drugs available in the market. Many thiadiazole derivatives can be considered as lead compounds for drug synthesis. The most inhibitory active 1,3,4-thiadiazole compounds are those incorporating secondary alkyl(aryl)amido- and/or benzylthio(mercapto) groups at positions 2 and 5. Several thiadiazole derivatives demonstrated higher antibacterial, antitumor and antiviral activities than the standard drugs. Some thiadiazole derivatives exhibited high selective enzymes inhibitory activities based on the electronic properties of the substituents at positions 2 or 5.
本文综述了具有突出药理抑制应用的四种噻二唑基异构结构。噻二唑核存在于几种具有生物活性的天然产物和商业药物中。本文报道的大多数噻二唑类化合物都具有广泛的药用活性。
本综述代表了 2010 年至 2016 年期间以全文形式发表的噻二唑异构支架的最新抑制活性及其广谱生物应用，以及 2005 年至 2016 年期间发表的专利。涵盖的抑制领域包括抗炎、抗菌、抗肿瘤、抗氧化、抗结核、抗病毒、抗利什曼原虫、抗惊厥、除草和杀藻活性，以及酶、人血小板聚集和神经保护抑制剂。
这项调查显示了关于噻二唑应用的非常有趣的数据，其中一些合成或天然噻二唑衍生物是市场上可用药物的成分。许多噻二唑衍生物可以被认为是药物合成的先导化合物。最具抑制活性的 1,3,4-噻二唑化合物是那些在 2 位和 5 位上含有仲烷基（芳基）酰胺基和/或苄基硫基（巯基）的化合物。一些噻二唑衍生物表现出比标准药物更高的抗菌、抗肿瘤和抗病毒活性。一些噻二唑衍生物表现出基于 2 位或 5 位取代基的电子性质的高选择性酶抑制活性。
