Kumawat Mukesh Kumar
Anand College of Pharmacy, Keetham, Agra-282006, Uttar Pradesh, India.
Curr Drug Discov Technol. 2018;15(3):196-200. doi: 10.2174/1570163814666170725114159.
Heterocyclic compounds are the main class of medicinally important compounds. Many heterocyclic compounds bearing a five-membered ring in their structure have a good spectrum of biological activities. Thiazole is an important class of five-membered heterocyclic compounds. Thiazole and its derivatives exhibited a broad range of biological activities due to the presence of various reaction posseses. Thiazole, heterocyclic nucleus is present in several potent pharmacologically active molecules such as Sulfathiazole (antimicrobial drug), Ritonavir (antiretroviral drug), Tiazofurin (antineoplastic drug) and Abafungin (antifungal drug) etc. The search for some novel biologically active thiazoles is to be continued in the field of medicinal chemistry for investigators. An aim of this review is to identify and try making a SAR (Structure Activity Relationship) of substituted thiazole nucleus as possible new antimalarials.
Author undertook a structured search of bibliographic databases for peerreviewed research literature using a focused review question and inclusion/exclusion criteria. The quality of retrieved papers was appraised using standard tools. The characteristics of screened papers were described, and a deductive qualitative content analysis methodology was applied to analyse the interventions and findings of included studies using a conceptual framework.
Fifteen papers were included in the review; the majority were described about many biological activity of thiazole nucleus. Seven papers were find that had impacted upon the thaizoles as antimalarials. Some papers focused on the design, synthesis and antimalarial activity evaluation of thiazole derivatives. This review identified and made a SAR (Structure Activity Relationship) of substituted thiazole nucleus as possible new antimalarials.
This review describes ongoing research in the search for novel thiazoles as targets and new antimalarial drug molecules.
杂环化合物是医学上重要化合物的主要类别。许多结构中带有五元环的杂环化合物具有良好的生物活性谱。噻唑是一类重要的五元杂环化合物。由于存在各种反应可能性,噻唑及其衍生物表现出广泛的生物活性。噻唑杂环核存在于几种强效药理活性分子中,如磺胺噻唑(抗菌药物)、利托那韦(抗逆转录病毒药物)、替拉扎明(抗肿瘤药物)和阿巴芬净(抗真菌药物)等。在药物化学领域,研究人员仍在继续寻找一些新型生物活性噻唑。本综述的目的是识别并尝试建立取代噻唑核作为可能的新型抗疟药的构效关系(SAR)。
作者使用聚焦的综述问题和纳入/排除标准,对书目数据库进行结构化搜索,以获取经同行评审的研究文献。使用标准工具评估检索到的论文质量。描述筛选论文的特征,并应用演绎定性内容分析方法,使用概念框架分析纳入研究的干预措施和结果。
该综述纳入了15篇论文;大多数论文描述了噻唑核的多种生物活性。发现有7篇论文对噻唑作为抗疟药有影响。一些论文专注于噻唑衍生物的设计、合成和抗疟活性评估。本综述识别并建立了取代噻唑核作为可能的新型抗疟药的构效关系(SAR)。
本综述描述了在寻找新型噻唑作为靶点和新型抗疟药物分子方面正在进行的研究。