Shalmali Nishtha, Ali Md Rahmat, Bawa Sandhya
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi-110062. India.
Mini Rev Med Chem. 2018;18(2):142-163. doi: 10.2174/1389557517666170228113656.
In recent years, a drastic rise has been observed in incidences of resistance, low efficacy rates and toxicities to various drugs used in therapeutic application. Presence of imidazole nucleus in several categories of therapeutic agents such as anti-microbials, anti-virals, anti-cancer, etc has made it a vital anchor for the development of new therapeutic agents. Still, there is a need to couple the newest information with the already available knowledge to recognize the present standing of imidazole motif in medicinal chemistry research. In the present review, importance of this nucleus in some less explored activities like anti-malarial and anthelmintic is mentioned along with well explored fields like cancer. Substitution pattern around imidazole nucleus is discussed here with an aim to help medicinal chemists for the development of SAR of imidazole based compounds for each activity. This discussion will further help in the advancement of existing imidazole derivatives and in the generation of new and safe imidazole compounds.
近年来，人们观察到用于治疗的各种药物的耐药性、低效率和毒性发生率急剧上升。在几类治疗剂如抗菌剂、抗病毒剂、抗癌剂等中存在咪唑核，这使其成为新型治疗剂开发的重要关键。然而，仍有必要将最新信息与现有知识相结合，以认识咪唑基序在药物化学研究中的现状。在本综述中，除了癌症等已充分研究的领域外，还提到了该核在一些较少探索的活性如抗疟疾和驱虫方面的重要性。本文讨论了咪唑核周围的取代模式，旨在帮助药物化学家开发基于咪唑的化合物针对每种活性的构效关系。这一讨论将进一步有助于现有咪唑衍生物的改进以及新型安全咪唑化合物的产生。
