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关于色胺-1,2,3-三唑杂合体的药理学意义的小型综述。

A Mini Review on Pharmacological Significance of Isatin-1,2,3-Triazole Hybrids.

机构信息

Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana 125001, India.

出版信息

Curr Top Med Chem. 2023;23(10):833-847. doi: 10.2174/1568026623666230202160925.

Abstract

Molecular hybridization is one of the recent stratagems in medicinal chemistry to synthesize a novel hybrid molecule having better affinity and efficacy by combining two or more pharmacophoric moieties. Molecular hybridization, i.e., a linker or framework integration technique, can be used to connect the two pharmacophoric components. It has often been found that hybrid compounds perform more effectively and possess lower toxicity than their parent molecules. In order to create a new generation of effective and safe therapeutic candidates, such as anti-cancer, anti-viral, anti-HIV, antioxidant, and antibacterial, for a variety of frontline diseases, several articles have been published that discuss the molecular hybridization of preclinically or clinically proven compounds. Isatin and its derivatives have been studied extensively due to diversified biological activities, including antitumor, antimicrobial, anti-inflammatory, analgesic, antiviral, antioxidant, anticonvulsant, etc. Similarly, 1,2,3-triazoles have received significant interest as a bio-isostere in medicinal chemistry for generating a large number of pharmaceutically significant molecules. As it possesses diversified physiochemical properties, such as hydrogen bond formation capacity, ease of synthesis, moderate dipole moment, stability towards acidic/basic hydrolysis, inertness towards oxidizing/ reducing agents, and good binding potential with several biological targets, triazole is an important choice of the medicinal chemists for the novel medication development. The aim of the current review is to summarize the research articles showing the pharmacological significance of hybrid molecules containing isatin and 1,2,3-triazole moieties. The present review may assist chemists in designing and synthesizing isatin-1,2,3-triazole hybrids with better efficacy and low cytotoxicity.

摘要

分子杂交是药物化学中的最新策略之一,通过将两个或多个药效团结合在一起,可以合成具有更好亲和力和疗效的新型杂合分子。分子杂交,即连接子或框架整合技术,可用于连接两个药效团成分。人们经常发现,杂合化合物比其母体分子更有效,毒性更低。为了开发新一代有效的、安全的治疗候选物,如抗癌、抗病毒、抗 HIV、抗氧化和抗菌药物,用于治疗各种一线疾病,已经发表了几篇讨论临床前或临床证明的化合物的分子杂交的文章。由于具有多样化的生物活性,包括抗肿瘤、抗菌、抗炎、镇痛、抗病毒、抗氧化、抗惊厥等,色酮及其衍生物得到了广泛的研究。同样,1,2,3-三唑因其具有多样化的物理化学性质,如氢键形成能力、易于合成、适中的偶极矩、对酸/碱性水解的稳定性、对氧化/还原试剂的惰性以及与多个生物靶标良好的结合潜力,已成为药物化学中产生大量具有重要意义的药物分子的生物等排体之一。三唑是药物化学家用于新型药物开发的重要选择。本综述的目的是总结显示含有色酮和 1,2,3-三唑部分的杂合分子的药理意义的研究文章。本综述可能有助于化学家设计和合成具有更好疗效和低细胞毒性的色酮-1,2,3-三唑杂合分子。

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