分子杂交是药物化学中的最新策略之一,其通过组合两个或更多个药效部分来合成具有更好亲和力和功效的新型杂合分子。分子杂交,即,链接器或框架集成技术,可用于连接两种药效成分。通常已经发现杂化化合物比它们的母体分子更有效并且具有更低的毒性。为了创造新一代有效和安全的治疗候选人,比如抗癌,抗病毒,抗艾滋病毒,抗氧化剂,和抗菌,对于各种前线疾病,已经发表了几篇文章,讨论了临床前或临床证实的化合物的分子杂交。Isatin及其衍生物因其具有多样化的生物活性而被广泛研究,包括抗肿瘤,抗菌,抗炎,镇痛药,抗病毒,抗氧化剂,抗惊厥活性,等。同样,1,2,3-三唑作为用于产生大量药学上有意义的分子的药物化学中的生物等排物已经受到了极大的关注。由于它具有多样化的理化性质,如氢键形成能力,易于合成,中等偶极矩,对酸性/碱性水解的稳定性,对氧化/还原剂的惰性,以及与几个生物靶标的良好结合潜力,是药物化学家开发新型药物的重要选择。本综述的目的是总结研究文章,这些文章显示了含有靛蓝和1,2,3-三唑部分的杂化分子的药理学意义。本文的综述可以帮助化学家设计和合成具有更好功效和低细胞毒性的靛蓝-1,2,3-三唑杂化物。
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.