CICS-UBI-Health Sciences Research Centre, University of Beira Interior, 6200-506 Covilhã, Portugal.
Molecules. 2022 Jan 3;27(1):276. doi: 10.3390/molecules27010276.
The molecular hybridization approach has been used to develop compounds with improved efficacy by combining two or more pharmacophores of bioactive scaffolds. In this context, hybridization of various relevant pharmacophores with phenothiazine derivatives has resulted in pertinent compounds with diverse biological activities, interacting with specific or multiple targets. In fact, the development of new drugs or drug candidates based on phenothiazine system has been a promising approach due to the diverse activities associated with this tricyclic system, traditionally present in compounds with antipsychotic, antihistaminic and antimuscarinic effects. Actually, the pharmacological actions of phenothiazine hybrids include promising antibacterial, antifungal, anticancer, anti-inflammatory, antimalarial, analgesic and multi-drug resistance reversal properties. The present review summarizes the progress in the development of phenothiazine hybrids and their biological activity.
分子杂交方法已被用于通过将两个或多个生物活性支架的药效团结合来开发疗效更好的化合物。在这种情况下，将各种相关药效团与吩噻嗪衍生物杂交，得到了具有多种生物活性的相关化合物，与特定或多个靶标相互作用。事实上，基于吩噻嗪系统开发新药或候选药物是一种很有前途的方法，因为与三环系统相关的多种活性，传统上存在于具有抗精神病、抗组胺和抗毒蕈碱作用的化合物中。实际上，吩噻嗪类杂种的药理作用包括有前途的抗菌、抗真菌、抗癌、抗炎、抗疟、镇痛和多药耐药逆转特性。本综述总结了吩噻嗪类杂种的发展及其生物学活性的进展。
