Journal
MOLECULES
Volume 27, Issue 1, Pages -Publisher
MDPI
DOI: 10.3390/molecules27010276
Keywords
phenothiazine; molecular hybridization; antimicrobial; antitumor; anti-Alzheimer; pharmacophore
Funding
- national funds through the Portuguese Foundation for Science and Technology/MCTES [UIDB/00709/2020, UIDP/00709/2020]
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The molecular hybridization approach has been utilized to develop compounds with improved efficacy by combining pharmacophores of bioactive scaffolds. Hybridizing phenothiazine derivatives with various relevant pharmacophores has resulted in compounds with diverse biological activities, interacting with specific or multiple targets. The pharmacological actions of phenothiazine hybrids include antibacterial, antifungal, anticancer, anti-inflammatory, antimalarial, analgesic, and multi-drug resistance reversal properties.
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.
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