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Pharmacologic Activities of 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4- triazines as a Privileged Scaffold in Drug Development

[ Vol. 21 , Issue. 19 ]


Zahra Zakeri Khatir and Hamid Irannejad*   Pages 2874 - 2928 ( 55 )


1, 2, 4-Triazine derivatives have received much attention due to their multifunctional nature, especially in diverse pharmacological properties as well as a key fragment in many drug candidates. Introduction of a vicinal 5, 6-diaryl/heteroaryl moiety on the 1, 2, 4-triazine ring has attracted plentiful attention in the field of medicinal chemistry. 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4- triazine is a prominent scaffold in many drug candidates, which has shown a wide range of pharmacological activities such as anti-diabetic, antifungal, anti-inflammatory, anticancer, anti-HIV, neuroprotective, anticonvulsant, anti-Alzheimer, anti-Parkinson, and antioxidant. In this review, we have discussed synthesis, various pharmacological activities of 5, 6-diaryl/heteroaryl-3-substituted-1, 2, 4- triazines, their structure-activity relationship (SAR), pharmacophoric elements, and their mechanism of action reported in the published articles during 2000-2019. Evaluation of compounds by PAINS filtering tool was accomplished and showed that this versatile structure could be considered as a privileged structure. Compilation of the biological data confirmed that position 3 of the 1,2,4-triazine is a key location to determine the affinity and selectivity of the 5,6-diaryl/heteroaryl-3-substituted-1, 2, 4- triazines towards different biologic targets. Specific geometrical and thermodynamic characters of this motif have prompted it as a frequent hitter.


1, 2, 4-triazine, 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4-triazine, Pharmacologic activity, privileged scaffold, SAR, drug.


Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari

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