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Triazine nuclei have occupied a propitious place in pharmaceutical chemistry due to their diverse biological behaviour. The marketed drugs such as Azacitidine, Melarsoprol, Altretamine and Almitrine display broad pharmacological activities like anti‐cancer, anti‐parasitic, anti‐inflammatory, Respiratory stimulant and many more. Literature studies reveal that the 2, 4, and 6 substitution on s‐triazine is important for varied biological activities. This diversity in pharmacological activities of triazine scaffold has fascinated the various researchers to further investigate its applications in the treatment of several diseases. This review is complementary to earlier reports and aims to review the work reported on various synthetic methods and biological activities of substituted s‐triazine derivatives from 2016 to 2020 with a list of patents. The enriched structure‐activity relationship may open the doors for further rational drug development of s‐triazine containing analogues as good clinical candidates.

A total of 19 linezolid-based novel molecules (6 a-d, 8 a-d and 10 a-k) were synthesized by utilizing a simple and convenient synthetic method. Structures of all the novel derivatives were established by 1 H, 13 C NMR, FT-IR and mass spectroscopic methods. In addition, structural elucidation of some representative compounds by 19 F, 2D NMR and single crystal X-ray experiment's (6 d and 8 b) further confirmed the structures of the desired compounds. All the final compounds were evaluated for their in vitro antitubercular (Mycobacterium tuber-culosis H 37 RV strain), antibacterial (S. aureus, B. subtilis, E. coli and P. aeruginosa) and antifungal (C. neoformans, C. albicans and A. niger) activities. The docking study of most active compounds were also performed towards 50S ribosomal unit of Haloarcula marismortui. The Lipinski's rule of five and significant ADME pharmacokinetic parameters were also analysed indicating potential to develop good oral antimicrobial and antitubercular drug candidates.

We demonstrate a simple yet efficient one-pot synthesis of two triazolotriazine isomers via DBU mediated Dimroth type rearrangement with excellent yields.