Synthesis of fused 1,2,4-triazines as potential antimicrobial and antitumor agents

An effective one-pot access to polynuclear dispiroheterocyclic structures comprising pyrrolidinyloxindole and imidazothiazolotriazine moieties via a 1,3-dipolar cycloaddition strategy

“…The pyrimido[5,4- e ]-1,2,4-triazine constitutes the core of the antibiotics fervenulin, xanthothricin, and reumycin [33–34]. Other hetero-annelated 1,2,4-triazines reveal antiviral effect against influenza A and B viruses [35], anti-HIV and anticancer [36–37], antimicrobial and antifungal activities as well as cytotoxicity to MCF-7 cells [38–39]. Based on these observations we therefore aimed at combining the spiropyrrolidinyloxindole motif with hetero-annelated 1,2,4-triazine scaffolds.…”

Design, Synthesis and Pharmacological Evaluation of Novel Annelated Pyrimido[2,1-<em>c</em>][1,2,4]Triazolo[3,4-<em>f</em>][1,2,4]Triazines as Antimicrobial Agents

“…The chloro triazine 6 underwent further, hydrazinolysis with excess of N2HNH2.H2O to afford the hydrazinyltriazine derivative 7, which undergoes further cyclization aiming at exploring the reactivity of its hydrazinyl tag, in building triazolotriazine derivatives. Thus, the hydrazinyl 7 was underwent to various one carbon donors, to afford the target azoles and/or azines (8,(10)(11)(12), (Scheme 2). The structures of isolated products (8, 10-12), were confirmed via spectral data together with correct elemental analyses (Tables 1 and 2).…”

“…which have important biological activities as antiviral drugs [4]. Tumor growth inhibitors [5][6][7][8], antiviral [9], antibacterial, and antifungal [8,10].…”

Cascade of Michael Addition/Retro‐Michael Reaction/Skeletal Rearrangement in the Synthesis of Arylmethylidene Derivatives of Imidazothiazolotriazines

“…Thus, azolo[5,1‐ c ][1,2,4]triazines possess antiviral, antidiabetic, cytotoxic and antioxidant activities . 1,2,4‐Triazino[2,1‐ a ][1,2,4]triazines and 1,2,4‐triazino[4,5‐ a ]benzimidazoles exhibit antimicrobial and antiproliferative effects . 1,2,4‐Triazino[5,6‐ b ] indoles are antileishmanial agents against Leishmania donovani .…”