Synthesis and Anti-Inflammatory Effect of Some More New Fluorinated 3-Substituted Amino/ 3,5-Diamino-1,2,4-Triazine Derivatives as Lamotrigine Analogs.

AIM AND OBJECTIVE: It is known that the Lamotrigine drug has anti-inflammatory activity. So it was the goal to prepare similar compounds containing fluorine atoms (fluorine-substituted 3,5-diamino-6-aryl- 1,2,4-triazines) as Lamotrigine drug analogs to evaluate them as an anti-inflammatory. MATERIALS AND METHODS: The novel fluorine substituted 3,5-diamino-6-aryl-1,2,4-triazines as new Lamotrigine analogs were prepared via aminolysis and/ or ammonolysis of the corresponding 3-thioxo-6-aryl-1,2,4-triazin- 5-ones in ethanolic media. RESULTS: All the new targets were deduced upon their elemental analysis and spectral data as well as screened as anti-inflammatory agents, where we found that the fluorinated systems 15 and 9-11 exhibited high and more activity. CONCLUSION: Simple routes to synthesize some more novel fluorinated Lamotrigine analogs have been reported. The new targets exhibited high and moderate anti-inflammatory probes. Presence of both amino and CF3 groups caused high biological activities of these compounds were studied.

Synthesis of Novel Fluorine Compounds Substituted-4-thiazolidinones Derived from Rhodanine Drug as Highly Bioactive Probes.

AIM AND OBJECTIVE: It is known that rhodanine drug has various biocidal activities. The aim of this work was to improve the structure of rhodanine drug via alkylation at N, S, and O- centers in addition to the introduction of fluorine atoms. The new fluorinated modified rhodanines 2-16 were evaluated as enzymatic probes for cellobiase activity produced by fungi and as CDK2 inhibitors of tumor cells. MATERIALS AND METHODS: Novel fluorine substituted N-alkyl, S-alkyl and amino-rhodanines were obtained via Hydroxy methylation, Mannich reactions, chlorination and amination of 5-(4'-fluorophenylene)-2-thioxothiazolidin- 4-one, and the enzymatic effects of cellobiase produced by fungi and /or CDK2 inhibition of tumor cells were evaluated. RESULTS: Most of the targets were obtained in high yield and in the form of very pure crystals with characteristic colors. Only compounds 5, 8, 10, 13, and 14 exhibited a higher activity as cellobiase while compounds 2 and 5 showed a highly enzymatic effect on tumor cells. In addition, compounds 2 and 10 can be used as Olomoucine (standard referees). CONCLUSION: Various N, S and O-alkyl derivatives of fluorine-substituted rhodanines were prepared via a simple method and used as enzymatic probes for cellobiase activity produced by fungi and CDK2 inhibitors for tumor cells. The more bioactive compounds had rich fluorine atoms as p-fluorophenyl and p-fluorobenzoyl bearing N, S, O-alkyl rhodanine. The highly active compounds may be used as enzymatic materials for various biological transformations in the future.

A Convenient Methods for Synthetic Isomeric Structures of Pyrimido-1,2,4-triazine Derivatives as Biocidal Agents.

Some new isomeric structures of pyrimido[2,1-c][1,2,4]triazines 4-8 and 10-14 have been synthesized via the ring closure reactions of 2-hydrazinyl-1-methylpyrimidine 3 and/or 2-hydrazinopyrimidine 9 with acyclic and cyclic oxygen compounds under various conditions. Structures of the targets have been established from their elemental analyses and spectral data (UV, IR, 1H/13C NMR and mass spectrometry). Most of the obtained compounds were evaluated as antimicrobial agents and compared with pipericillin and mycostatine as standard antibiotics. Only compound 7 had highly biocidal effects.