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 and biological evaluation of some novel urea and thiourea derivatives of isoxazolo[4,5-d]pyridazine and structurally related thiazolo[4,5-d]pyridazine as antimicrobial agents.

This study reports the synthesis of some novel isoxazolo[4,5-d]pyridazines and structurally related thiazolo[4,5-d]pyridazines, and their biological evaluation as antimicrobial agents. The proposed compounds were designed to contain pharmacophores such as urea, thiourea, sulfonylurea (thiourea) and some derived functionalities that are believed to contribute to the anticipated biological activities. The results revealed that 25 compounds displayed broad spectrum of antibacterial activity, with greater inhibitory effect on the growth of the tested Gram positive strains compared to Gram negative ones. Moreover, 14 compounds were able to produce appreciable growth inhibitory activity against Candida albicans fungus when compared to Clotrimazole. Most of the tested isoxazolo[4,5-d]pyridazines displayed better antimicrobial profile than their corresponding thiazolo[4,5-d]pyridazine congeners. Four compounds namely, p-(3,7-dimethyl-4-oxo-4H-isoxazolo [4,5-d]pyridazine-5-yl)benzenesulfonylthioureas (11c-d), 3-substituted-2-[p-(3,7-dimethyl-4-oxo-4H-isoxazolo[4,5-d]pyridazine-5-yl)-benzene-sufonylimino]-4-oxothiazolidines (13d) and p-(2,7-dimethyl-4-oxo-4H-thiazolo[4,5-d]pyridazin-5-yl)benzenesulfonylthiourea (24c) were found to be most active antimicrobial members in present study.