Synthesis of Pteridine Derivatives as Anti-TB Agents (Research Article)

Author(s): Sweta Desai*, Zarna Dedania, and Naishadh Solanki

Abstract: Tuberculosis (TB) is a major global health issue with a high mortality rate, particularly due to the emergence of drug-resistant strains of Mycobacterium tuberculosis. Hence, the development of novel anti-TB agents is of great significance. In this regard, pteridine derivatives have emerged as a promising scaffold for the development of novel drugs. This study focuses on the synthesis of N-phenyl-6,7-dip-tolylpteridin-4-amine derivatives, and their evaluation for anti-TB activity. The three-step synthesis process involved the preparation of 6,7-dip-tolylpteridin-4-ol from 4,5-diamino-6-hydroxypyrimidine and 4,4-dimethylbenzil, followed by its reaction with phosphoryl chloride and dimethylformamide to yield 4-chloro-6,7-dip-tolylpteridine, and finally, the reaction of the latter with aniline in dimethylformamide to obtain N-phenyl-6,7-dip-tolylpteridin-4-amine derivatives. The synthesized compounds were evaluated for their anti-TB activity against standard drugs streptomycin, ciprofloxacin, and pyrazinamide. The results showed that all the compounds demonstrated significant anti-TB activity, with some displaying activity comparable to the reference drugs. Specifically, compounds E6, E8, E13, and E17 showed activity like that of streptomycin and ciprofloxacin, while compounds E3, E25, E9, E14, E19, and E4 demonstrated activity similar to pyrazinamide. In conclusion, the study highlights the potential of pteridine derivatives as promising anti-TB agents. The synthesized compounds exhibited significant anti-TB activity and could serve as an alternative to current standard therapies.

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