SYNTHESIS AND CHARACTERIZATION OF NOVEL PYRIMIDINE-4,5-DIAMINE/ PYRIMIDINE-2,4,5-TRIAMINE AS ANTITB AGENTAbstract
Pyrimidine derivative had a wide range of biological activities, including antiTB activity. In this view, pyrimidine moiety containing N N5-(3-substituted benzylidene)-N4-phenyl and N5-(2-substituted benzylidene)-N2,N2-dimethyl-N4-phenyl compounds was designed, and a novel series of N5-(3-substituted benzylidene)-N4-phenyl pyrimidine-4,5-diamine [5A-5F]/N5-(2-substituted benzylidene)-N2,N2-dimethyl-N4-phenyl pyrimidine-2,4,5-triamine [5a-5f], were synthesized, evaluated for their antiTB activity against MTB H37Ra strain by MABA screening. Among the all 12 derivatives tested, N5-(4-methoxybenzylidene)-N4-phenylpyrimidine-4,5-diamine[5A], N5-(4-chloro benzylidene)-N4-phenylpyrimidine-4,5-diamine [5C], N5-(4-chloro benzylidene)-N2, N2-dimethyl-N4-phenyl pyrimidine-2,4,5-triamine [5c], and N5-(4-amino benzylidene)-N4-phenyl pyrimidine-4,5-diamine [5E] was found to have potent activity against MTB H37Ra strain. The compounds bearing electron-withdrawing, donating group’s substitution, and its positioning function was important to produce significant activity proved. The obtained results showed that the most active compounds could be useful as a template for future design, structural modification, and investigation to produce more active analogs.
M. S. Rao *, T. B. Rao and C. P. Koteswara
Department of Chemistry, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh, India.
05 February 2020
24 April 2020
30 April 2020
01 February 2021