1234200-05-5Relevant articles and documents
Synthesis and in vitro evaluation of substituted pyrimido[5,4-d]pyrimidines as a novel class of Antimycobacterium tuberculosis agents
Bacelar, Ana H.,Carvalho, M. Alice,Proen?a, M. Fernanda
, p. 3234 - 3239 (2010)
Novel pyrimido[5,4-d]pyrimidines were efficiently synthesized and evaluated for antibacterial activity against Mycobacterium tuberculosis strain H 37Rv. This new structural class of compounds showed high activity against the bacilli. The activity depends on the substituents present in N-3 and C-8 of the pyrimido[ 5,4-d]pyrimidine core. Compounds having a 4-MeOC 6H4, a Ph or a 4-FC6H4 group as the substituent on C-8 and a 4′-pyridinyl, a Ph or 2′-furyl group as the substituent on N-3 were active. The highest activity was registered for compounds having 4- FC6H4 or 4-MeO C6H 4 as substituents in C-8 and a heteroaryl group as substituent in N-3. The new compounds showed high potency and promising antitubercular activity, as is the case of N-[8-[(4-fluorophenyl)amino]-4-iminopyrimido[5,4-d] pyrimidin- 3(4H)-yl]isonicotinamide with an IC90= 3.58 μg/mL, and should be regarded as new hits for further development as a novel class of Antimycobacterium tuberculosis agents.
