2,4-Dialkyl-8,9,10,11-tetrahydrobenzo[g]pyrimido[4,5-c]isoquinoline-1,3,7,12(2H,4H)-tetraones as new leads against Mycobacterium tuberculosis

Synthesis, biological evaluation and 3D QSAR study of 2,4-disubstituted quinolines as anti-tuberculosis agents

“…More recently, a large number of reports on the design of synthesis of several new and versatile classes of anti-tuberculosis agents have appeared [10][11][12][13][14].…”

“…The compounds 3-10 were converted to 4-(1-cycloalkyl)quinoline-2-carbohydrazides (11)(12)(13)(14)(15)(16)(17)(18)(19) …”

“…6H);13 C NMR (CDCl 3 ): δ 162.9, 157.7, 147.9, 147.7, 131.6, 128.8, 128.2, 126.4, 126.3, 115.8, 42.1, 39.1, 36.8, 28.9; analysis for C 20 H 22 N 2 O 2 (322.4) calcd C, 74.51; H, 6.88; N, 8.69; found: C, 74.48; H, 6.84; N, 8.68.…”

Design, synthesis, and characterization of (1-(4-aryl)-1<em>H</em>-1,2,3-triazol-4-yl)methyl, substituted phenyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates against <em>Mycobacterium tuberculosis</em>

“…1,2,3-Triazoles could be easily constructed by click chemistry reaction25 and which yielded small molecules with special properties, such as moderate dipole character, hydrogen bonding capability, rigidity, and stability 26. Heterocyclic27–29 fluorine-containing compounds have been shown to exhibit promising anti-tuberculosis (anti-TB) activity,30 including 1,2,3-triazole analogs, for their promising anti-TB activity 31. Keeping this in mind and considering the pharmacological significance of dihydropyrimidine and 1,2,3-triazole pharmacophores, in the present investigation it was decided to design and synthesize a series of novel 1,2,3-triazole hybrid with dihydropyrimidinone (DHPM) scaffolds in accordance with Lipinski rule except compound 7d 32.…”

One-pot synthesis of new triazole—Imidazo[2,1-b][1,3,4]thiadiazole hybrids via click chemistry and evaluation of their antitubercular activity

“…In view of this, a great deal of research work is being devoted to identify newer molecular entities which are active against the bacterial strains. The most important molecular design strategies in this direction are (i) structural modification of the known drug molecule; 5 (ii) computer-aided drug design based on the study on ligand-protein interaction; 6 (iii) hybridisation of two active pharmacophoric units into a single molecular framework 7,8 and (iv) the random screening of different structural units and proceeding in an observed window of anti-TB activity, [9][10][11][12] all these approaches are being considered as promising to develop effective drugs.…”