Design, synthesis and biological evaluation of novel triazole, urea and thiourea derivatives of quinoline against Mycobacterium tuberculosis

Synthesis of Isoxazole and 1,2,3-Triazole Isoindole Derivatives via Silver- and Copper-Catalyzed 1,3-Dipolar Cycloaddition Reaction

“…The aim of this present work focuses on the synthesis of N-heterocyclic compounds, namely the synthesis of substituted isoxazole and triazole derivatives, since an important number of compounds containing the isoxazole and the triazole scaffold are known to exhibit a variety of biological activities in the pharmaceutical [16] and medicinal areas [17]. Representative examples of synthetic drugs incorporating these motifs are Tazobactam I [18][19][20][21][22], Rufinamide II [23][24][25], phenylisoxazole derivatives III [26,27], and Bextra (Valdecoxib) IV [28][29][30].…”

“…Tazobactam I [18][19][20][21][22], Rufinamide II [23][24][25], phenylisoxazole derivatives III [26,27], and Bextra (Valdecoxib) IV [28][29][30].…”

Crystal structure of 3-(2-bromophenyl)-1,1-dimethylthiourea, C9H11BrN2S

“…Thiourea derivatives show various biological activities [2][3][4][5]. Therefore, the synthesis of such compounds is of general interest.…”

Oxyhalogen-sulfur chemistry: Kinetics and mechanism of oxidation of n-acetylthiourea by aqueous bromate and acidified bromate

“…1 Thiourea and its derivatives are thus a vast group of very active biological molecules. [2][3][4][5][6][7][8] Major pathway to their bioactivation is oxidative and specifically via S-oxygenation in which there is a successive addition of oxygen to the sulfur center until oxidative saturation is attained at sulfate. [9][10][11] Small molecule thioureas are oxygenated predominantly by catalysis from the flavin-containing monooxygenases 12,13 to form reactive sulfenic acids that reversibly react with glutathione [14][15][16][17][18][19] to drive oxidative stress through a redox cycle.…”