Synthesis, biological activity, and evaluation of the mode of action of novel antitubercular benzofurobenzopyrans substituted on A ring

Design and synthesis of novel carbazolo–thiazoles as potential anti-mycobacterial agents using a molecular hybridization approach

“…The various starting material i.e. These findings were further substantiated from their respective 13 C-NMR spectra of the title compounds. Further, compound (1) was subjected to formylation reaction (Vilsmayer Hack) in the presence of POCl 3 and DMF to afford 9-methyl-carbazole-3-carbaldehyde (2),which was further treated with thiosemicarbazide in the presence of methanol and catalytic glacial acetic acid to yield 1-((9-methyl-carbazol-6-yl methylene)thiosemicarbazide (3).…”

“…9-methyl-carbazole (1) was prepared from commercially available carbazole by N-methylation process using iodo-methane and sodium hydride. The characteristic 13 In addition, the desired title compounds 6 (a-o) were synthesized by Hantzsch cyclo-condensation reaction of compound (3) with various appropriately substituted α-Bromoaromatic/heteroaromatic ketones 5 (a-o) in the presence of methanol.…”

“…1 The literature reported derivatives of carbazoles and thiazoles along with their anti-mycobacterial activities [11][12][13][14][15][16][17] . Fig.…”

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

“…In contrast, electron donating group substitutions such as hydroxy or methoxy show a significant increase in activity (62, figure 21). While all compounds showed a possible mechanism of action of interaction with lipid biosynthesis of the M. tuberculosis cell wall, a specific compound was an epoxy-mycolate synthesis inhibitor (Termentzi et al, 2010). Other compounds containing a phthalimide moiety have been described as biophoro to design new prototypes of drug candidates with different biological activities.…”

Antitubercular drugs: advances in nitrogen containing heterocyclic compounds and some other derivatives

“…All these compounds showed a possible mechanism of action of interaction with lipid biosynthesis of the M. tuberculosis cell wall and act as an epoxy--mycolate synthesis inhibitor. 37 Other compounds with phthalimide moiety have described as biophoro to design new drugs with different biological activities. The hybridization of both phthalimide (thalidomide) and sulfonamide (dapsone) moiety leads to compounds with antileprotic activity.…”