Click-chemistry-based multicomponent condensation approach for design and synthesis of spirochromene-tethered 1,2,3-triazoles as potential antitubercular agents

A Mini Review on Isatin, an Anticancer Scaffold with Potential Activities against Neglected Tropical Diseases (NTDs)

“…The synthesized scaffold, 65 , exhibited promising antimycobacterial activity on Mtb H 37 Ra and M. bovis BCG, with MIC values of 5.21 and 2.97 μg/mL, respectively ( Figure 10 ). The SAR studies revealed the dependence of activity on the nature of the substituents on the phenyl rings, with a preference for halogen [ 82 ].…”

The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules

“…The obtained compounds were then tested against MTB, using the XTT reduction menadione assay (XRMA), and M. bovis (BCG), using the nitrate reductase assay, both in active and dormant stage, and evaluating two parameters e MIC and IC 50 , using rifampicin as positive control. Compounds 82e84 and 85e89 displayed interesting bioactivity and good selectivity (Scheme 21B), as they did not demonstrate relevant cytotoxicity towards three different cell lines (MCF-7, HCT116 and A549) [95].…”

Recent Developments on Five-Component Reactions

“…Desai and co-workers introduced a reaction of benzyl halides, N-propargyl isatins, sodium azide, malononitrile, and 5,5-dimethyl-1,3-cyclohexanedione (3a), 6-methyl-2Hpyran-2,4(3H)-dione (3b) or 4-hydroxycarbazole (3c) for the synthesis of 1,2,3-triazoletethered spirochromenocarbazoles 4, 5 or 6 using cellulose-supported CuI nanoparticles (Cell-CuI NPs) as a reusable catalyst (Scheme 3) [13,14]. The first step is the condensation of N-propargyl isatins, malononitrile and 3a, followed by cyclization to form spirochrome-is captured by SO 2 to form arylsulfonyl radical which then attacks the terminal position of the styrenes to provide intermediate radicals 9.…”