Tasneem Taj

One-pot synthesis of pyrazoline derivatised carbazoles as antitubercular, anticancer agents, their DNA cleavage and antioxidant activities.

Novel tricyclic carbazoles 4a-k were synthesized in one-pot employing sydnone derivatives 3a-k as masked hydrazines by the ring transformation in presence of conc. HCl and cyclohexanone. The title compounds were screened for anti-tubercular, anti cancer, DNA cleavage, antioxidant activity. MIC, GI50, LC50, TGI were evaluated. The title compounds have exhibited significant antitubercular, DNA cleavage and antioxidant activities and partial anticancer activity.

An efficient one-pot cyclization of quinoline thiosemicarbazones to quinolines derivatized with 1,3,4-thiadiazole as anticancer and anti-tubercular agents

A series of 6,7,8-substituted thiosemicarbazones (2a–j) of 2-chloro-3-formyl-quinoline derivatives were cyclized to the title compounds (3a–j) using acetic anhydride. The structures of the final compounds (3a–j) were confirmed by elemental and spectral (IR, 1H NMR and MS) analysis. Some of the title compounds have shown promising anticancer and antitubercular activities.

Synthesis of novel imidazo[2,1-b][1,3,4]thiadiazoles appended to sydnone as anticancer agents

A novel series of 3-aryl-4{6′-(6′′-substituted-coumarin-3′′-yl) imidazo[2,1-b][1,3,4]thiadiazol-2′-yl}-sydnones 5h–5s were synthesized and screened for their anticancer and DNA cleavage activities and analyzed for pharmacological parameters such as toxicity, drug-likeliness, and drug score for oral bioavailability. In vitro toxicity assay was carried out by assessing the survival E. coli AB1157 (wild type) cultures. Some of the compounds have shown significant anticancer activities also.

Synthetic utility of sydnones: synthesis of pyrazolines derivatized with 1,2,4-triazoles as antihyperglymic, antioxidant agents and their DNA cleavage study

Ring transformation of sydnone (1a–i) to 1,3,4-oxadiazoline-2-one (2a–i) was carried out using bromine in acetic anhydride. The compounds (2a–i) on heating with hydrazine hydrate gave 1,2,4-triazole (3a–i) in good yields. The structure of these unknown compounds was confirmed by IR, 1H NMR, MS and elemental analysis. Further, these compounds were evaluated for the extent of penetration into biological membranes (clogP) drug likeliness and finally drug score was calculated. The title compounds were also screened for their antihyperglycemic, DNA cleavage and antioxidant activity.

Synthesis of Novel 1,2,4-Triazole Derivatives as Antimicrobial Agents via the Japp-Klingemann Reaction: Investigation of Antimicrobial Activities

In the present investigation, 1,2,4-triazole appended to pyrazoline and pyrazole rings (4a–g) using N-arylsydnone as synthon was prepared. The title compounds were subjected to Osiris property explorer for the oral bioavailability to analyze their drug likeness and drug score. Further, the compounds were subjected to the antimicrobial activity and analyzed the IC 50 and MIC values.