2-Aryl-Benzoimidazoles as Type II NADH Dehydrogenase Inhibitors of .

The nonproton pumping type II NADH dehydrogenase in is essential for meeting the energy needs in terms of ATP under normal aerobic and stressful hypoxic environmental states. Type II NADH dehydrogenase conduits electrons into the electron transport chain in , which results in ATP synthesis. Therefore, the inhibition of NDH-2 ensures the abolishment of the entire ATP synthesis machinery.

Antitubercular activity of 2-mercaptobenzothiazole derivatives targeting type II NADH dehydrogenase.

() type II NADH dehydrogenase (NDH-2) transports electrons into the mycobacterial respiratory pathway at the cost of reduction of NADH to NAD and is an attractive drug target. Herein, we have synthesised a series of 2-mercaptobenzothiazoles (C1-C14) and evaluated their anti-tubercular potential as NDH-2 inhibitors. The synthesised compounds C1-C14 were evaluated for MIC and ATP depletion against H37Ra, , and H37Rv mc 6230.

Cytochrome oxidase: an emerging anti-tubercular drug target.

Cytochrome (cyt-) oxidase, one of the two terminal oxidases in the () oxidative phosphorylation pathway, plays an indispensable role in maintaining the functionality of the metabolic pathway under stressful conditions. However, the absence of this oxidase in eukaryotic cells allows researchers to select it as a potential drug target for the synthesis of anti-tubercular (anti-TB) molecules. Cyt- inhibitors have often been combined with cytochrome / super-complex inhibitors in anti-TB drug regimens to achieve a desired bactericidal response.

DNA topoisomerases as a drug target in Leishmaniasis: Structural and mechanistic insights.

Leishmaniasis, caused by a protozoan parasite, is among humanity's costliest banes, owing to the high mortality and morbidity ratio in poverty-stricken areas. To date, no vaccine is available for the complete cure of the disease. Current chemotherapy is expensive, has undesirable side effects, and faces drug resistance limitations and toxicity concerns.

Design, synthesis, and biological evaluation of 3,3'-diindolylmethane -linked glycoconjugate as a leishmanial topoisomerase IB inhibitor with reduced cytotoxicity.

Leishmaniasis, one of the neglected diseases, ranks second to malaria in the cause of parasitic mortality and morbidity. The present chemotherapeutic regimen faces the limitations of drug resistance and toxicity concerns, raising a great need to develop new chemotherapeutic leads that are orally administrable, potent, non-toxic, and cost-effective. Several research groups came forward to fill this therapeutic gap with new classes of active compounds against leishmaniasis, one such being 3,3'-diindolylmethane (DIM) derivatives.

Visible light induced regioselective C-3 thiocyanation of imidazoheterocycles through naphthalimide dye based photoredox catalysis.

A visible light induced C-3 thiocyanation of imidazo[1,2-]pyridines by using a naphthalimide based photoredox catalyst has been reported. Tolerance of electron withdrawing and donating groups at different positions of the imidazo[1,2-]pyridine ring led to a wide substrate accessibility of this method. This methodology is further reproducible with other heterocycles like benzo[]imidazo[2,1-]thiazoles, indoles, azaindoles, and anilines.