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A standard goal of medicinal chemists has been to discover efficient and potent drug candidates with specific enzyme-inhibitor abilities. In this regard, boron-based bioactive compounds have provided amphiphilic properties to facilitate interaction with protein targets. Indeed, the spectrum of boron-based entities as drug candidates against many diseases has grown tremendously since the first clinically tested boron-based drug, Velcade. In this review, we collectively represent the current boron-containing drug candidates, boron-containing retinoids, benzoxaboroles, aminoboronic acid, carboranes, and BODIPY, for the treatment of different human diseases.In addition, we also describe the synthesis, key structure–activity relationship, and associated biological activities, such as antimicrobial, antituberculosis, antitumor, antiparasitic, antiprotozoal, anti-inflammatory, antifolate, antidepressant, antiallergic, anesthetic, and anti-Alzheimer’s agents, as well as proteasome and lipogenic inhibitors. This compilation could be very useful in the exploration of novel boron-derived compounds against different diseases, with promising efficacy and lesser side effects.

Benzo[c][1,2,5]oxadiazoles and benzo[c][1,2,5]thiadiazoles are recognized to possess potent pharmacological activities including anticancer potential. In continuation of our research endeavors in the development of boron-based heterocycles as potential therapeutic agents, herein we report the design and synthesis of new series of boron-based benzo[c][1,2,5]oxadiazoles and benzo[c][1,2,5]thiadiazoles as anticancer agents targeting tumor hypoxia. A series of seventeen compounds were synthesized in two steps in an efficient manner via substitution reactions followed by subsequent hydrolysis of aryltrifluoroboronate salts into corresponding boronic acid derivatives in the presence of silica. This is the first example to develop boron-based hypoxia agents. The synthesized hybrids were characterized by suitable spectroscopic techniques. The biological studies are currently underway.

Aim: The purpose of the study was to investigate the effect of different compounds from leaves of Gymnema sylvestre (GS) on nitric oxide (NO) production. Materials and Methods: To study the binding and effect of different compounds from GS 10 molecules were docked on the enzyme endothelial NO synthase (eNOS) using molegro virtual docker and the result was compared with that of the agonists (acetylcholine, bradykinin, and serotonin). Further to confirm the activity animal studies were done on albino rats blood glucose levels were measured using glucometer and NO levels were estimated spectrophotometrically using griess agent. Results: Docking studies showed that almost all the compounds from the leaves of GS bind perfectly with eNOS with the lowest binding energies similar to that of the agonists. Animal studies confirmed the docking results when blood glucose levels decreased and NO levels increased in diabetic rats treated with GS leaf extract. Conclusion: Docking and animal studies show that leaf extract of GS might help in improving the production of NO by stimulating eNOS and thus, can be used as an agent to avoid diabetes and diabetic vascular complications.

The authors have withdrawn their manuscript owing to massive revision and data validation. Therefore, the authors do not wish this work to be cited as reference for the project. If you have any questions, please contact the corresponding author.