Recent Progress on Pyrazole Scaffold‐Based Antimycobacterial Agents

Abstract

New and reemerging infectious diseases will continue to pose serious global health threats well into the 21st century and according to the World Health Organization report, these are still the leading cause of death among humans worldwide. Among infectious diseases, tuberculosis claims approximately 2 million deaths per year worldwide. Also, agents that reduce the duration and complexity of the current therapy would have a major impact on the overall cure rate. Due to the development of resistance to conventional antibiotics there is a need for new therapeutic strategies to combat Mycobacterium tuberculosis. Subsequently, there is an urgent need for the development of new drug candidates with newer targets and alternative mechanism of action. In this perspective, pyrazole, one of the most important classes of heterocycles, has been the topic of research for thousands of researchers all over the world because of its wide spectrum of biological activities. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review, we have collated published reports on the pyrazole core to provide an insight so that its full therapeutic potential can be utilized for the treatment of tuberculosis. In this article, the possible structure-activity relationship of pyrazole analogs for designing better antituberculosis (anti-TB) agents has been discussed and is also helpful for new thoughts in the quest for rational designs of more active and less toxic pyrazole-based anti-TB drugs.

Development of New Pyrazole Hybrids as Antitubercular Agents: Synthesis, Biological Evaluation and Molecular Docking Study

“…Pioneering scientists had reported pyrazole and its derivatives for an extensive range of pharmacological activities such as antipyretic, analgesic, antimicrobial, anticancer, antitubercular, antiviral, antihypertensive, antioxidant, antidepressant, and anxiolytic [5][6][7]. Rangappa S. Keri et al reviewed and discussed the possible structure-activity relationship of different types of pyrazole scaffold for designing of better antitubercular agents [8]. Synthetic analogues of pyrazole are known to exhibit significant antitubercular activity especially 1, 3-diphenyl pyrazole motif is known to be a potent antitubercular agent ( fig.…”

Fluorous Supported Synthesis of Pyrazolone Derivatives From Allylic Alcohols Using a Palladium-Catalyzed Strategy

“…To a 3, 3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,10-heptadecafluorodecyl--acrylate (2 g, 3.86 mmol, 1 eq) was added DABCO (490 mg, 3.86 mmol, 1 eq) and 2 eq of aldehyde (R 1 CHO) in neat conditions. After stirring at room temperature for 48 h, the crude reaction mixture is diluted in CH 2 Cl 2 (30 mL), washed three times with water and dried over anhydrous sodium sulphate.…”

“…The reaction was then quenched by addition of sat. NH 4 Cl followed by addition of 1 mol L -1 HCl until the pH was acid. The mixture was extracted with diethyl ether.…”

“…[1][2][3][4] They were first extensively developed for their anti-inflammatory, 5 analgesic 6 and antipyretic 7 properties. More recently, great attention has been paid to their versatile role as antimicrobial, 8 antiparasitic, 9 antiviral 10 and antineoplastic 11 agents.…”

Microwave-Assisted Synthesis and Cytotoxicity Evaluation of Some Novel Pyrazole Containing Imidiazole, Pyrazole, Oxazole, Thiadiazole and Benzochromene derivatives

“…1). Various five membered heterocycles like 1,3,4-thiadiazole derivatives attracted a great attention due to their wide range of biological activities such as antimicrobial [23], antituberculosis [24], antifungal [25], diuretic agents [26], and anticancer [27]. Microwave assisted technique has attracted a great attention of chemists in current organic synthesis [28,29] due to its unique advantages, such as higher yields, reduced pollution, shorter reaction times and low cost.…”