Design, synthesis, and biological evaluation of coumarin derivatives against tuberculosis: a pharmacophore-based approach.

Rising cases of drug resistance tuberculosis including multidrug-resistant and extensively drug-resistant emphasize the need for development of drugs with novel mechanism of action. The study aimed to explore novel inhibitors targeting Mycobacterium thymidine monophosphate kinase (Mtb TMPK), a promising but unexplored drug target for tuberculosis treatment. A library of 200 coumarin derivatives was rationally designed and screened against Mtb TMPK, an essential enzyme in nucleotide biosynthesis of mycobacterium tuberculosis.

A review on experimental and epidemiological research exploring the pathophysiology and progression of pesticide-induced diabetes mellitus.

Global epidemic of diabetes mellitus (DM) is a multifactorial metabolic disorder that includes insulin resistance, β-cell dysfunction, and chronic hyperglycemia. DM is known traditionally as lifestyle and genetic predisposition, but the role of environmental pollutants, especially pesticides, has increasingly been at the forefront of attention. Pesticides such as organophosphates, organochlorines, carbamates, and pyrethroids are strong endocrine disruptors, disturbing glucose homeostasis by inhibiting insulin signaling pathways, producing oxidative stress, and activating chronic inflammation.

Structure-Guided Development of Mycobacterial Thymidine Monophosphate Kinase (MtbTMPK) Inhibitors: Unlocking New Frontiers in Tuberculosis Research.

Researchers are actively engaged in developing new antitubercular drugs targeting the enzyme Mycobacterial Thymidine Monophosphate Kinase (MtTMPK). This newer target has specificity and selectivity over other thymidylate kinases and especially differs from human thymidylate kinase (hTMPK). Over the last two decades, various potent MtTMPK inhibitors comprised of both nucleoside and non-nucleoside structures have been developed.

Quinoline Derivatives as Promising Scaffolds for Antitubercular Activity: A Comprehensive Review.

Background: Heterocyclic compounds and their derivatives play a significant role in the design and development of novel quinoline drugs. Among the various pharmacologically active heterocyclic compounds, quinolines stand out as the most significant rings due to their broad pharmacological roles, specifically antitubercular activity, and their presence in plant-based compounds. Quinoline is also known as benzpyridine, benzopyridine, and 1-azanaphthalene.