Current Organic Chemistry - Volume 29, Issue 18, 2025

Herbal medications provide universal benefits such as effectiveness, safety, cost, and acceptance. With increased interest in plant extract research, there is also increased concern about the activity of bioactive lumberjack climber plants indigenous to Sri Lanka and Indian submontane forests. It was recently determined that plants containing kotalanol, salacinol (derived from roots, especially stems), and mangiferin (xanthone from roots) are anti-diabetic agents. Salacia reticulata (S. reticulata) contains 1,3-diketone, dulcitol, leucopelargonidin, epicatechin, furovatannin, glycoside tannin, triterpene, 30-hydroxy-20(30)-dihydroisoigesterol, hydroxyferruginol, acidic Lambert, and 16-acetate. Chemical components such as collagen in 26-hydroxy-1,3-friederandione and maitenfolate have also been discovered in S. reticulata roots. Root decoction treats skin conditions, rheumatic conditions, gonorrhoea, hemorrhoids, asthma, edema, irritation, dry mouth, menstrual cramps, and dysmenorrhea. The gastrointestinal suppression of enzymes that take over glucose through the blood reduces postprandial hyperglycemia and improves blood sugar control. Additionally, mangiferin can impede the action of aldose reductase, which delays the development or worsening of diabetes. Consequently, efforts are underway to discover new therapeutic targets, signifying a novel approach to medication development. In this regard, S. reticulata has been widely consumed owing to its discoveries and is currently the focus of substantial studies on diabetes treatment.

The multifunctionalized chiral furan derivatives are important building blocks as many natural products and bioactive compounds contain these scaffolds. The chiral furan derivatives also act as potent intermediates in valuable synthetic transformations. Therefore, the development of facile methodologies for accessing the substituted chiral furans from easily available precursors is an intriguing topic in the field of organic chemistry. In this review, several efficient strategies for the synthesis of substituted chiral furans have been discussed. Amongst these, the functionalization of furan moieties, organocatalytic/enantioselective approaches, chemoenzymatic kinetic resolution, and utilizations of carbohydrates as chiral pool precursors are of great importance.

Millions of people worldwide suffer from Alzheimer's disease (AD), a progressive neurological illness whose incidence is rising as the population ages. Since existing medicines are ineffective and mainly treat symptoms rather than delaying the course of the disease, recent research conducted in 2023 and 2024 highlights the urgent need for novel therapeutic methods. Because of its adaptable chemical structure, which enables it to interact with important enzymes and receptors involved in AD disease, the pyrazole moiety has garnered significant attention in Alzheimer's research. The ability of recent developments in the synthesis of pyrazole derivatives to inhibit the enzymes acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), which are linked to cognitive impairment in AD, has shown promise. These novel compounds may be used as multi-target therapies for AD because several of them also have anti-inflammatory, anti-amyloid, and antioxidant properties. These pyrazole-based substances have demonstrated neuroprotective benefits in preclinical studies by lowering the generation of amyloid-beta plaque and shielding neurons from oxidative stress, two important processes in the development of AD. Pyrazole-based drugs may prove to be a useful addition to AD therapy choices as researchers work to improve these derivatives for increased bioavailability and fewer adverse effects. These advancements give patients hope and move the quest for disease-modifying medications closer to more potent treatments that target the intricate pathways underlying Alzheimer's disease.

Covalent inhibitor drugs or targeted covalent inhibitors (TCIs) are a type of drug category that interact with their target by covalent bond formation. They represent a unique category having desired properties such as high potency and longer duration of action, making them an attractive opportunity to pursue by researchers in drug discovery. In history, covalent inhibitors were often discovered serendipitously (e.g. aspirin and penicillin). However, modern times have witnessed numerous cases of rational design of these drugs, which has caused their rise to occupy a significant fraction of marketed drugs (over 30%). Here, we have given an overview of the discovery process of covalent inhibitors, including target identification/validation, warhead selection and optimization, linker design and conjugation and the role of computational tools in covalent inhibitors. To conclude, the challenges in this field and future directions to foresee are discussed. The objective of this article is to provide a summary of the general development process of covalent inhibitors as well as prospects or research gaps awaiting to be solved to overcome the challenges that hinder the discovery of covalent drugs.

Heterocyclic scaffolds, particularly indole and thiazole compounds, are revolutionizing the treatment of lung diseases due to their structural diversity and broad therapeutic potential. Their ability to target multiple biological pathways positions them as powerful tools for developing innovative treatments for lung disorders, particularly lung cancer. This review systematically explores recent advances in the synthesis and biological evaluation of indole and thiazole derivatives, emphasizing detailed synthetic strategies and the identification of the most potent molecules reported in the studies referenced within this manuscript for their relevance to lung diseases, particularly lung cancer. The SAR studies elucidate the role of molecular features and key functional groups in enhancing the potency, selectivity, and therapeutic efficacy of synthetic indole and thiazole derivatives. Given that lung cancer remains the leading cause of cancer-related deaths worldwide, the findings highlight the urgent need for developing innovative and effective anti-lung cancer agents, with indole and thiazole scaffolds serving as promising therapeutic frameworks.