Medicinal Chemistry - Online First

Introduction Histamine Type I Receptor Antagonists (H1 blockers) are widely used to mitigate histamine-induced inflammation, particularly in allergic reactions. Histamine, a biogenic amine found in endothelial cells, vascular smooth muscle, bronchial smooth muscle, and the hypothalamus, is a key player in these responses. H1 blockers are essential in cough syrups and flu medications and are divided into two Read More

Introduction Heterocyclic derivatives, particularly those containing heteroatoms such as oxygen and nitrogen, represent a significant portion of currently marketed drugs. Among these, the aromatic heterocycle 1,3,4-oxadiazole, characterized by an N=C=O-linkage, stands out due to its remarkable biological activities. These activities include anti-inflammatory, anti-cancer, antioxidant, anti-tubercular, antiviral, anti-diabet Read More

The escalating prevalence of lifestyle and microbial diseases poses a significant threat to human well-being, necessitating the discovery and development of novel drugs with distinct modes of action. Addressing this challenge involves employing innovative strategies, and one current approach involves utilizing heterocyclic compounds to synthesize hybrid molecules. These hybrids have resulted from the fusion of two o Read More

BackgroundWe continue to struggle with the prevention and treatment of the influenza virus. The 2009 swine flu pandemic, caused by the H1N1 strain of influenza A, resulted in numerous fatalities. The threat of influenza remains a significant concern for global health, and the development of novel drugs targeting these viruses is highly desirable.ObjectiveThe objective of this study is to explore the inhibitory potential of terpen Read More

Pyrazoline is a 5-membered ring that has two adjacent nitrogen. It has gained advanced attention from medical and organic chemists due to very low cytotoxic activities. It is applicable and more applied in research fields and has various pharmacological activities, including cardiovascular, anti-tumor, and anti-cancer properties. In this review, the main objective is to study the pharmacological aspects of pyrazoline and its deriva Read More

Introduction The marine habitat is a plentiful source of diverse, active compounds that are extensively utilised for their medicinal properties. Pharmaceutical trends have currently changed towards utilising a diverse range of goods derived from the marine environment. Method This study aimed to examine the inhibitory effects of bioactive chemicals derived from marine algae and bacteria. The identification of these comp Read More

Indazole, a heterocyclic molecule, has emerged as a useful scaffold in synthetic and medicinal chemistry due to its broad biological activity and ease of synthesis. This article thoroughly analyzes unique synthetic methods used to diversify indazole derivatives, such as metal-catalyzed reactions, ecologically friendly approaches, and novel multicomponent reactions. These advances have increased the efficiency and sel Read More

Introduction Breast cancer remains a formidable health concern for women, necessitating the development of potent anticancer agents with improved safety profiles. Dihydropyrimidinones (DHPM), pyrazole, and benzofuran scaffolds have emerged as promising targets due to their diverse pharmacological profiles. In this study, we employed a scaffold hopping approach to design a novel DHPM-Pyrazole-Benzofuran core. A s Read More

The complex interaction between carboxylic acids and molecular signaling pathways, particularly the nuclear factor erythroid 2-related factor 2 (NRF2) pathway, is of growing interest in medicinal chemistry due to its potential therapeutic benefits. Carboxylic acids, which are widely distributed in nature, are versatile regulators of cellular responses due to their ability to interact with multiple signaling pathways, especially those i Read More

The 2-isoxazoline scaffold has emerged as a key structure in medicinal chemistry, with great therapeutic potential for a wide range of biological targets. This review investigates the medicinal value of the 2-isoxazoline scaffold, emphasizing its adaptability and usefulness in the development of new medications. Isoxazoline has a wide range of biological actions, including antibacterial, anti-inflammatory, anticancer, and anti-para Read More

Background Over the past ten years, a remarkable number of changes have occurred in the field of cancer drug research. Most anticancer drugs from the first generation work by breaking down DNA, preventing its production, interfering with cell division processes, or attaching to microtubules. The potential use of tryptanthrin as well as its analogues is well documented for anticancer properties. Objective To design Read More

Aims The aim is to halt the progression of liver cancer [Hepatocellular carcinoma] by suppressing the VEGF-R1 receptor using Myricetin and its de novo-designed analogues. Background VEGF/VEGFR autocrine signalling promotes the growth, progression, and metastasis of Hepatocellular carcinoma, making the development of molecularly targeted therapies highly feasible. Invasive and metastatic behaviours in various ca Read More