Letters in Drug Design & Discovery - Volume 21, Issue 8, 2024

Introduction and Objective: The identification of a bioactive template (or lead) is one of the important features of modern drug discovery. Natural products, synthetic and biotechnological sources, serve as important templates for the development of novel bioactive molecules. Quinazoline is one of the heterocyclic templates present in many natural and synthetic drugs and exhibits various biological activities, including antican Read More

Background: Rearranged during transfection (RET) is a receptor tyrosine kinase and a bona fide oncogene that drives various cancers. Oncogenic RET induces abnormal activation of RET kinase, causing tumorigenesis. RET can be abnormally activated through RET point mutations and RET fusions. Although RET kinase has been discovered in tumors more than 30 years ago, patients with RET-altered tumors gain limited bene Read More

Background: Drug delivery across human nails is termed a transungual drug delivery system. It is recommended for the amelioration of nail disorders and infectious nail diseases like onychomycosis. Thereby, vivid anti-fungal regimens have been prescribed in the form of different types of formulations, including nail lacquers, nail film, nail paint, and other types for treating onychomycosis. Methods: All the formulations curr Read More

Background: Herbal medicines have been extensively used to treat diseases since the prehistoric era, but written records date back more than 5,000 years only. All civilizations developed their knowledge of herbal medicines in a well-ordered system, such as Ayurveda, Unani, Traditional Chinese Medicine, etc. The interest in traditional medicine declined after the discovery of modern medicine. However, in the 21st centur Read More

Background & Objective: Christopher A. Lipinski, in 1997, formulated Lipinski’s rule of five for drug-likeness prediction of potent molecules. It states that molecular weight (less than 500 Daltons), octanol/water partition coefficient (not exceeding more than 5), hydrogen bond acceptor (no more than 10), and hydrogen bond donor (no more than 5) are important for good oral bioavailability. Many drugs among various important cl Read More

Background: The United States Food and Drug Administration (FDA) has authorized paclitaxel for the treatment of numerous types of cancer, including breast, lung, ovarian, and Kaposi's sarcoma. It possesses all the characteristics of BCS class IV medications, including low bioavailability, low water solubility, poor permeability, unpredictable and poor absorption, and inter- and intrasubject variability. Objective: The purpose Read More

Wine production is the result of the interaction between various strains and grapes, and its good quality is also affected by many factors. Aureobasidium, Cladosporium, Candida, Filobasidium, Hanseniaspora, Hannaella, Saccharomyces, Wickerhamomyce, Alternaria, Starmerella, Acetobacter, Papiliotrema, Bradyrhizobium, Leuconostoclia, Gluconobacter, Comamonas, and Massilia, are significantly correlated with Read More

Background: Intra-abdominal adhesions are severe complications which occur after abdominal surgery. Currently, no specific anti-adhesive medications can completely prevent Intra-abdominal adhesion formation. Therefore, recent studies are exploring new approaches for preventing this complication. Anti-inflammatory properties of Trigonella Foenum-graecum L. (Fenugreek) have been reported in various studies. In t Read More

Purpose: The use of common carriers like talc for topical drug delivery leads to diminished efficacy as a result of poor aqueous solubility and low dissolution rate. The objective of this study was to improve the efficiency of fluconazole topical dosage form using MCM-41 as a carrier material. The aim was to load fluconazole in carriers like MCM-41 as well as ß-Cyclodextrin and to compare the prepared powder formulation with Read More

Background: Yellow fever (YF) is a mosquito-borne flaviviral hemorrhagic fever (VHF) that causes severe hepatitis, renal failure, bleeding, and quick terminal events such as shock and multi-organ failure. There are currently no particular anti-viral medications for the management of the YF virus (YFV). Despite the availability of a commercial YFV vaccination, there are roughly 30,000 fatalities globally each year, with instances risi Read More

Background: The monoamine oxidase (MAO) enzymes are important drug targets. Inhibitors of MAO-A and MAO-B have been used to treat the symptoms of depression and Parkinson’s disease. Methods: A series of seventeen pyridazinone-substituted benzenesulfonamides was synthesized and evaluated as potential inhibitors of human MAO-A and MAO-B. This study is a continuation of our interest in the pharmacological acti Read More