Letters in Drug Design & Discovery - Volume 20, Issue 11, 2023

ATP dependent MurC-F ligases are essential for the biosynthesis of peptidoglycan, an essential bacterial cell wall component that is required for bacterial cell survival. Last, in the series, MurF catalyzes the ATP-dependent addition of D-Ala-D-Ala dipeptide to UDP-N-acetylmuramyl-tripeptide to form the UDP-N-acetylmuramy-pentapeptide monomeric precursor of peptidoglycan. Owing to its critical essentiality in peptidoglycan bi Read More

The world needs a paradigm change from the current views on many plants to secure future food and nutrition. Many neglected and underutilized plants, specially medicinal and aromatic plants, are nutrient dense, appropriate in diversifying diets, provide enough vitamins and micronutrients for people, high resistant to diseases and pests, and can be adapted in many regions and of course with tremendous pharmaceutical be Read More

The review aims to summarize the major and dominant natural antioxidants and their resources from medicinal and herbal plants with antiviral, anti-inflammation and antimicrobial activities. For this review manuscript, online databases, including Web of Science, Scopus, PubMed, and Science Direct, were searched for papers published from 1960 to November, 2021. Search terms consisted of “medicinal plants”, “traditional Ira Read More

Background: Curcumin, a polyphenolic compound present in the turmeric plant (Curcuma longa) is well known for its anti-aging, anti-tumor, anti-inflammatory, anti-mutagenic and antioxidative properties due to which turmeric has been used as a medicinal plant from ages. Objective: Our current study aims at finding the most potent targets of curcumin displaying efficient binding by using various systems biology tools. Aro Read More

Background: A large scale experimental validation conducted at the National Center for Advancing Translational Sciences (NCATS/NIH, USA) confirmed the predictions of our 3D-SDAR model of hERG blockage and phospholipidosis induction. It was demonstrated that both hERG blockage and phospholipidosis induction are driven by a common three-center toxicophore composed of two aromatic rings and an amino group. Read More

Background: Lycopene, a natural antioxidant from carotenoids, is produced by plants and microorganisms. It has been investigated in many studies in relation with potential health effects. Objective: Due to the high lipid-solubility of lycopene, its skin penetration is challenged. Therefore, in the present study, lycopene was loaded into lipid nanoparticles to improve penetration and pharmacological properties. Methods: Solid lipid Read More

Background: Sustained release of synthetic polymeric microparticles has gained more attention as drug delivery carriers because of their properties such as good stability, low toxicity, dosing frequency, and simple and mild preparation method. The present work was envisaged to reduce the dosing frequency by preparing drug loaded biodegradable microspheres by the O/O emulsion solvent evaporation technique. Read More

Background: Inhibition of cholinesterase enzyme has been recognized as an important target in the symptomatic treatment of Alzheimer’s disease. Objective: In the current work, a series of new N-(4-(imidazo[1,2-a]pyridin-2-yl)phenyl)cinnamamide derivatives were synthesized and their inhibitory activities against acetyl cholinesterase, butrylcholinesterase, and Lipoxygenase were evaluated. Methods: The target compoun Read More

Background: Diabetes mellitus (DM) is a metabolic disorder in which blood sugar levels are elevated over a prolonged period of time. SGLT2 inhibitors have recently demonstrated positive effects on diabetes care by minimizing hyperglycemia through decreased glucosuria. Objective: The aim was to carry out molecular docking and ADMET studies of 1,2,4 triazole and 1,2,4 oxadiazole scaffolds as SGLT2 inhibitors. Methods: Read More

Background: Bronchopulmonary dysplasia (BPD) is a common chronic lung disease in the respiratory system of premature infants. Gm15886, as a lncRNA, is highly expressed in lung tissue of BPD newborn mice. Aims: This study aimed to clarify the roles of the Gm15886 gene in the pathogenesis of BPD mice by determining the expression of Gm15886 and Hipk1 in lung tissues. Methods: Sequence and localization of t Read More

Background: Argan oil is one of the products used for antidiabetic purposes in Morocco. Objective: This work aims to study the acute and subchronic effect treatment of the roasted (Roil) and unroasted (UnRoil) Argan oils on oral glucose tolerance test (OGTT) and body weight in normal and diabetic rats, evaluate the effect of these oils on glucose absorption by the diaphragm and determine total polyphenol, flavonoids, t Read More

Background: Diabetic neuropathic pain seriously affects the quality of a patient’s life. To predict molecular mechanism based on network pharmacology and verify the interaction between the active ingredient of Astragalus membranaceus and Panax notoginseng coupled-herbs (AP) and target genes related to Diabetic neuropathic pain (DNP) molecular docking assay was performed. AP and their target genes related Read More

Background: The COVID-19 outbreak is a serious concern and has caused a great loss to the global economy. Therefore, COVID-19 has become an urgent public health problem. Although new vaccines and small molecule drugs are now available, these prevention and treatment methods cannot completely control the epidemic due to the constant mutation of SARS-CoV-2. Targeting 3CLpro/RdRp is expected to develop drugs that Read More

Background: Many contagious diseases have been caused by a variety of nontuberculous mycobacteria, opportunistic pathogens that can cause disseminated or localized diseases, particularly pulmonary, skin, and soft tissue infections. Objective: In this study fifty-five substituted 4-N-alkylated-2-trifluoromethylquinolines were evaluated against five species of nontuberculous mycobacteria: Mycobacterium fortuitum, M Read More

Background: Heterocyclic sulfone-bearing small molecules are particularly important objects in medicinal chemistry. Structure-diversified pyridinyloxy-substituted imidazo[2,1-b][1,3]thiazines are characterized by satisfactory drug-like parameters and possess significant anti-inflammatory effects in in vivo studies. Objective: Oxidation of a series of 6-(2-pyridinyloxy) imidazo[2,1-b][1,3]thiazines under the action Read More