Letters in Drug Design & Discovery - Volume 16, Issue 5, 2019

Aims: The aim of this review is to survey the recent progress made in developing the nanoparticles as antifungal agents especially the nano-based formulations being exploited for the management of Candida infections. Discussion: In the last few decades, there has been many-fold increase in fungal infections including candidiasis due to the increased number of immunocompromised patients worldwide. The efficacy of availabl Read More

Aim: The present review aims to explore the development of novel antifungal agents, such as pharmacology, pharmacokinetics, spectrum of activity, safety, toxicity and other aspects that involve drug-drug interactions of the azole antifungal agents. Introduction: Fungal infections in critically ill and immune-compromised patients are increasing at alarming rates, caused mainly by Candida albicans an opportunistic fun Read More

Background: The emergence of fungal resistance to commercial drugs has been observed, and because of that, research with natural products have been performed with the aim of obtaining bioactive compounds. Objective: Evaluate the chemical composition and antifungal activity of the ethanolic extract of Costus cf. arabicus L leaves (EECAL) over strains of the genus Candida, as well as its inhibitory potential over yeast v Read More

Background: A series of novel substituted 2-mercaptoimidazoles was synthesised efficiently and in high yields using one-pot synthesis from m-hydroxyacetophenones. Methods: The structures of the newly synthesized compounds were established, their molecular activity was investigated against some bacteria and fungi were further validated using molecular docking study. Results: Reaction of o-hydroxyphenacylbromide ( Read More

Background: Hydrazones, one of the important classes of organic molecules, are pharmaceutical agents comprising –CO-NH-N=CH- group in the structure therefore and exhibiting significant biological activity. Methods: 5-Chloro-N’-[(substituted)methylidene] pyrazine-2-carbohydrazide (3a-g) and their Pd(II) complexes (4a-h) were synthesized and investigated in vitro anticancer activity on A549, Caco2 cancer and normal 3T3 fi Read More

Background: Cancer continues to pose a great problem and burden on society despite new treatment options. While surgery, radiotherapy, and chemotherapy have led to major improvements in patient prognosis, newer treatments are needed to more effectively manage this disease in its advanced stage. Epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase (RTK), which is catalytically active and under tigh Read More

Background: Cancer cells are described as an unregulated growth and spread of abnormal cells. Recently, cancer has become the most important major reason for deaths in the world. Methods: For anticancer activity, we have used the MTT method and determine the early/late apoptosis by flow cytometry. Results: The title compounds were procured by reacting 2-chloro-N-[4-(pyridin-4-yl)thiazol-2- yl]acetamide with some su Read More

Background: Chemotherapy is a routine approach in treatment of patients with cancer, while side effects of chemotherapeutic drugs are inevitable. To minimize side effects, specific targeting of neoplastic cells is a promising strategy in cancer therapy. Sodium arsenite is a metalloid toxin with anti-neoplastic properties, but low selectivity and carcinogenic activity have limited its clinical usage. Methods: Targeting of HER2-overex Read More

Background: Nepeta species is a rich source of phytochemicals with multiple pharmacological activity. The aim of the present study was to study the cytotoxicity and pro-apoptotic activity of Nepeta binaloudensis different extracts and essential oil on prostate (PC3 and DU-145) and breast cancer (MCF-7) cell lines. Methods: To explore that cytotoxicity and apoptosis inducing activity, resazurin assay, propidium iodide (PI) stai Read More

Background: B-Raf has become an important and exciting therapeutic cancer target. Methods: In the present work, molecular modeling protocols like molecular docking, MM/GBSA calculations, 3D-QSAR and binding site detection were performed on a dataset of 41 Type II inhibitors. Molecular docking was applied to explore the detailed binding process between the inhibitors and B-Raf kinase. Furthermore, the good linear relati Read More

Background: Middle East Respiratory Syndrome coronavirus (MERS CoV) is a newly emerged viral disease with a fatal outcome. Methods: During the search for new antiviral drugs, MERS CoV papain-like protease (Plpro) was identified as a possible target. In this work, MERS CoV Plpro was investigated by virtual screening, enzyme inhibition and molecular dynamics to find new inhibitors. After the virtual screening of a datas Read More

Background: The present paper focuses on the in vitro inhibition of some sedative drugs such as Midazolam, Propofol, Hipnodex, Ketamine, and Pental sodium on acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), and α-glycosidase (α-Gly) enzymes. Methods: These drugs were tested in diverse concentrations, which showed positive effects in vitro AChE, BChE, and α-Gly activities. Ki values were 20.14, 94.93, 636.78, 4 Read More

Background: Inhibition of the DNA repair enzyme, tyrosyl-DNA phosphodiesterase 1 (TDP1), may increase the efficacy of cancer drugs that cause damage to tumor cell DNA. Among the known TDP1 inhibitors, there are compounds containing moieties of natural substances, e.g., monoterpenoids. In this work, we synthesized several compounds containing aromatic/ heteroaromatic amines and monoterpenoid grou Read More