Medicinal Chemistry - Volume 15, Issue 8, 2019

Background: Due to emerging resistances against antibiotics there is a strong need to find novel antibacterial agents with a novel structure to prevent early resistance developments. Objective: Bisindole compounds with antibacterial activities which formally result from the reaction of an aldehyde with indole motivated to investigate the reaction of a dialdehyde and indole to give novel structures with potential antibacterial Read More

Background: Rhodanine is known for its potential and important role in the medicinal chemistry since its derivatives exhibit a wide range of pharmacological activities such as antibacterial, antifungal, antidiabetic, antitubercular, anti-HIV, antiparasitic, antioxidant, anticancer, antiproliferative and anthelmintic agents. Objectives: Since N-substituted rhodanine synthons are rarely commercially available, it is desi Read More

Background: Ischemic heart disease, cerebrovascular accident, and venous thromboembolism have the presence of a thrombotic event in common and represent the most common causes of death within the population. Objective: Since Schiff base copper(II) complexes are able to interact with polyphosphates (PolyP), a procoagulant and potentially prothrombotic platelet agent, we investigated the antiplatelet aggre Read More

Background: Platelet aggregation plays a pathogenic role in the development of arterial thrombi, which are responsible for common diseases caused by thrombotic arterial occlusion, such as myocardial infarction and stroke. Much efforts are directed toward developing platelet aggregation inhibitors that act through several mechanisms: The main antiplatelet family of COXinhibitors, phosphodiesterase inhibitors, and thrombi Read More

Background: Marine sponges and tunicates have been a wealthy source of cytotoxic compounds such as indole alkaloids. Most of the indole alkaloids show in vitro cytotoxic and antineoplastic activities against a wide range of cancer cell lines. Objective: Three series of bioisosteres of marine indole alkaloids (meridianins) were synthesized and the compounds were tested for their in vitro anti-proliferative activity agains Read More

Background: Previously, we have identified 3,3′–carbonyl–bis(chromones) (1a-h, 5e) and 3–(5–(benzylideneamino)thiozol–3–yl)–2H–chromen–2–ones (7a-j) as potent inhibitors of tissue non-specific alkaline phosphatase (TNAP). The present study was designed to investigate the cytotoxic and pro-apoptotic effect of the said derivatives. Methods: The anti-proliferative effect of the derivatives was investigated in three cancer cell line Read More

Background: Cancer is a far-reaching and lethal but curable disease. Researchers have investigated numerous anticancer agents with only a few commercially available effective drugs which are very costly. Objective: Herein, we report the synthesis , characterization and anti cancer assays of a series of novel dithiocarbamates derivatives. Methods: All compounds were synthesized from different secondary amines and substitut Read More

Background: Hydrazine-hydrazones represent a group of bioactive compounds that display antibacterial, anti-inflammatory, antiviral or anticancer activities. Objective: In this study, we designed new derivative compounds from groups of hydrazones. Methods: The group of new derivatives was evaluated by the viability assay in human cancer and normal cells. Results: The dimethylpyridine hydrazones showed potent inhibition of Read More

Background: Pyrroles and fused pyrroles are of great interest as biologically active compounds, among these activities; antidepressant activity is of special concern. Objective: Synthesis of a series of pyrrolopyrazoles and their pyrimidine derivatives and their characterization using spectral data to be monitored for antidepressant activity using behavioral techniques. Methods: A control group was administered the vehicle i.p., posi Read More

Background: Antioxidant, anti-inflammatory, antiviral and antitumoral activities among others are essential characteristics in the development of novel therapeutic compounds. Acid hydrazides can form complexation with certain metal ions that positively enhance these biological characteristics. Objective: Five new complexes of uranium with hydrazide ligands were synthesized at room temperature. Methods: The Read More