Medicinal Chemistry - Volume 14, Issue 5, 2018

Background: Purinergic signaling accounts for a complex network of receptors and extracellular enzymes responsible for the generation, recognition and degradation of extracellular ATP and adenosine. The main components of this system include P2X, P2Y and Adenosine Receptors, ectonucleotidases CD39 and CD73 and Adenosine Deaminase. The purinergic network recently emerged as a central player in several p Read More

Background: HSP90 is necessary for the conformational maturation of proteins, proteins disaggregation, folding newly synthesized peptides and the refolding of denatured proteins. The inhibition of HSP90 leads to proteasomal degradations of client proteins that finally kill cancer cells. Methods: In this research, molecular docking and comparative molecular field analysis (CoMFA) were used to investigate the interactions of tetrah Read More

Background: In the past few decades, design, synthesis, and characterization of novel heterocyclic compounds with auspicious biological profile received the considerable attention of the scientific community. Among them, the small and simple organic molecular backbone like triazole moiety have a broad spectrum of applications in the medicinal as well as diagnostic areas. Objective: The objective of present study was synthe Read More

Background: Candida albicans belongs to the most common fungal pathogens in humans, but recently an increased proliferation of strains called non-albicans Candida has been reported. Species belonging to this group are often characterised by a reduced susceptibility to antifungal agents. Objective: In view of the emergence of non-albicans Candida and their resistance to available antifungals, an attempt has been made to Read More

Background: Amidrazones have been reported to have significant anti-tumor properties against several cancer cell lines. Objectives: The current project aims to profile the structure-anticancer activity relationship of phenyl-amidrazons. Methods: Fifteen phenyl-amidrazone-piperazine derivatives were prepared and tested against four cancer cell lines (leukemia, prostate, breast and colon cancers). Results: Six compoun Read More

Background: Discovery of novel agents with anticoagulant and antioxidant activity is very important to treat cerebrovascular disease. Lead compound LR3d discovered in our laboratory exhibited stronger anticoagulant ability and good antioxidant activity, compared with scutellarein (2), which is the major in vivo active metabolite of the natural product scutellarin (1). Objective: Design and synthesis novel scutellarein deriv Read More

Background: The natural products containing a common 3,4-diarylpyrrole skeleton have attracted considerable attention due to their unique structures and multiplex biological activities. In our previous study, lycogarubin C was synthesized and showed cytotoxicity against MDAMB- 231, A549, PC3 and HeLa cell lines and topoisomerase II inhibitory activities. Objective: We present the design, synthesis and antitumor studie Read More

Background: Directed Enzyme Prodrugs Therapy (DEPT) as an alternative method against conventional cancer treatments, in which the non-toxic prodrugs is converted to highly cytotoxic derivative, has attracted an ample attention in recent years for cancer therapy studies. Objective: The metabolite profile, cell cytotoxicity and molecular modeling interactions of a series of nitro benzamides with Ssap-NtrB were investigate Read More

Background: Obesity is one of the major health problems with inherent risk of type 2 diabetes, hypertension, CVDs, etc. Adipogenesis is a major contributor in the process of obesity. Inhibition of adipocytes differentiation is one of the key approaches to treat obesity. Objective: To discover the new inhibitors of adipogenesis as the treatment for obesity. Method: We describe here, the synthesis, and anti-adipogenic activity of thio Read More

Background: Anthranilic acid derivatives are important pharmacophores in drug discovery. Several of them are currently being used, such as mefenamic acid and meclofenamates, possess analgesic, anti-inflammatory and antipyretic activities. Some anthranilic acid-based scaffolds have also been reported for the management of metabolic disorders. Objectives: The aim of the current study was to investigate the antiglyc Read More

Background: Xanthine oxidase is an important enzyme which catalyzes the production of uric acid and superoxide anion from xanthine. The over-production of these products leads to different disease conditions. For instance, uric acid is responsible for hyperuricemia, gout, and arthritis, while superoxide anion contributes to the oxidative stress, and related diseases. Hence XO is an important pharmacological target for the trea Read More

Background: Pyrazolones have identified as significant antioxidant agents and many marketed and clinically prescribed NSAIDs have pyrazolone ring as main scaffold. Method: Keeping in consideration the antioxidant potential of pyrazolone scaffold, new bispyrazolones 3-30 were synthesized by a green and enviroment friendly reaction route, in which two equivalents of 1-(4-chlorophenyl)-3-methyl-1H-pyrazol-5-ol were treate Read More