Letters in Drug Design & Discovery - Volume 14, Issue 12, 2017

Background: Aminopeptidase N also known as APN/CD13 is a zinc-dependent type II membrane-bond ectopeptidase that is overexpressed on cancer cells. APN/CD13 is considered as an attractive target for anti-cancer drug design due to key roles in tumor invasion, angiogenesis and metastasis. Therefore, study of quantitative relationships between activity and structures of APN/CD13 inhibitors can provide useful infor Read More

Background: Imidazolones as well as Schiff base are extensively used as building blocks for the synthesis of various pharmaceutically active agents. The use of synthetic antioxidant for use in the diet and therapy demands a great deal of research attention for synthetic antioxidants. It was observed that the π-excessive ring systems are responsible for antioxidant activity of the compounds. Objective: The primary objective o Read More

Background: Dolutegravir sodium is a HIV-1 integrase strand transfer inhibitor (INSTI) and in combination with other anti-retroviral agents, is recommended for the treatment of HIV-1 infection. Moreover, it is a second generation HIV integrase inhibitor designed to deliver potent antiviral activity. Originally, collaboration between Shionogi and Glaxo Smith Kline (GSK) led to dolutegravir sodium which is marketed under the t Read More

Background: Hepatitis C Virus (HCV) infection is one of the causes for liver cirrhosis and hepatocellular carcinoma leading to liver failure. An estimated 2-3% of the world population is chronically infected with HCV. HCV is a positive single stranded RNA virus encoding for a single polypeptide, which cleaves into structural and non-structural proteins. The non-structural (NS) proteins play critical roles in viral replicati Read More

Background: Thiazolopyrimidines possessed their structural diversity and various biological activity. Up to date, thiazolopyrimidines derivatives have widespread applications in pharmaceutical fields. In this article, a series of thiazolopyrimidine derivatives were designed based on the lead compound structure in our previous studies. Methods: All the target compounds were synthesized with the coupling reaction, Biginelli re Read More

Background: Elevated levels of serum LDL and total cholesterol are considered important risk factors for the development of atherosclerosis. Cholesteryl ester transfer protein inhibition raises HDL levels and reduces atherosclerotic lesions. Objective: Consequently, there is a great interest in developing new CETP inhibitors. Methods: Herein, synthesis of four chlorobenzyl benzamides 8a-d that aim at CETP inhibition was perf Read More

Introduction: Currently, there are a significant number of drugs getting approval with poor biopharmaceutical characteristics, as low solubility and bioavailability. These facts lead to a decrease of the therapeutic effect and to an increase of the drug dosage. In this regard, there is a need to overcome this problem, in which the development of new drug delivery systems (DDS) arises as a promising strategy, since these syste Read More

Background: Pyrimidine-based drugs stimulate tissue regeneration and immunity, two components that need to be improved in a number of respiratory diseases of different etiology (e.g. influenza and asthma). In the present study we investigated relationships between the character of substitutions in the uracil structure and the impact of the respective uracil derivatives on the immortalized lung cells. Methods: The level Read More

Background: Brominated 8-hydroxy, 8-methoxy, 8-amino quinolines 5, 6, 8, 9 and novel cyano 8-hydroxyquinolines 11, 12 were evaluated in vitro for their anticancer effects on various cell lines. 5,7-Dibromo- 5, 7-bromo- 6, 7-cyano- 11 and 5,7-dicyano-12 8-hydroxyquinolines were shown to have strong antiproliferative activity against various tumor cell lines, including C6 (rat brain tumor), HeLa (human cervix carcinoma), an Read More

Background: Curcumins were reported to possess anti-inflammatory and antiangiogenic. Furthermore, Curcumin is a very potent free radical scavenger than vitamin E. Moreover, cyanoacetamides were reported to possess, antimicrobial antifungal, insulin releasing, antiinflammatory and antitumor. Thus the present study focuses on the synthesis of some novel structure hybrids incorporating either curcumin or cyanoacet Read More

Background: Salmonella typhimurium is a pathogen, causing a threat to human health worldwide. The severity in treatment raises as the pathogen develops resistance against wellestablished drugs. To combat these multidrug-resistant pathogens, novel target and antimicrobial agents are needed. The literature supports the potency of L-asparaginase as a novel target as it provides survival benefit to the pathogen. The plan Read More

Background: High attrition rate in late drug discovery and development stages leads to financial loss to industries and Governments. Despite the global prevalence of HIV infection and lack of promising treatment for AIDS patients, there are only a few drugs approved for the management of infected patients. There is an urgent need to discover newer anti-HIV drugs with novel mechanism of action and with efforts to reduce a Read More

Background: Many studies support the involvement of the substance P (SP)/neurokinin-1 receptor (NK-1R) system in cancer. SP, after binding to the NK-1R, regulates cancer cell proliferation, induces cell migration and invasion, which are steps of the metastatic process, exerts an antiapoptotic effect, and triggers endothelial cell proliferation necessary for neoangiogenesis. Lung cancer is the first cause of cancer-related deaths i Read More