Medicinal Chemistry - Volume 13, Issue 1, 2017

Background: Microbes attach to surfaces and form biofilms where they are difficult to eradicate. Here they are embedded in a complex matrix of polymers and are much less sensitive against antibiotics or the immune system. Objective: This is a growing problem, especially for implants; hence, novel approaches are urgently needed to control biofilm infections. Methods: Many of these approaches interfere with the comm Read More

Assessment of toxicity is an important component of the drug discovery process. Cellbased assays are a popular choice for assessing cytotoxicity. However, these assays are complex because of the wide variety of formats and methods that are available, lack of standardization, confusing terminology and the inherent variability of biological systems and measurement. This review is intended as a guide on how to take these Read More

Background: Group A streptococcus (GAS) is an exclusively human pathogenic bacteria. A delay in treatment of GAS infection often lead to severe diseases such as rheumatic heart disease which attributes to hundreds of thousands deaths annually. For the past few decades, the quest for a commercial GAS vaccine has been futile. Currently one of the most investigated strategies to develop vaccine against GAS includes the Read More

Background: Glioblastoma multiforme (GBM) is often associated with a poor survival prognostic for patients. The main reason seems to be the acquired or inherent resistance to the chemotherapeutic agent used to treat the tumor, temozolomide (TMZ). To this day, the most recognized pathway of resistance is the DNA Direct Repair pathway by the means of the protein O6- methylguanine DNA-methyltransferase (MGMT) Read More

Background: Tyrosine kinases (TK) are enzymes that catalyze the phosphorylation of tyrosine residues on proteins by the transfer of phosphate moiety of ATP. TK are key regulators of various cell functions, such as cellular growth, proliferation, migration, differentiation, and apoptosis. Src mutations and/or overexpression has been correlated with tumor growth, metastasis, and angiogenesis [4,5]. Thus, the design and the d Read More

Background: According to a review of recent literature, no previous studies have reported the dose-dependent selective inhibition of the antiproliferative activity using colony and sphere formation assays and immunoblotting in human hepatoma cells in response to doxorubicin and mitoxantrone structural analogs such as AM3. Objective: We evaluated the anticancer activity of mitoxantrone (MIT) structural analogs 1 Read More

Background: Previously, glycopeptides antibiotics such as vancomycin, ramoplanin and an antifungal antibiotic nystatin have been studied for their diagnostic and therapeutic potential. Objective: To further explore the diagnostic and chemotherapeutic potential of other antibiotics we have now employed daptomycin, a lipopetide antibiotic and bacitracin, a polypeptide antibiotic in uptake and vitality tests on human cell lines. Met Read More

Background: Antagonists to the H3 receptor are considered to be potential drugs for the treatment of Alzheimer’s disease, attention deficit-hyperactive disorder, memory and learning deficits, and epilepsy. The initial development of potent H3 receptor antagonists focused on extensive modification of the natural ligand histamine. However, it has appeared that imidazole-containing ligands are associated with inhibition of Read More

Background: The field of coordination chemistry has registered a phenomenal growth during the last few decades. It is well known that precious metals have been used for medicinal purposes for at least 3500 years. At that time, precious metals were believed to benefit health because of their rarity, but research has now well established the link between medicinal properties of inorganic drugs and specific biological prope Read More

Background: The antimicrobial activity of a synthesized series of 28 2-thioxobenzo[ g]quinazolin-4(3H)-one derivatives was evaluated in vitro against five Gram-positive bacteria, including Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus pyogenes. The antibacterial activity was extended to include five Gramnegative bacteria: Pseudomonas aeruginosa, Esch Read More

Background: Coumarin derivatives as dihydrocoumarins have been reported to have multiple biological activities, such as antioxidant and anti-inflammatory properties. Apocynin (APO), which is a substituted-methoxy-catechol, is the most commonly used inhibitor of the multienzymatic complex NADPH-oxidase. Objective: To increase the potency of APO as an NADPH oxidase inhibitor and its antioxidant and anti-inflamma Read More