Mini Reviews in Medicinal Chemistry - Volume 7, Issue 5, 2007

To develop the newer pharmaceuticals and to spur the strong growth, being a general property of ‘handedness’, chirality plays a major role. The Easson-Stedman principle shows the differences in the biological activity between enantiomers resulted from selective reactivity of one enantiomer with its receptor. It helps to improve the pharmacokinetic properties and to remove undesirable side effects by virtue of the unique activ Read More

Basic part of the current standard treatment of organophosphate (OP) agent poisoning is administration of cholinesterase reactivators. It includes different types of oximes with a similar basic structure differing by the number of pyridinium rings and by the position of the oxime group in the pyridinium ring. Oximes hydrolytically cleave the organophosphates from acetylcholinesterase (AChE), restoring enzymatic function. Thi Read More

Objective: To review the main pharmacological properties and clinical applications of the drugs used in the medical therapy of Cushing's syndrome. Data Sources: Search for articles were performed in the following dababases: MEDLINE, EMBASE, Cochrane Database of systematic Reviews and The Cochrane Central Register of Controlled Trials (CENTRAL). Search terms included Cushing's syndrome and drug therapy. Data Synth Read More

The development of prodrugs that are enzymatically activated into anticancer agents is a promising perspective in cancer therapy. Many nitrogen-containing quinoid heterocycles have been reported to show antitumor effect. The principal interest in these compounds lies on their potential to produce tumor-selective toxicity. Selectivity occurs by difference in oxygen tension between normal and tumor tissue and by levels of th Read More

The application of 2H solid-state NMR in determining structure activity relationships and mechanism of action of membrane active peptides is discussed. The enhancement of the disruption of anionic lipids in the membrane by new lead compounds is shown to be a key determinant of both DNA vector and antimicrobial activity.

In Silico predictive ADME/Tox screening of compounds is one of the hottest areas in drug discovery. To provide predictions of compound drug-like characteristics early in modern drug-discovery decision making, computational technologies have been widely accepted to develop rapid high throughput in silico ADMET analysis. It is widely perceived that the early screening of chemical entities can significantly reduce the expe Read More

Recent evidence has suggested improved outcomes following incorporation of intraperitoneal chemotherapy administration with intravenous systemic chemotherapy as first-line treatment of small volume residual epithelial ovarian cancer. This review focuses on the mechanism of actions of the chemotherapeutic drugs and reviews the possible reasons for the superior outcomes of intraperitoneal chemotherapy.

Over the past decade, an epidemic of obesity has developed throughout the Western World. In recent years, significant interest has focused on the role of the AMP-activated protein kinase (AMPK) as a potential therapeutic target for the treatment of obesity and type 2 diabetes and is such the focus of this review. Specifically, the potential role of AMPK in skeletal muscle metabolism as it relates to the insulin sensitizing effects of Read More

An increasing body of evidence suggests that different genetic factors, such as angiotensin-converting enzyme (ACE) I/D , angiotensin II type-1 receptor (AT1R) A1166C, methylenetetrahydrofolate reductase (MTHFR) C677T and ENOS G894T variants are associated with an endothelial dysfunction (ED). EDs are relatively new phenomena that are presumed to contribute to vasoregulatory malfunctions at the small-vessel Read More

Preventive doping research includes the development of methods for the detection of new or emerging drugs to be implemented in routine screening analysis. Candidates with great potential for misuse in elite sports include selective androgen receptor modulators, growth hormone secretagogues, hypoxia-inducible factor stabilizers and erythropoietin mimetics.

Asthma is a chronic respiratory condition affecting many adults and children. An association between asthma and raised gaseous nitric oxide in the exhaled breath was first reported in 1993. In the absence of an objective test for diagnosing and monitoring asthma, a vigorous research effort has subsequently sought to determine the nature of the relationship between exhaled nitric oxide (ENO) and asthma and to determine the cl Read More

Natural vitamin E comprises 8 different analogues, the α-, β-, γ-, and δ-tocopherols and the α-, β-, γ-, and α-tocotrienols. However, only α-tocopherol is selectively enriched by the liver; the other vitamin E analogues and also excess α-tocopherol are converted to several metabolites and eliminated. Recently, a novel phosphorylated form of tocopherol, α-tocopheryl phosphate, was shown to occur naturally in animal a Read More