Mini Reviews in Medicinal Chemistry - Volume 12, Issue 10, 2012

This special issue of the journal of MRMC is dedicated to Dr. Atta-ur-Rahman on the occasion of his 70th birthday and in recognition of his many outstanding contributions to Organic Chemistry. Prof. Rahman's honors include: the first scientist from the Muslim world to have won the prestigious UNESCO Science Prize (1999) in the 35 year old history of the Prize; elected as Fellow of Royal Society (London) in July 2006; conferred h Read More

Parkinson's disease (PD) is one of the most common neurodegenerative disorders. The role of monoamine oxidase (MAO) inhibitors has expanded in the PD treatment. The present review will summarize the current structureactivity relationship information available on MAOs inhibitors of unrelated families of compounds of oxygen heterocyclic type based on coumarin, chromone and chalcone scaffolds. As the current hitti Read More

The adjustment of multiple criteria in hit-to-lead identification and lead optimization is a major advance in drug discovery. Thus, the development of approaches able to handle additional criteria for the early simultaneous treatment of the most important properties determining the pharmaceutical profile of a drug candidate is an emergent issue in this area. In this paper, we review a desirability-based multi-objective Read More

This article reviews multi-criteria QSAR applications on Acetylcholinesterase inhibitors as palliative drugs for Alzheimer's Disease, published in the period 2001-2011. It includes QSAR models for different series of compounds, comparative studies, and advances in methodologies. This period is marked by a shift in focus from palliative treatment to pathogenesis. However, we believe that research into palliative treatment should Read More

With the significant increase of life expectancy of populations in societies today, the importance of the discovery of drugs associated with neurodegenerative diseases has emerged. Therefore, neurodegenerative diseases are an important topic in Medicinal Chemistry. Although drug discovery is considered a complex and slow process, new approaches and methods have been developed with the intention of finding n Read More

CNS drug development is characterized by an especially high attrition rate, despite clear unmet medical needs in the field of neuro-pharmacology and significant investment in R&D of novel CNS drug treatments. Here, we overview the issues underlying the intrinsic difficulty of CNS drugs development, including obstacles of pharmacokinetic nature and lack of predictivity of preclinical tests. We highlight current efforts to o Read More

The matrix protein 2 of the influenza A virus (M2 or AM2) is one of the important components of the viral membrane. This protein can form a proton channel in the viral envelope. Owing to its ability to regulate the surrounding pH in endosome, this protein is an attractive target for drug design against influenza A virus. In this minireview, we summarized the current progresses in computational approaches for studying th Read More

De-novo drug design (DND) is a complex procedure, requiring the satisfaction of many pharmaceutically important objectives. Several computational methodologies employing various optimization approaches have been developed to search for satisfactory solutions to this multi-objective problem varying from composite methods, which transform the problem to a single objective one to Pareto methods searchin Read More

Cancer cells are able to elaborate enzymatic mechanisms allowing tumors to resist or escape imune rejection. Among the enzymes involved, indoleamine 2,3-dioxygenase (IDO), an intracellular enzyme that initiates the first and rate-limiting step of tryptophan breakdown along the kynurenine pathway, has emerged as a promising molecular target for the development of new immunotherapeutic anticancer agents. Read More

Thrombophilias are defined as a predisposition to thrombosis due to hematological changes which induce blood hypercoagulability; they can be inherited or acquired. They are individually characterized by a large phenotypic variability, even when they occur within the same family. Hereditary thrombophilias are, in most cases, due to changes related to physiological coagulation inhibitors or mutations in the genes of coagulatio Read More

Drug development in the recent times often relies on use of natural and synthetic drugs that are promising candidates as therapeutic agents for prevention of diseases and disorders. They possess different chemical structures with wide range of therapeutic activities. Many natural and synthetic drugs act as antioxidant agents in various metabolic processes. Increasing epidemiological, clinical and experimental studies h Read More

Epilepsy is a chronic disorder of abnormal electrical activity in the brain characterized by recurrent unprovoked seizures. Currently used pharmaceutical agents do not treat the underlying disease process, and a significant proportion of epileptic patients are refractory to current therapies. Therefore there is a strong need for additional therapeutic agents, especially those that address the underlying disease proce Read More

Cytochrome P450 (CYP) inhibition and induction are the key mechanisms in drug-drug interactions which should be avoided in clinic for the uncertain influence on the efficacy and safety of drug co-administration. The CYPmediated drug-drug interactions urgently need to be predicted by in vitro models before animal and clinical trials, while the primary hepatocytes may represent the most appropriate experimental syste Read More