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Several New Classes (several + new_class)
Selected AbstractsSynthesis, in-vitro Microbial and Cytotoxic Studies of New Benzimidazole DerivativesARCHIV DER PHARMAZIE, Issue 7 2009Reddy S. Harisha Abstract Several new classes of benzimidazole derivatives were synthesized and evaluated for in-vitro antimicrobial and cytotoxic activities. The results showed that all synthesized compounds exhibited moderate antimicrobial activity, and compounds 2, 4, and 13 displayed cytotoxic activity (as LD50) at the concentration 1×10,3 M against Artemia salina. [source] Thiazolidinedione derivatives in diabetes and cardiovascular disease: an updateFUNDAMENTAL & CLINICAL PHARMACOLOGY, Issue 3 2008Pantelis A. Sarafidis Abstract As the incidence and the public health impact of type 2 diabetes are constantly rising, treatment of hyperglycemia, prevention of diabetes-related complications are currently top medical priorities. Within the last decade several new classes of oral hypoglycemic agents were added to our armamentarium against diabetes. Among these new classes, the group of thiazolidinediones, which act through reduction of insulin resistance is perhaps the most widely used. For about 20 years, numerous background and clinical studies have evaluated the beneficial and adverse effects of these compounds. Current knowledge suggests that thiazolidinediones are as effective as metformin or sulfonylurea derivatives in improving glycemic control and exert several other beneficial metabolic and vascular effects, such as improvement in lipid profile, blood pressure lowering, redistribution of body fat away from the central compartment, microalbuminuria regression, reduction in subclinical vascular inflammation and others. On the other hand, currently used thiazolidinediones have well-established side effects, most important of which are fluid retention leading to weight gain and heart failure deterioration. Further, in the expectance of proper outcome studies to clarify the effects of these agents in cardiovascular morbidity and mortality, data from recent meta-analyses suggest that rosiglitazone may increase the risk for some cardiovascular outcomes. This article will discuss all the above issues attempting to provide an updated overview of this expanding field. [source] The development of PET radioligands for imaging the translocator protein (18,kDa): What have we learned?JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 7 2010Christopher Luus Abstract The translocator protein (TSPO; 18,kDa), formerly known as the peripheral benzodiazepine receptor (PBR), is minimally expressed in the healthy brain. On the other hand, increased levels of TSPO have been noted in brain disorders for which an immune response is elicited. This increase in TSPO expression has been reported to coincide with the process of microglial activation making the measurement of TSPO density a useful indicator of active brain disease. To this end several new classes of TSPO positron emission tomography radioligands have been developed and evaluated. However, the incomplete pharmacological characterization of the TSPO and its ligands as well as differences in pathophysiology, pharmacology and molecular nature across species and tissue types means that caution must be exercised when comparing data obtained with various TSPO radioligands. A re-evaluation of our interpretation of imaging data, which better correlates with our current understanding of TSPO pharmacology in disease, requires consideration. Copyright © 2010 John Wiley & Sons, Ltd. [source] The clique partitioning problem: Facets and patching facetsNETWORKS: AN INTERNATIONAL JOURNAL, Issue 4 2001Maarten Oosten Abstract The clique partitioning problem (CPP) can be formulated as follows: Given is a complete graph G = (V, E), with edge weights wij , , for all {i, j} , E. A subset A , E is called a clique partition if there is a partition of V into nonempty, disjoint sets V1,,, Vk, such that each Vp (p = 1,,, k) induces a clique (i.e., a complete subgraph), and A = , {{i, j}|i, j , Vp, i , j}. The weight of such a clique partition A is defined as ,{i,j},Awij. The problem is now to find a clique partition of maximum weight. The clique partitioning polytope P is the convex hull of the incidence vectors of all clique partitions of G. In this paper, we introduce several new classes of facet-defining inequalities of P. These suffice to characterize all facet-defining inequalities with right-hand side 1 or 2. Also, we present a procedure, called patching, which is able to construct new facets by making use of already-known facet-defining inequalities. A variant of this procedure is shown to run in polynomial time. Finally, we give limited empirical evidence that the facet-defining inequalities presented here can be of use in a cutting-plane approach for the clique partitioning problem. © 2001 John Wiley & Sons, Inc. [source] Reversible acetylation of chromatin: Implication in regulation of gene expression, disease and therapeuticsBIOTECHNOLOGY JOURNAL, Issue 3 2009Ruthrotha B. Selvi Abstract The eukaryotic genome is a highly dynamic nucleoprotein complex that is comprised of DNA, histones, nonhistone proteins and RNA, and is termed as chromatin. The dynamicity of the chromatin is responsible for the regulation of all the DNA-templated phenomena in the cell. Several factors, including the nonhistone chromatin components, ATP-dependent remodeling factors and the chromatin-modifying enzymes, mediate the combinatorial post-translational modifications that control the chromatin fluidity and, thereby, the cellular functions. Among these modifications, reversible acetylation plays a central role in the highly orchestrated network. The enzymes responsible for the reversible acetylation, the histone acetyltransferases (HATs) and histone deacetylases (HDACs), not only act on histone substrates but also on nonhistone proteins. Dysfunction of the HATs/HDACs is associated with various diseases like cancer, diabetes, asthma, cardiac hypertrophy, retroviral pathogenesis and neurodegenerative disorders. Therefore, modulation of these enzymes is being considered as an important therapeutic strategy. Although substantial progress has been made in the area of HDAC inhibitors, we have focused this review on the HATs and their small-molecule modulators in the context of disease and therapeutics. Recent discoveries from different groups have established the involvement of HAT function in various diseases. Furthermore, several new classes of HAT modulators have been identified and their biological activities have also been reported. The scaffold of these small molecules can be used for the design and synthesis of better and efficient modulators with superior therapeutic efficacy. [source] | ||||||||||