Showing papers in "Bioorganic & Medicinal Chemistry in 2007"

TL;DR: An attempt has been made to explore the in-depth knowledge from the classification of this enzyme to the clinical trials of their inhibitors, and QSAR results on the inhibition of various compound series against MMP-1 reveal a number of interesting points.

TL;DR: Several important physiological and physio-pathological functions are played by CAs present in organisms all over the phylogenetic tree, related to respiration and transport of carbon dioxide to bicarbonate between metabolizing tissues and the lungs, pH and CO(2) homeostasis, electrolyte secretion in a variety of tissues/organs, biosynthetic reactions, such as the gluconeogenesis and ureagenesis among others.

TL;DR: This review presents the drugs currently used in antituberculosis treatments and the most advanced compounds undergoing clinical trials and provides a description of their mechanism of action along with other series of inhibitors known to act on related biochemical targets.

TL;DR: While most compounds were exhibiting high activity in the analgesic-anti-inflammatory field, most of them were found to be inactive against bacteria and fungi.

TL;DR: A series of synthetic chalcones, flavanones, and flavones has been synthesized and evaluated for antitumor activity against the human kidney carcinoma cells TK-10, human mammary adenocarcinoma cells MCF-7 (estrogen receptor-positive), and human colon adenOCarcinomas cells HT-29.

TL;DR: Six small molecule VDAs, namely DMXAA, ZD6126, TZT1027, CA4P, AVE8062, and Oxi4503, are discussed, their synthesis, biological mechanism of action, and current clinical status.

TL;DR: The newly synthesized compounds were found to possess potential anti-inflammatory and analgesic activities and to be compatible with existing thiazolidin-4-one derivatives.

TL;DR: This review offers the first comprehensive analysis of strategies in drug development that either inhibit or exploit CYP enzymes for the treatment of cancer.

TL;DR: This review summarizes the disorders associated with elevation of lipids in blood and the current strategies to control them and the emphasis has been laid in particular on the new potential biological targets and the possible treatments.

TL;DR: The compound 2-(N'-2-pentylidene-hydrazino)-3-phenyl-3H-quinazolin-4-one (AS3) showed more potent anti-inflammatory activity when compared to the reference standard diclofenac sodium.

TL;DR: The hypothesis that stilbenes could be of therapeutic value in AD is supported as the mechanism of anti-amyloidogenic activity is still unknown and an original routine in vitro assay to search for inhibitors of Aβ fibril formation is described.

TL;DR: Darunavir contains a privileged, structure-based designed high-affinity P2 ligand, 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane (bis-THF), which has recently been approved for the treatment of HIV/AIDS patients harboring multidrug-resistant HIV-1 variants that do not respond to previously existing HAART regimens.

TL;DR: Alkylsulfone derivatives were found to be much more potent analgesic-antiinflammatory agents than the corresponding alkylthio analogs, in contrast to reference compound acetyl salicylic acid.

TL;DR: The compounds have been shown to be fungicidally active and can inhibit mycelia growth by approximately 50% at 2.9-93.3 microg/mL in vitro against 10 kinds of fungi.

TL;DR: Results indicate that di- and tri-substituted isatins may be useful leads for anticancer drug development in the future.

TL;DR: A novel series of 1-thiocarbamoyl-3-substituted phenyl-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole derivatives as promising MAO-B inhibitors was synthesized and investigated for the ability to inhibit selectively the activity of the A and B isoforms of monoamine oxidation.

TL;DR: While all the test compounds exhibited significant antihypertensive activity, 3-benzyl-2-methyl-3H-[1,2,4]triazolo[5,1-b] quinazolin-9-one exhibited antihyertensive activity more than the reference standard prazocin.

TL;DR: Interestingly, all compounds show noticeable selectivity toward breast cancer cell line MCF-7, and the most distinct and selective antiviral activity toward coxsackieviruses and echoviruses was observed with compounds having pyridine ring at C-2.

TL;DR: An efficient microwave-assisted synthesis of new (Z)-5-arylidenerhodanines under solvent-free conditions is described and their in vitro antifungal activity was evaluated following the CLSI guidelines against a panel of both standardized and clinical opportunistic pathogenic fungi.

TL;DR: Five polymethoxyflavones and hydroxylated PMFs showed strong inhibitory activities against the proliferation and induced apoptosis of HL-60 cell lines.

TL;DR: Several structurally unrelated scaffolds of the RhoKinase inhibitor were designed using pharmacophore information obtained from the results of a high-throughput screening and structural information from a homology model of Rho kinase to comprehensively understand and predict the structure-activity relationship of the inhibitors.

TL;DR: About 140 chiral pheromones are reviewed with regard to their stereochemistry-bioactivity relationships and problems encountered in studying chirality of phersomones were examined and analyzed to think about possible future directions in peromone science.

TL;DR: The results of in vitro tests showed that the compound 9 exhibited EC50 at 0.26 microM with minimal toxicity in MT-4 cells as compared to 0.35 microM for thiazobenzimidazole (TBZ), indicating that majority of compounds in this series exhibit higher selectivity index than TBZ.

TL;DR: All the compounds have been screened for their anti-inflammatory and analgesic activities at the dose of 50mg/kg po.

TL;DR: A prominent neuroprotective activity of FABT was observed in the neuronal cultures exposed to neurotoxic agents like serum deprivation and glutamate, and in anticancer concentrations it exerted a trophic effect in neuronal cell culture and had no influence on viability of normal cells including astrocytes, hepatocytes, and skin fibroblasts.

TL;DR: In the present study, a series of N-{4-[(4-amino-5-sulfanyl-4H-1,2,4-triazol-3-yl)methyl]-1,3-thiazol-2-yl}- 2-substituted-amide (1a-d) derivatives were synthesized in good yields and characterized by IR, 1H NMR, mass spectral and elemental analyses.

TL;DR: Findings indicate unique mechanisms of alpha-mangostin-induced apoptosis and its action as an effective chemosensitizer in DLD-1 cells.

TL;DR: The antituberculosis activity of molecules with diverse skeletons was investigated by means of the Electronic-Topological Method (ETM) and Artificial Neural Networks were used after the ETM to obtain the algorithmic base for the activity prediction.

TL;DR: In vitro binding assays showed that the implementation of phosphonates as phosphate mimetics provided compounds with similar receptor binding affinities as compared to their phosphate precursors.

TL;DR: This is the first QSAR model derived for description of flavonoid direct/indirect antioxidant effects in a cellular system, and this model could form the basis for further drug development of Flavonoid-like antioxidant compounds with therapeutic potential.