Showing papers in "Bioorganic & Medicinal Chemistry in 1998"

TL;DR: This review summarises current knowledge on adenosine receptors, an important G protein-coupled receptor, with special reference to the opportunities for drug development.

TL;DR: These phenolic compounds were shown to be effective to protect biological systems against various oxidative stresses and protected red cells against oxidative hemolysis.

TL;DR: This work concludes that rather than engineering a 'new' pocket by mutation of Ile 338 in v-Src, the I338G and I338A mutants possess a 'path' for the N6 substituent on ATP to gain access to an existing pocket in the ATP binding site.

TL;DR: Several structural classes of small molecules are identified that are capable of inhibiting the TTR conformational changes facilitating amyloid fibril formation and are desirable as a promising approach to treat amyloids diseases.

TL;DR: An improved synthesis of the hindered PEG-camptothecin diester transport form has been achieved using the Mukaiyama reagent, and the use of a glycine linker group was found to provide similar efficacy in rodent models to that of simple camPTothecin 20-PEG ester, and displayed enhanced pharmacokinetics.

TL;DR: A valuable model which enables prediction of their activities was obtained from the CoMFA analysis, which may be employed for the drug designs of new bufadienolide analogues.

TL;DR: A number of model compounds resembling the fundamental bonding patterns of residual kraft lignin, including a series of stilbenes, were incubated with laccase from Trametes versicolor in the presence and absence of delignification 'mediators' ABTS and HBT, yielding several products showing side-chain oxidation/transposition, demethoxylation and hydroxylation reactions.

TL;DR: Comparison of the structures of functionary related proteins has shown that mutation may occur but necessary CH/pi interactions are conserved.

TL;DR: Comparison of the equilibrium constant in a zinc chlorin with those of the corresponding zinc bacteriochlorin and porphyrin led to an increase in the saturation and flexibility of the tetrapyrrole pi-plane ligands making the central zinc more axial-ligated.

TL;DR: 7 positional phenyl quinolone isomers were synthesized and 3-Phenyl-4-quinolone showed the greatest potency and was superior to indomethacin, although the two structures are quite different.

TL;DR: New galanthamine derivatives, especially bis-interacting ligands 3-5 and 7-9 were prepared in order to interact with the catalytic and the peripheral sites of acetylcholinesterase (AChE).

TL;DR: A series of novel phenethylthiazolylthiourea (PETT) derivatives targeting the nonnucleoside inhibitor (NNI) binding site of HIV reverse transcriptase (RT) have been designed based on the structure of the NNI binding pocket and showed potent anti-HIV activity.

TL;DR: Several phosphonate and bisphosphonate analogues of farnesyl pyrophosphate have been prepared for an examination of their ability to inhibitFarnesyl protein transferase (FPTase).

TL;DR: In general, the series of 9-ethylpurine derivatives exhibited a similar pharmacological profile at A1 and A2A receptors whereas some differences were found for the A3 and the A2B subtypes, which give raise to the hope that further modifications will result in the development of currently unavailable leads with good affinity and selectivity for A 2B adenosine receptors.

TL;DR: A series of Δ2-isoxazoline derivatives related to Broxaterol 1 and Falintolol 3 has been prepared and evaluated for their binding affinity to β1- and β2-adrenergic receptors.

TL;DR: Seven 4-methylcoumarins bearing different functionalities have been examined for the first time for their effect on NADPH-catalysed liver-microsomal lipid peroxidation and 7,8-dihydroxy- and diacetoxy-4-methylCoumarin were found to possess superb antioxidant and radical scavenging activities.

TL;DR: Derivatives 7dy and 7ey, lacking the ethylidene substituent, showed to be more active than tacrine in reversing the partial neuromuscular blockade induced by d-tubocurarine.

TL;DR: R rabdosiin exhibited the highest hyaluronidase-inhibitory activity and scavenging activities against active oxygens species such as superoxide anion radicals and hydroxyl radicals among the tested compounds.

TL;DR: Data indicate that the pyrrolidinone ring, especially the quarternary center at P2, interferes with the normal substrate binding mode with cruzain, but not with falcipain or the leishmania protease.

TL;DR: 3-Oxiranylbenzamide, 5-bromoisoquinolin-1-one and 5-iodoisoquolin- 1-one were among the most potent inhibitors of PARP activity in a preliminary screen in vitro.

TL;DR: The total synthesis and in vitro activities of a series of chemical inducers of dimerization (CIDs) is described, and some congeners possess potency comparable to or better than the first generation natural product-derived CID, FK1012.

TL;DR: A series of N-naphthylethyl amide derivatives were synthesized and evaluated as melatonin receptor ligands, leading to the conclusion that naphthalene is a bioisostere of the indole moiety of melatonin.

TL;DR: The results of these studies demonstrate that the 1,2,5-thiadiazolidin-3-one 1,1, dioxide platform provides an effective means for appending recognition elements in a well-defined vector relationship, and in fashioning highly-selective and potent inhibitors of serine proteinases.

TL;DR: It is demonstrated that dihydroeponemycin forms a covalent adduct with at least two intracellular proteins in human endothelial cells, indicating a specific interaction between natural product and the target proteins.

TL;DR: Several effective compounds have been found which possess higher selectivity indexes (SIs, 50% cytotoxic concentration/50% effective concentration) than those of T22 and TW70, attributed mainly to a decrease in cytotoxicity.

TL;DR: The design, synthesis and biological evaluation of a series of nitroaryl ether-based, nonpeptide mimetics based on Merck's arylether/alpha-aminoacid/guanidine framework and incorporates a novel nitro Daryl system are described.

TL;DR: A series of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid diesters substituted at the N-1 and/or C-4 positions of the dihydropyrsidine ring synthesized afforded better radioprotection than those without this substituent.

TL;DR: Evaluation of a variety of small molecule, non-peptidyl inhibitors of protein tyrosine phosphatase 1B (PTP1B), bearing the alpha, alpha-difluoromethylenephosphonic acid (DFMP) group, a non-hydrolyzable phosphate mimetic indicates that studies of non-PEP substrates with rat PTP1 can be used as a guide for the development of human P TP1B inhibitors

TL;DR: Structural-activity relationship studies on T22 have disclosed the contributions of each region of T22 to activity or cytotoxicity, and have provided the following useful information to develop new CXCR4 antagonists.