Showing papers in "Bioorganic & Medicinal Chemistry Letters in 2000"

TL;DR: Physically significant descriptors such as the solvent-accessible surface area, numbers of hydrogen bonds, and indices for cohesive interactions in solids are correlated with pharmacologically important properties including octanol/water partition coefficient (log P) and aqueous solubility (log S).

TL;DR: A series of benzylidene-1H-indol-2-one (oxindole) derivatives was synthesized and evaluated as cRaf-1 kinase inhibitors and inhibited the intracellular MAPK pathway.

TL;DR: Activity against the bacterial enzyme MurB supports the postulate that 4-thiazolidinones may be recognized as diphosphate mimics by a biological selector.

TL;DR: New 4',5',2,3,4-substituted 2'-amino chalcones were synthesized and evaluated for cytotoxicity against a panel of human tumor cell lines and demonstrated significantly increased antitumor activity.

TL;DR: Compounds containing a 1,2,3-triazole-substituted benzenesulfonamide were prepared and found to be potent and selective human beta3-adrenergic receptor agonists.

TL;DR: In order to develop new inhibitors of NF-kappaB activation, the authors designed and synthesized dehydroxymethyl derivatives of epoxyquinomicin C, namely, DHM2EQ and its regioisomer DHM3EQ.

TL;DR: Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are potent and selective inhibitors of Ick in vitro; some compounds are selective for lck over src.

TL;DR: The synthesis and in vivo activities of a series of substituted quinoline carboxyguanidines as a possible novel class of antidiabetic agents is described.

TL;DR: Two new anthraquinone glucosides and two stilbene glucoside gallates showed inhibitory activity of NO production in lipopolysaccharide-activated macrophages, and the active stilbenes inhibited iNOS induction.

TL;DR: Most compounds exhibited potent and well-balanced antibacterial activity as well as high stability to DHP-I comparable to that of meropenem.

TL;DR: Positively charged fullerene derivatives, moderately soluble in water:DMSO 9:1, have been tested using three strains of Mycobacterium spp.

TL;DR: High inhibitory activity against Mycobacterium tuberculosis was found for 9-benzylpurines carrying a phenylethynyl-, trans-styryl or aryl substituents in the 6-position and generally chlorine in the 2-position tends to increase activity.

TL;DR: Some of the screened compounds, 3a, 4c, 4e, 4f and 4i, have shown significant activity at 100 mg/kg dose against sensitive strain of Plasmodium berghei.

TL;DR: The synthesis of optically pure isomers of L- and D-TBOA and its erythro-isomers suggest that bulky substituents are crucial for non-transportable blockers.

TL;DR: The conventional Ala-scanning study is conducted in order to define the anti-HIV activity pharmacophore of T140 (the strongest analogue among the authors' compounds) and identified four indispensable amino acid residues (Arg2, Nal3, Tyr5, and Arg14).

TL;DR: A structure–activity relationship (SAR) study of a high-throughput screening lead resulted in the discovery of a potent and selective non-β-lactam inhibitor of class C β- lactamases.

TL;DR: New DOTA-based bifunctional prochelators for a broad application in the modification of biomolecules with metal ions were prepared and the coupling of 6d to a bioactive peptide on solid-phase was exemplified with use of a CCK-B (cholecystokinin) analogue.

TL;DR: A series of 8-alkylamino-5,7-dihydroxyflavones was prepared from chrysine via a seven step sequence and found to be efficient neuroprotective agents in vitro.

TL;DR: Structure-activity studies on a hexapeptide N-terminal cleavage product of a dodecamer substrate led to the identification of very potent and highly specific inhibitors of the HCV NS3 protease/NS4A cofactor peptide complex.

TL;DR: N-Benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine (BS/5-OMe DMT) was shown to bind at human 5-HT6 serotonin receptors with high affinity with Structural variation failed to result in significantly enhanced affinity.

TL;DR: A new series of coumarin inhibitors of DNA gyrase B bearing a N-propargyloxycarbamate at C-3' of various 5',5'-dialkylnoviose were synthesised and their antibacterial activities have been delineated.

TL;DR: In this article, Peptide-based α-Ketoamides, α-ketoesters and α-diketones were designed, synthesized and evaluated against HCV NS3 protease.

TL;DR: A novel ferrocene flu Conazole analogue was synthesized and its antifungal properties investigated against yeast strains of medical importance, including those intrinsically resistant to fluconazole.

TL;DR: The synthesis of twelve types of novel ferrocenyl sugars and their biological properties towards the malaria parasite and mouse cancer cell are described.

TL;DR: It is demonstrated that immunostimulatory activity is significantly reduced when the 5'-end of the PS-oligo is not accessible, rather than the 3'-end, suggesting that the 5'end plays a critical role in immunostIMulatory activity.

TL;DR: The design and synthesis of ATP-analogues, namely 4-amino-pyrazolo[3,4-d]pyrimidines and 4-AMino- pyrazolo [1,5-a][1,3,5]triazines, with DNA gyrase inhibitory activity are reported, with some compounds exhibited promising antibacterial activity.

TL;DR: The bis-dimethylaminoethyl derivative of quindoline (10H-indolo[3,2-b]quinoline), an alkaloid from the West African shrub Cryptolepis sanguinolenta, has been synthesised and has been shown to have modest cytotoxicity, as well as inhibitory activity against the telomerase enzyme.

TL;DR: Examination of the relative rates of hydrolysis of a variety of natural and unnatural fatty acid primary amide substrates using pure recombinant rat FAAH finds them to be similar to that of conventional fatty acid amides.

TL;DR: The synthesis of a series of new antitumour agents, the benzothiazole substituted quinol ethers and esters, is reported via the hypervalent iodine mediated oxidation of hydroxylated 2-phenylbenzothiazoles.

TL;DR: The N5-C6 double bond of NK109 (an antitumor benzo[c]phenanthridine alkaloid) is easily reduced under biological environment and to suppress the inactivation caused by reduction, 5, 6, and 8-substituted NK109 were synthesized.