abstract：:Two new bisalkaloids, dipiperamides D and E, were isolated as inhibitors of a drug metabolizing enzyme cytochrome P450 (CYP) 3A4 from the white pepper, Piper nigrum. Their structures were elucidated by spectroscopic methods. Dipiperamides D and E showed potent CYP3A4 inhibition with IC(50) values of 0.79 and 0.12 micr...

journal_title：Bioorganic & medicinal chemistry

authors： Tsukamoto S,Tomise K,Miyakawa K,Cha BC,Abe T,Hamada T,Hirota H,Ohta T

更新日期：2002-09-01 00:00:00

abstract：:In order to improve the immunotherapeutical potential of H-Cys-Leu-Gly-Gly-Leu-Leu-Thr-Met-Val-OH (CLG) peptide, an Epstein-Barr virus (EBV) subdominant epitope derived from the membrane protein LMP2, we have synthesized and tested CLG analogues containing cis- and/or trans-4-aminocyclohexanecarboxylic acid (ACCA) rep...

journal_title：Bioorganic & medicinal chemistry

authors： Marastoni M,Bazzaro M,Micheletti F,Gavioli R,Tomatis R

更新日期：2002-09-01 00:00:00

abstract：:A series of N-aryl heteroarylisopropanolamines in which an indole or a 3-arylpyrrole moiety was linked to an aryl group through an isopropanolamine linker, were designed and synthesized as potential anti-HIV-1-PR agents. Series was tested for their ability in blocking PR activity. As a rule, indole derivatives of clas...

journal_title：Bioorganic & medicinal chemistry

authors： Di Santo R,Costi R,Artico M,Massa S,Ragno R,Marshall GR,La Colla P

更新日期：2002-08-01 00:00:00

abstract：:Considerable efforts have been engaged in the design, synthesis and pharmacological characterization of radioligands for imaging the serotonin transporter, based on its implication in several neuropsychiatric diseases, such as depression, anxiety and schizophrenia. In the 5-halo-6-nitroquipazine series, the fluoro der...

journal_title：Bioorganic & medicinal chemistry

authors： Karramkam M,Dollé F,Valette H,Besret L,Bramoullé Y,Hinnen F,Vaufrey F,Franklin C,Bourg S,Coulon C,Ottaviani M,Delaforge M,Loc'h C,Bottlaender M,Crouzel C

更新日期：2002-08-01 00:00:00

abstract：:We have developed esonarimod, (+/-)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid, as a new antirheumatic drug. Now we describe herein the preparation of the enantiomers of (+/-)-deacetylesonarimod, the pharmaceutically active metabolites of esonarimod, and comparison of their antirheumatic activities. No s...

journal_title：Bioorganic & medicinal chemistry

authors： Noguchi T,Onodera A,Tomisawa K,Yamashita M,Takeshita K,Yokomori S

更新日期：2002-08-01 00:00:00

abstract：:The crystal structure of ABT-378 (lopinavir), bound to the active site of HIV-1 protease is described. A comparison with crystal structures of ritonavir, A-78791, and BILA-2450 shows some analogous features with previous reported compounds. A cyclic urea unit in the P(2) position of ABT-378 is novel and makes two bide...

journal_title：Bioorganic & medicinal chemistry

authors： Stoll V,Qin W,Stewart KD,Jakob C,Park C,Walter K,Simmer RL,Helfrich R,Bussiere D,Kao J,Kempf D,Sham HL,Norbeck DW

更新日期：2002-08-01 00:00:00

abstract：:New 6-[(2'-dialkylamino)ethyl]-4(3H)-pyrimidinones were prepared by a multistep procedure starting from acetone dicarboxylic acid diethyl ester and urea derivatives. These compounds were used as starting materials to obtain 4-N,N-dialkyl-6-vinyl-pyrimidine derivatives by an unprecedented tandem C-6 side chain Hofmann-...

journal_title：Bioorganic & medicinal chemistry

authors： Saladino R,Ciambecchini U,Maga G,Mastromarino P,Conti C,Botta M

更新日期：2002-07-01 00:00:00

abstract：:Tea catechins, an important class of polyphenols, have been shown to have wide spectrum of antitumor activity believed to be due mainly to their antioxidative effect. In this study, the radical scavenging behavior of catechins on 2,2-diphenyl-1-picrylhydrazyl (DPPH) was studied. Two reaction products of (+)-catechin, ...

journal_title：Bioorganic & medicinal chemistry

authors： Sang S,Cheng X,Stark RE,Rosen RT,Yang CS,Ho CT

更新日期：2002-07-01 00:00:00

abstract：:A series of 2',3'-exo-methylene carbocyclic nucleosides was synthesized as potential antiviral agents. These compounds were built on a bicyclo[3.1.0]hexane template that exhibits a rigid pseudoboat conformation and is capable of maintaining an identical conformation in solid state and in solution. The structures of th...

journal_title：Bioorganic & medicinal chemistry

authors： Bhushan RG,Vince R

更新日期：2002-07-01 00:00:00

abstract：:The pyrazolopyridine stimulators of soluble guanylate cyclase BAY 41-2272 and 41-8543 were oxidised in rats and dogs at their 5-pyrimidinyl-cyclopropyl and -morpholino residue. These metabolites activate the soluble guanylate cyclase, induce vasoelaxation and thereby may contribute to the in vivo activity of BAY 41-22...

journal_title：Bioorganic & medicinal chemistry

authors： Straub A,Benet-Buckholz J,Fröde R,Kern A,Kohlsdorfer C,Schmitt P,Schwarz T,Siefert HM,Stasch JP

更新日期：2002-06-01 00:00:00

abstract：:A series of secondary face modified cyclodextrins (CDs) were synthesised with the aim of constructing host molecules capable of forming host-guest complexes with neuromuscular blockers, especially with rocuronium bromide. Perfacial 2-O-substitution of gamma-CD with 4-carboxybenzyl resulted in a CD host molecule 1 that...

journal_title：Bioorganic & medicinal chemistry

authors： Tarver GJ,Grove SJ,Buchanan K,Bom A,Cooke A,Rutherford SJ,Zhang MQ

更新日期：2002-06-01 00:00:00

abstract：:Nitric oxide (NO) plays a critical role in a number of physiological processes and is produced in mammalian cells by nitric oxide synthase (NOS) isozymes. Because of the diverse functions of NO, pharmaceutical interventions which seek to abrogate adverse effects of excess NOS activity must not interfere with the norma...

journal_title：Bioorganic & medicinal chemistry

authors： Montgomery HJ,Perdicakis B,Fishlock D,Lajoie GA,Jervis E,Guy Guillemette J

更新日期：2002-06-01 00:00:00

abstract：:Glycamino acids, a family of sugar amino acids, are derivatives of C-glycosides that possesses a carboxyl group at the C-1 position and an amino group replacing one of the hydroxyl groups at either the C-2, 3, 4, or 6 position. We have prepared a series of glucose-type glycamino acids as monomeric building blocks: the...

journal_title：Bioorganic & medicinal chemistry

authors： Suhara Y,Yamaguchi Y,Collins B,Schnaar RL,Yanagishita M,Hildreth JE,Shimada I,Ichikawa Y

更新日期：2002-06-01 00:00:00

abstract：:A novel one-pot synthesis of imidazo[1,2-c]pyrimido[5,4-e]pyrimidinones (2), tetraazaacenaphthene-3,6-diones (4), tetarazaphenalene-1,7-dione (4d) is delineated from the reaction of cyclic ketene aminal (1) and alkyl or aryl isothiocyanate through tandem addition-cyclization reactions. However, reaction of ketene amin...

journal_title：Bioorganic & medicinal chemistry

authors： Ram VJ,Goel A,Sarkhel S,Maulik PR

更新日期：2002-05-01 00:00:00

abstract：:3-D-Quantitative structure--activity relationships of N-(3-acyloxy-2-benzylpropyl)-N'-dihydroxytetrahydro-benzazepine and tetrahydroisoquinoline and N-(3-acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea analogues as potent vanilloid receptor ligands were investigated using the CoMFA and the COMSIA metho...

journal_title：Bioorganic & medicinal chemistry

authors： Kim KH

更新日期：2002-05-01 00:00:00

abstract：:The pH dependence of the affinity of a 11-mer phosphotyrosine (pY) peptide (EPQpYEEIPIYL-NH2) for the SH2 domain of the tyrosine kinase p56(lck) was investigated with surface plasmon resonance (SPR). From SPR competition experiments the affinity in solution was obtained. The pH dependence of the affinity in solution c...

journal_title：Bioorganic & medicinal chemistry

authors： de Mol NJ,Gillies MB,Fischer MJ

更新日期：2002-05-01 00:00:00

abstract：:Aggregation of amyloid peptide (Abeta) has been identified as a major feature of the pathogenesis of Alzheimer's disease. Increased risk for disease is associated with increased formation of polymerized Abeta. Inhibition of formation of toxic (aggregated) form of Abeta is one of the therapeutic possibilities. Beta she...

journal_title：Bioorganic & medicinal chemistry

authors： Hetényi C,Körtvélyesi T,Penke B

更新日期：2002-05-01 00:00:00

abstract：:Mainly driven by the needs of antisense research, a large number of oligonucleotide analogues have been prepared and evaluated over the last 15 years. Besides minor structural modifications of the building blocks of DNA and RNA itself, a considerable effort has been devoted to the de novo design of nucleoside analogue...

journal_title：Bioorganic & medicinal chemistry

authors： Leumann CJ

更新日期：2002-04-01 00:00:00

abstract：:20-fluoro-17(20)-pregnenolone derivatives were designed as enol mimics of pregnenolone. All of the targeted, novel fluoroolefins were potent inhibitors of C17(20) lyase. ...

journal_title：Bioorganic & medicinal chemistry

authors： Burkhart JP,Weintraub PM,Gates CA,Resvick RJ,Vaz RJ,Friedrich D,Angelastro MR,Bey P,Peet NP

更新日期：2002-04-01 00:00:00

abstract：:MO theoretical calculations were used with the aim to investigate the electronic properties of a number of sulphonylureas 1-8 which are employed as antifeedants. Quantum chemical descriptors [electron density, molecular electrostatic potential (MEP), the topology of frontier orbitals and reactivity index] were determi...

journal_title：Bioorganic & medicinal chemistry

authors： Galeazzi R,Marucchini C,Orena M,Zadra C

更新日期：2002-04-01 00:00:00

abstract：:Design and synthesis of an EP2-receptor selective agonist began with the chemical modification of alpha- and omega-chains of butaprost 1a, which exhibits an affinity for the IP-receptor. Two series of prostaglandin (PG) analogues with a 16-hydroxy-17,17-trimethylene moiety as an omega-chain were identified. Among thos...

journal_title：Bioorganic & medicinal chemistry

authors： Tani K,Naganawa A,Ishida A,Sagawa K,Harada H,Ogawa M,Maruyama T,Ohuchida S,Nakai H,Kondo K,Toda M

更新日期：2002-04-01 00:00:00

abstract：:Novel ferulic acid derivatives in which feruloyl groups were attached to the hydroxyl groups of myo-inositol 1,3,5-orthoformate derivatives were synthesized. These feruloyl-myo-inositols suppressed the cyclooxygenase-2 (COX-2) promoter activity in a concentration-dependent manner. Among the examined compounds, compoun...

journal_title：Bioorganic & medicinal chemistry

authors： Hosoda A,Ozaki Y,Kashiwada A,Mutoh M,Wakabayashi K,Mizuno K,Nomura E,Taniguchi H

更新日期：2002-04-01 00:00:00

abstract：:The Thermotoga maritima aldolase gene has been cloned into a T7 expression vector and overexpressed in Escherichia coli. The preparation yields 470 UL(-1) of enzyme at a specific activity of 9.4 U mg(-1). During retroaldol cleavage of KDPG, the enzyme shows a k(cat) that decreases with decreasing temperature. A more t...

journal_title：Bioorganic & medicinal chemistry

authors： Griffiths JS,Wymer NJ,Njolito E,Niranjanakumari S,Fierke CA,Toone EJ

更新日期：2002-03-01 00:00:00

abstract：:(+)-4-Demethoxy-1,4-dimethyldaunomycinone 1 was synthesized using a convergent approach. Here, the key tetracyclic compound 10 was assembled by way of a Diels-Alder reaction using the sugar-based diene 8 and the quinizarin-related dienophile 7. ...

journal_title：Bioorganic & medicinal chemistry

authors： Kotha S,Stoodley RJ

更新日期：2002-03-01 00:00:00

abstract：:We have examined the efficiency of DNA photooxidation in DNA/PNA duplex and DNA/(PNA)(2) triplex for the first time. DNA/PNA duplex was cleaved at GG steps by external riboflavin with high efficiency like specific GG cleavage in DNA/DNA duplex. However, the 5'G selectivity of the GG oxidation in DNA/PNA duplex was muc...

journal_title：Bioorganic & medicinal chemistry

authors： Okamoto A,Tanabe K,Dohno C,Saito I

更新日期：2002-03-01 00:00:00

abstract：:Aminocarbonyloxymethyl esters based on (S)-amino acid carriers were synthesised and evaluated as potential prodrugs of carboxylic acid agents. In addition, the compounds were evaluated as topical prodrugs with the aim of improving the dermal delivery of two non-steroidal anti-inflammatory agents: naproxen and flufenam...

journal_title：Bioorganic & medicinal chemistry

authors： Mendes E,Furtado T,Neres J,Iley J,Jarvinen T,Rautio J,Moreira R

更新日期：2002-03-01 00:00:00

abstract：:A series of new 4-amino-3-[3-[4-(2-methoxy or nitro phenyl)-1-piperazinyl] propyl]thio]-5-(substitutedphenyl)[1,2,4]triazoles 11a-t was synthesized in order to obtain compounds with high affinity and selectivity for 5-HT(1A) receptor over the alpha(1)-adrenoceptor. A series of isomeric 4-amino-2-[3-[4-(2-methoxy or ni...

journal_title：Bioorganic & medicinal chemistry

authors： Sarvà MC,Romeo G,Guerrera F,Siracusa M,Salerno L,Russo F,Cagnotto A,Goegan M,Mennini T

更新日期：2002-02-01 00:00:00

abstract：:omega-(1H-Imidazol-4-yl)alkane-1-sulfonamides were prepared and found to be potent histamine H(3) receptor antagonists. High receptor affinity and a low difference in the data between the bioassays were achieved with 5-(1H-imidazol-4-yl)pentane-1-sulfonic acid 4-chlorobenzylamide (16). Good in vitro profiles were also...

journal_title：Bioorganic & medicinal chemistry

authors： Tozer MJ,Buck IM,Cooke T,Kalindjian SB,Pether MJ,Steel KI

更新日期：2002-02-01 00:00:00

abstract：:Further structure-activity relationship (SAR) studies with the 1,2,3,4-tetrahydroisoquinoline (THIQ) class of 5-HT(1A) ligands led to the synthesis of new 1-adamantoyloaminoalkyl derivatives. The impact of substituent variations in the aromatic part of THIQ moiety on 5-HT(1A) and 5-HT(2A) receptor affinities, as well ...

journal_title：Bioorganic & medicinal chemistry

authors： Bojarski AJ,Mokrosz MJ,Minol SC,Kozioł A,Wesołowska A,Tatarczyńska E,Kłodzińska A,Chojnacka-Wójcik E

更新日期：2002-01-01 00:00:00

abstract：:5-Demethylovalicin was isolated from the fermentation broth Chrysosporium lucknowense and the structure was identified by spectroscopic methods. 5-Demethylovalicin inhibited the recombinant human MetAP-2 (IC(50)=17.7 nM) and the growth of human umbilical vein endothelial cells (HUVEC; IC(50)=100 nM) in cell proliferat...

journal_title：Bioorganic & medicinal chemistry

authors： Son KH,Kwon JY,Jeong HW,Kim HK,Kim CJ,Chang YH,Choi JD,Kwon BM

更新日期：2002-01-01 00:00:00

abstract：:Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies for 3-aryloxazolidin-2-one antibacterials were performed using the genetic function approximation algorithm. This study was performed using 60 compounds, in which the QSAR models were developed using a training set of 50 compounds. The in...

journal_title：Bioorganic & medicinal chemistry

authors： Karki RG,Kulkarni VM

更新日期：2001-12-01 00:00:00

abstract：:In an effort to expand the spectrum of activity of the oxazolidinone class of antibacterial agents to include Gram-negative bacteria, a series of new carbon-carbon linked pyrazolylphenyl analogues has been prepared. The alpha-N-substituted methyl pyrazole (10alpha) in the C3-linked series exhibited very good Gram-posi...

journal_title：Bioorganic & medicinal chemistry

authors： Lee CS,Allwine DA,Barbachyn MR,Grega KC,Dolak LA,Ford CW,Jensen RM,Seest EP,Hamel JC,Schaadt RD,Stapert D,Yagi BH,Zurenko GE,Genin MJ

更新日期：2001-12-01 00:00:00

abstract：:Bacterial DNA and synthetic oligodeoxynucleotides containing unmethylated CpG-motifs in a particular sequence context activate vertebrate immune cells. We examined the significance of negatively charged internucleoside linkages in the flanking sequences 5' and 3' to the CpG-motif on immunostimulatory activity. Cell pr...

journal_title：Bioorganic & medicinal chemistry

authors： Yu D,Kandimalla ER,Zhao Q,Cong Y,Agrawal S

更新日期：2001-11-01 00:00:00

abstract：:Oligonucleotides with a 3'-3' inversion of polarity site assured by one lysine residue have been synthesized, characterized and used as third strands in alternate strand triple helix formation. UV melting studies and molecular mechanics calculations have been carried out to investigate the stability and the geometry o...

journal_title：Bioorganic & medicinal chemistry

authors： Barone G,De Napoli L,Di Fabio G,Giancola C,Messere A,Montesarchio D,Petraccone L,Piccialli G

更新日期：2001-11-01 00:00:00

abstract：:The 3-D QSAR analysis with new imidazo- and pyrrolo-quinolinedione derivatives was conducted by Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA). When crossvalidation value (q(2)) is 0.844 at four components, the Pearson correlation coefficient (r(2)) of the C...

journal_title：Bioorganic & medicinal chemistry

authors： Suh ME,Kang MJ,Park SY

更新日期：2001-11-01 00:00:00

abstract：:A quantitative structure-activity relationship (QSAR) study has been made on two different series of tetrahydropyrimidinones acting as HIV-1 protease inhibitors. A structural parameter, the first order valence molecular connectivity index ((1)chi(v)), has been used to account for the variation in the activity. The pro...

journal_title：Bioorganic & medicinal chemistry

authors： Gayathri P,Pande V,Sivakumar R,Gupta SP

更新日期：2001-11-01 00:00:00

abstract：:A growing number of proteins are known to exert their regulatory or biological functions via RNA binding. In some cases genetic interactions allow us to infer candidate targets for RNA directed regulation, but in many other cases identification of potential regulatory targets is problematic. We have developed an in vi...

journal_title：Bioorganic & medicinal chemistry

authors： Brunel C,Ehresmann B,Ehresmann C,McKeown M

更新日期：2001-10-01 00:00:00

abstract：:Transport across the intestinal barrier of compounds with low permeability may be facilitated by targeting the human oligopeptide transporter, hPepT1. A flexible synthetic pathway for attaching compounds to dipeptides through ester or amide bonds was developed. Furthermore, a synthetic approach to functionalize model ...

journal_title：Bioorganic & medicinal chemistry

authors： Friedrichsen GM,Jakobsen P,Taub M,Begtrup M

更新日期：2001-10-01 00:00:00

abstract：:Theoretical and structural studies followed by the directed synthesis and in vitro biological tests lead us to novel noncovalent thrombin pseudopeptide inhibitors. We have incorporated an azapeptide scaffold into the central part of the classical tripeptide D-Phe-Pro-Arg inhibitor structure thus eliminating one stereo...

journal_title：Bioorganic & medicinal chemistry

authors： Zega A,Mlinsek G,Sepic P,Golic Grdadolnik S,Solmajer T,Tschopp TB,Steiner B,Kikelj D,Urleb U

更新日期：2001-10-01 00:00:00

abstract：:Configurational stability of dinucleoside H-phosphonates and the stereochemical course of their sulfurisation in the presence of diazabicyclo[5.4.0]undec-7-ene (DBU) were investigated using 31P NMR spectroscopy. It was found that under the reaction conditions and irrespective of the type of protecting groups present i...

journal_title：Bioorganic & medicinal chemistry

authors： Johansson T,Stawinski J

更新日期：2001-09-01 00:00:00