abstract：:Bacterial chemotactic responses are initiated when certain small molecules (i.e., carbohydrates, amino acids) interact with bacterial chemoreceptors. Although bacterial chemotaxis has been the subject of intense investigations, few have explored the influence of attractant structure on signal generation and chemotaxis...

journal_title：Bioorganic & medicinal chemistry

authors： Gestwicki JE,Strong LE,Borchardt SL,Cairo CW,Schnoes AM,Kiessling LL

更新日期：2001-09-01 00:00:00

abstract：:We have used fluorescence anisotropy to measure in situ the thermodynamics of binding of alanine-rich mutants of the GCN4 basic region/leucine zipper (bZIP) to short DNA duplexes, in which thymines were replaced with uracils, in order to quantify the contributions of the C5 methyl group on thymines with alanine methyl...

journal_title：Bioorganic & medicinal chemistry

authors： Kise KJ Jr,Shin JA

更新日期：2001-09-01 00:00:00

abstract：:A new meso-2,4,6-trimethoxyphenyl porphyrin covalently linked to a 2',6'-dinitro-4'-trifluoromethylphenyl group by an amine bond 5 and its metal complex with Cd(II) 6 was prepared. The photodynamic activities of 5 and 6 were evaluated in vitro on Hep-2 cells. A considerable increase in the photocytotoxic effect was fo...

journal_title：Bioorganic & medicinal chemistry

authors： Milanesio ME,Morán FS,Yslas EI,Alvarez MG,Rivarola V,Durantini EN

更新日期：2001-08-01 00:00:00

abstract：:A series of specific alpha-ketoheterocycles (benzoxazole, thiazole, imidazole, tetrazole, and thiazole-4-carboxylate) has been synthesized in order to assess their potential as beta-lactamase inhibitors. The syntheses were achieved either by construction of the heterocycle (benzoxazole) from an appropriate alpha-hydro...

journal_title：Bioorganic & medicinal chemistry

authors： Kumar S,Pearson AL,Pratt RF

更新日期：2001-08-01 00:00:00

abstract：:Two novel series of all-trans-beta-retinoic acid derivatives were synthesized and found to possess anticancer activity. The first series, cephalosporin 3'-retinoic esters 6 and 7 were, respectively, obtained by the condensation of all-trans-beta-retinoic acid (2) with cephalosporins 4 and 5. The second series, 7-(reti...

journal_title：Bioorganic & medicinal chemistry

authors： Hakimelahi GH,Ly TW,Yu SF,Zakerinia M,Khalafi-Nezhad A,Soltani MN,Gorgani MN,Chadegani AR,Moosavi-Movahedi AA

更新日期：2001-08-01 00:00:00

abstract：:A sensitive chemiluminescence (CL) sensor for berberine combined with flow-injection (FI) technology is described. The analytical reagents involved in the CL reaction, including luminol and potassium ferricyanide, were both immobilized on an anion-exchange resin column. While a volume of sodium phosphate was passed th...

journal_title：Bioorganic & medicinal chemistry

authors： Song Z,Zhao T,Wang L,Xiao Z

更新日期：2001-07-01 00:00:00

abstract：:Plaunotol, a known antiulcer drug, has antibacterial activities against Helicobacter pylori. Plaunotol thiourea derivatives 2--4 and diol derivatives 6--10 were designed in search for a compound with high antibacterial activities. Thiourea derivatives 2--4 were synthesized regioselectively using our effective syntheti...

journal_title：Bioorganic & medicinal chemistry

authors： Tago K,Minami E,Masuda K,Akiyama T,Kogen H

更新日期：2001-07-01 00:00:00

abstract：:Several benzaldoximes, benzaldehyde-O-ethyloximes, and acetophenonoximes were synthesized and evaluated as tyrosinase inhibitors by an assay based on tyrosinase catalyzed L-DOPA oxidation. Whereas benzaldoxime itself is only a weak inhibitor, its derivatives with one or two hydroxy or methoxy moieties in para and meta...

journal_title：Bioorganic & medicinal chemistry

authors： Ley JP,Bertram HJ

更新日期：2001-07-01 00:00:00

abstract：:A series of potent inhibitors of P-selectin as potential anti-inflammatory agents is reported. These compounds are derivatives of galactocerebrosides bearing a malonate side chain in positions 2 and 3 of the galactose moiety. Based on the binding mode of sialyl Lewis X, the two acidic groups of the malonate are design...

journal_title：Bioorganic & medicinal chemistry

authors： Marinier A,Martel A,Bachand C,Plamondon S,Turmel B,Daris JP,Banville J,Lapointe P,Ouellet C,Dextraze P,Menard M,Wright JJ,Alford J,Lee D,Stanley P,Nair X,Todderud G,Tramposch KM

更新日期：2001-06-01 00:00:00

abstract：:3D-Quantitative structure-activity relationships of 2,4,5- and 2,3,4,5-substituted imidazoles as a novel class of potent and nontoxic modulators of Pgp mediated MDR were investigated using CoMFA and COMSIA approaches. The best CoMFA model obtained from 46 imidazole analogues is a two-component model with the following...

journal_title：Bioorganic & medicinal chemistry

authors： Kim KH

更新日期：2001-06-01 00:00:00

abstract：:New sildenafil analogues containing an ether ring fused into the phenyl moiety, 6a--d and 7a--d, were efficiently synthesized from the readily available starting materials, 1a--d and 2, in five steps. Ab initio calculations indicated that introduction of a cyclic ether to the phenyl group might enhance the co-planarit...

journal_title：Bioorganic & medicinal chemistry

authors： Kim DK,Lee N,Lee JY,Ryu DH,Kim JS,Lee SH,Choi JY,Chang K,Kim YW,Im GJ,Choi WS,Kim TK,Ryu JH,Kim NH,Lee K

更新日期：2001-06-01 00:00:00

abstract：:Based on general SARs previously described for anti-HIV-1 diarylsulfone derivatives, a series of 2-amino- and 2-carboxamido-3-arylsulfonylthiophenes has been prepared and evaluated as potential antiviral and antitumor agents. In cell culture, some of the 2-aminothiophenes exhibited moderate and selective activity agai...

journal_title：Bioorganic & medicinal chemistry

authors： Stephens CE,Felder TM,Sowell JW Sr,Andrei G,Balzarini J,Snoeck R,De Clercq E

更新日期：2001-05-01 00:00:00

abstract：:A novel series of mutilin 14-carbamates has been discovered as a result of structure-activity studies on the naturally occurring antibiotic pleuromutilin (1). In particular, the 4-methoxybenzoylcarbamate, SB-222734 (15o) displays potent antibacterial activity against a number of bacterial pathogens which are resistant...

journal_title：Bioorganic & medicinal chemistry

authors： Brooks G,Burgess W,Colthurst D,Hinks JD,Hunt E,Pearson MJ,Shea B,Takle AK,Wilson JM,Woodnutt G

更新日期：2001-05-01 00:00:00

abstract：:There is currently interest in the metabolism of the various compounds which make up the vitamin E family, especially with regards to the possible use of vitamin E metabolites as markers of oxidative stress and adequate vitamin E supply. A number of vitamin E metabolites have been described to date and we have recentl...

journal_title：Bioorganic & medicinal chemistry

authors： Pope SA,Burtin GE,Clayton PT,Madge DJ,Muller DP

更新日期：2001-05-01 00:00:00

abstract：:A series of 5-aryl- and 3,5-bis-aryl-2-amino-1,4-pyrazine derivatives 4 and 6, and related imidazolopyrazinones 7, has been synthesized, the aryl groups of which are catechol and/or phenol substituents. These compounds, tested against human keratinocyte cells stressed by UVB irradiation, showed high antioxidative prop...

journal_title：Bioorganic & medicinal chemistry

authors： Cavalier JF,Burton M,Dussart F,Marchand C,Rees JF,Marchand-Brynaert J

更新日期：2001-04-01 00:00:00

abstract：:Two hybrid analogues of the kainic acid receptor agonists, 2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid (ATPA) and (2S,4R)-4-methylglutamic acid ((2S,4R)-4-Me-Glu), were designed, synthesized, and characterized in radioligand binding assays using cloned ionotropic and metabotropic glutamic acid recept...

journal_title：Bioorganic & medicinal chemistry

authors： Bunch L,Johansen TH,Bräuner-Osborne H,Stensbøl TB,Johansen TN,Krogsgaard-Larsen P,Madsen U

更新日期：2001-04-01 00:00:00

abstract：:The synthesis and biological activity of a novel series of 2-alkyl-4-pyrrolidinylthio-beta-methylcarbapenems containing a variety of cationic heteroaromatic substituents linked via a C-C bond is described. As a result of these studies, we selected FR21818 (In) as a candidate compound for development. FR21818 exhibited...

journal_title：Bioorganic & medicinal chemistry

authors： Zam HA,Barrett D,Tanaka A,Sasaki H,Matsuda K,Sakurai M,Terasawa T,Shirai F,Chiba T,Matsumoto Y,Tawara S

更新日期：2001-04-01 00:00:00

abstract：:The synthesis of a range of 2-amido-3-hydroxypyridin-4-ones as bidentate iron(III) chelators with potential for oral administration is described. The pKa values of the ligands together with the stability constants of their iron(III) complexes have been determined. Results indicate that the introduction of an amido sub...

journal_title：Bioorganic & medicinal chemistry

authors： Liu ZD,Piyamongkol S,Liu DY,Khodr HH,Lu SL,Hider RC

更新日期：2001-03-01 00:00:00

abstract：:In order to expand the recognition code by hairpin polyamides to include DNA sequences of the type 5'-CWWC-3' two polyamides, PyPyPyPy-(R)(H2N)gamma-ImPyPyIm-beta-Dp (1) and PyPyPyPy-(R)(H2N)gamma-ImPy-beta-Im-beta-Dp (2) were synthesized which have in common an Py/Im pair in the terminal position for targeting C x G ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang CC,Ellervik U,Dervan PB

更新日期：2001-03-01 00:00:00

abstract：:Synthesis of a range of indomethacin analogues, required for investigation in combination toxicity assays, bearing both N-benzyl and N-benzoyl groups, is described. ...

journal_title：Bioorganic & medicinal chemistry

authors： Maguire AR,Plunkett SJ,Papot S,Clynes M,O'Connor R,Touhey S

更新日期：2001-03-01 00:00:00

abstract：:The toxicity of the molecules currently used in the treatment of human cytomegalovirus (HCMV) in immunocompromised hosts often causes interruption of the therapy. Cyclodextrins (Cds), oligosaccharides possessing a hydrophobic cavity, have the property of forming inclusion complexes with a great number of molecules, im...

journal_title：Bioorganic & medicinal chemistry

authors： Nicolazzi C,Abdou S,Collomb J,Marsura A,Finance C

更新日期：2001-02-01 00:00:00

abstract：:While hemoglobin is one of the most well characterized proteins due to its function in oxygen transport, few additional properties of hemoglobin have been described. While screening serum samples for novel antimicrobial factors, it was found that intact hemoglobin tetramers, including that from human, exhibited consid...

journal_title：Bioorganic & medicinal chemistry

authors： Parish CA,Jiang H,Tokiwa Y,Berova N,Nakanishi K,McCabe D,Zuckerman W,Xia MM,Gabay JE

更新日期：2001-02-01 00:00:00

abstract：:Fully N- and O-sulfated homooligomers from octamer to nonadecamer of tyrosine were obtained as their sodium salts, aO3S-[Tyr(SO3Na)]n-ONa (n = 8-19), from reaction mixtures of tyrosine with sulfur trioxide trimethylamine and pyridine comlexes, respectively, in pyridine. Their anti-HIV activity increased along with the...

journal_title：Bioorganic & medicinal chemistry

authors： Ueki M,Watanabe S,Saitoh T,Nakashima H,Yamamoto N,Ogawara H

更新日期：2001-02-01 00:00:00

abstract：:8-Chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide, monohydrochloride (1, SC-51089) is a functional PGE2 antagonist selective for the EP1 receptor subtype with antinociceptive activity. Analogues of SC-51089, in which the diacylhydrazine moiety has been replaced with 2,...

journal_title：Bioorganic & medicinal chemistry

authors： Hallinan EA,Hagen TJ,Tsymbalov S,Stapelfeld A,Savage MA

更新日期：2001-01-01 00:00:00

abstract：:A series of N-(3-acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea derivatives were investigated as vanilloid receptor ligands in an effort to discover a novel class of analgesics. The proposed pharmacophore model of resiniferatoxin. which includes the C20 homovanillic moiety, the C3-carbonyl and the ort...

journal_title：Bioorganic & medicinal chemistry

authors： Lee J,Lee J,Kim J,Kim SY,Chun MW,Cho H,Hwang SW,Oh U,Park YH,Marquez VE,Beheshti M,Szabo T,Blumberg PM

更新日期：2001-01-01 00:00:00

abstract：:CD22 is a cell-surface glycoprotein uniquely located on mature B-cells and B-cell derived tumour cells. Current evidence suggests that binding of endogenous ligands to CD22 leads to modulation of B-cell activation by antigen. Incidentally, however, B-cell activation may derail. and lead to an undesired immune response...

journal_title：Bioorganic & medicinal chemistry

authors： Sliedregt LA,van Rossenberg SM,Autar R,Valentijn AR,van der Marel GA,van Boom JH,Piperi C,van der Merwe PA,Kuiper J,van Berkel TJ,Biessen EA

更新日期：2001-01-01 00:00:00

abstract：:Highly regioselective electrophilic substitution of dibenzofluorene was achieved and the nitro derivative was transformed to a variety of new anticancer agents. ...

journal_title：Bioorganic & medicinal chemistry

authors： Becker FF,Mukhopadhyay C,Hackfeld L,Banik I,Banik BK

更新日期：2000-12-01 00:00:00

abstract：:Molecular combinations of two antioxidants (i.e., ascorbic acid and the pharmacophore of alpha-tocopherol), namely the 2,3-dihydroxy-2,3-enono-1,4-lactone and the chromane residues, have been designed and tested for their radical scavenging activities. When evaluated for their capability to inhibit malondialdehyde (MD...

journal_title：Bioorganic & medicinal chemistry

authors： Manfredini S,Vertuani S,Manfredi B,Rossoni G,Calviello G,Palozza P

更新日期：2000-12-01 00:00:00

abstract：:We are investigating compounds that could be useful in the treatment of neoplastic lesions of the cervix by acting on the oncoprotein E6 of human papillomavirus-16. The E6 protein contains two potential zinc-binding domains that are required for most of its functions. We have published tests that measure (i) the relea...

journal_title：Bioorganic & medicinal chemistry

authors： Beerheide W,Sim MM,Tan YJ,Bernard HU,Ting AE

更新日期：2000-11-01 00:00:00

abstract：:5-epi, 10-epi, 8-Deethyl, and 10-demethyl analogues of callystatin A, a potent cytotoxic spongean polyketide, were synthesized to elucidate structure-requirement for cytotoxic potency. Inversion of the asymmetric center at C-10 in callystatin A minimally affected the activity, while lack of the 10-methyl group in call...

journal_title：Bioorganic & medicinal chemistry

authors： Murakami N,Sugimoto M,Nakajima T,Kawanishi M,Tsutsui Y,Kobayashi M

更新日期：2000-11-01 00:00:00

abstract：:An analogue 2 of coenzyme A (CoA) has been prepared in which the geminal methyl groups are replaced with hydrogens. An NMR titration study was conducted and shifts in frequency of protons in the pantetheine portion of the molecule upon titration of the adenine base were observed as has been previously reported with Co...

journal_title：Bioorganic & medicinal chemistry

authors： Vogel KW,Stark LM,Mishra PK,Yang W,Drueckhammer DG

更新日期：2000-10-01 00:00:00

abstract：:The discovery of the first class of potent glucose-6-phosphatase catalytic site inhibitors, substituted 4,5,6,7-tetrahydrothieno[3,2-c]- and -[2,3-c]pyridines, is described. Optimisation of this series involved solution phase combinatorial synthesis and very potent compounds were prepared with IC50 values down to 140 ...

journal_title：Bioorganic & medicinal chemistry

authors： Madsen P,Lundbeck JM,Jakobsen P,Varming AR,Westergaard N

更新日期：2000-09-01 00:00:00

abstract：:Furanfurin (2-beta-D-ribofuranosylfuran-4-carboxamide) derivatives and analogues were synthesized and their affinity for adenosine receptors was determined. The agonistic behavior of furanfurin against A1 receptors is preserved only when the furan ring is substituted with isosteric pentatomic ring systems such as oxaz...

journal_title：Bioorganic & medicinal chemistry

authors： Franchetti P,Cappellacci L,Marchetti S,Martini C,Costa B,Varani K,Borea PA,Grifantini M

更新日期：2000-09-01 00:00:00

abstract：:The highly selective I1-PBS imidazoline analogue PMS 952 has been selected to study the incidence of intramolecular hydrogen bond and molecular flexibility on its biological activity. On one hand, the weak energy difference between three calculated conformers does not support the stabilization of one conformer by an i...

journal_title：Bioorganic & medicinal chemistry

authors： Ye HF,Dive G,Dehareng D,Heymans F,Godfroid JJ

更新日期：2000-08-01 00:00:00

abstract：:Polyamides consisting of N-methylpyrrole (Py), N-methylimidazole (Im), and N-methyl-3-hydroxypyrrole (Hp) are synthetic ligands that recognize predetermined DNA sequences with affinities and specificities comparable to many DNA-binding proteins. As derivatives of the natural products distamycin and netropsin, Py/Im/Hp...

journal_title：Bioorganic & medicinal chemistry

authors： Bremer RE,Szewczyk JW,Baird EE,Dervan PB

更新日期：2000-08-01 00:00:00

abstract：:Synthesis and antimicrobial activity of squalamine analogue 2 are reported. The synthesis of 2 was accomplished from bisnoralcohol 3. The spermidine moiety was introduced via reductive amination of an appropriately functionalized 3beta-aminosterol with spermidinyl aldehyde 17 utilizing sodium triacetoxyborohydride as ...

journal_title：Bioorganic & medicinal chemistry

authors： Kim HS,Choi BS,Kwon KC,Lee SO,Kwak HJ,Lee CH

更新日期：2000-08-01 00:00:00

abstract：:The activated vitamin D3 derivative 26,27-F6-1alpha,25(OH)2D3 (2a), its three A-ring diastereomers (2b, 2c, 2d), and 5,6-trans isomer (2e) were prepared. Two analogues (2b, 2c) of these isomers were synthesized by a palladium catalyzed coupling reaction using vinyl bromide 5 and enynes (6a, 6b), which were derived fro...

journal_title：Bioorganic & medicinal chemistry

authors： Ikeda M,Takahashi K,Dan A,Koyama K,Kubota K,Tanaka T,Hayashi M

更新日期：2000-08-01 00:00:00

abstract：:Tertiary sulfonamidomethyl esters of benzylpenicillin (4) were synthesised and evaluated as a new class of potential prodrugs for beta-lactam antibiotics. Their hydrolysis in aqueous buffers was studied by HPLC and reveal a U-shaped pH rate profile with a pH-independent process extending from ca. pH 2 to ca. pH 10. Th...

journal_title：Bioorganic & medicinal chemistry

authors： Iley J,Barroso H,Moreira R,Lopes F,Calheiros T

更新日期：2000-07-01 00:00:00

abstract：:The synthesis and in vitro vasodilating properties of hybrid compounds in which furoxan (1,2,5-oxadiazole 2-oxide) moieties, endowed with different NO-donor properties, were substituted for the nitroxy function of Nicorandil are reported. The corresponding cyanoguanidine analogues are also considered. This approach ha...

journal_title：Bioorganic & medicinal chemistry

authors： Boschi D,Cena C,Di Stilo A,Fruttero R,Gasco A

更新日期：2000-07-01 00:00:00

abstract：:The metal-interaction of aurine tricarboxylic acid (ATA) and its inhibitory effect on the DNA binding of NFkappaB were studied. Chemical speciation and spectroscopic studies have shown the strong interaction of ATA with metal ions present in the biological systems. EPR, FTIR and electronic spectral studies indicated t...

journal_title：Bioorganic & medicinal chemistry

authors： Sharma RK,Garg BS,Kurosaki H,Goto M,Otsuka M,Yamamoto T,Inoue J

更新日期：2000-07-01 00:00:00