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Publisher: Elsevier

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Volume 13, Number 24, 15 December 2003

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Editorial Board
pp. CO2-CO2(1)

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Author Index
pp. V-X(6)

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Volume Contents
pp. X-V

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Contents List
pp. iii

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Graphical Abstracts
pp. 4251-4264(14)

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Phenolics with PPAR- ligand-Binding activity obtained from licorice (Glycyrrhiza uralensis Roots) and ameliorative effects of glycyrin on genetically diabetic KK-Ay mice
pp. 4267-4272(6)
Authors: Kuroda, M.; Mimaki, Y.; Sashida, Y.; Mae, T.; Kishida, H.; Nishiyama, T.; Tsukagawa, M.; Konishi, E.; Takahashi, K.; Kawada, T.; Nakagawa, K.; Kitahara, M.

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KMI-008, a novel -Secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-State mimic: design and synthesis of substrate-based octapeptides
pp. 4273-4276(4)
Authors: Shuto, D.; Kasai, S.; Kimura, T.; Liu, P.; Hidaka, K.; Hamada, T.; Shibakawa, S.; Hayashi, Y.; Hattori, C.; Szabo, B.; Ishiura, S.; Kiso, Y.

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A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic
pp. 4277-4279(3)
Authors: Hattori, K.; Tabuchi, S.; Okitsu, O.; Taniguchi, K.

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B-Ring unsaturated estrogens: biological evaluation of 17α-Dihydroequilein and novel B-Nor-6-thiaequilenins as tissue selective estrogens
pp. 4281-4284(4)
Authors: Lugar, C.W.; Magee, D.; Adrian, M.D.; Shetler, P.; Bryant, H.U.; Dodge, J.A.

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Non-peptide αv3 antagonists: Identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint
pp. 4285-4288(4)
Authors: Perkins, J.J.; Duong, L.T.; Fernandez-Metzler, C.; Hartman, G.D.; Kimmel, D.B.; Leu, C.; Lynch, J.J.; Prueksaritanont, T.; Rodan, G.A.; Rodan, S.B.; Duggan, M.E.; Meissner, R.S.

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Lysine sulfonamides as novel HIV-Protease inhibitors: optimization of the N-acyl-phenyl spacer
pp. 4289-4292(4)
Authors: Stranix, B.R.; Sauve, G.; Bouzide, A.; Cote, A.; Sevigny, G.; Yelle, J.

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Rational design, synthesis and structure-Activity relationships of a cyclic succinate series of TNF-α converting enzyme inhibitors. Part 1: lead identification
pp. 4293-4297(5)
Authors: Xue C.-B.; He, X.; Roderick, J.; Corbett, R.L.; Duan, J.J.; Liu, R.; Covington, M.B.; Newton, R.C.; Trzaskos, J.M.; Magolda, R.L.; Wexler, R.R.; Decicco, C.P.

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Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-α converting enzyme inhibitors. Part 2: lead optimization
pp. 4299-4304(6)
Authors: Xue C.-B.; He, X.; Roderick, J.; Corbett, R.L.; Duan, J.J.; Liu, R.; Covington, M.B.; Qian, M.; Ribadeneira, M.D.; Vaddi, K.; Christ, D.D.; Newton, R.C.; Trzaskos, J.M.; Magolda, R.L.; Wexler, R.R.; Decicco, C.P.

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3-Iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase
pp. 4309-4312(4)
Authors: Benjahad, A.; Guillemont, J.; Andries, K.; Nguyen, C.H.; Grierson, D.S.

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4-(4-Alkylpiperazin-1-yl)phenyl group: A novel class of basic side chains for selective estrogen receptor modulators
pp. 4317-4320(4)
Authors: Watanabe, N.; Nakagawa, H.; Ikeno, A.; Minato, H.; Kohayakawa, C.; Tsuji, J.

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Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-Based non-hydroxamates
pp. 4321-4326(6)
Authors: Suzuki, T.; Nagano, Y.; Matsuura, A.; Kohara, A.; Ninomiya, S.; Kohda, K.; Miyata, N.

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Synthesis and analgesic activity of hydrochlorides and quaternary ammoniums of epibatidine incorporated with amino acid ester
pp. 4327-4329(3)
Authors: Dong, J.; Wang, X.; Li R.-T.; Zhang, H.; Cheng, T.; Li, C.

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Catechol-Substituted l-Chicoric acid analogues as HIV integrase inhibitors
pp. 4331-4334(4)
Authors: Lee, J.Y.; Yoon, K.J.; Lee, Y.S.

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Design and synthesis of statine-Containing BACE inhibitors
pp. 4335-4339(5)
Authors: Hu, J.; Cwi, C.L.; Smiley, D.L.; Timm, D.; Erickson, J.A.; McGee, J.E.; Yang, H.; Mendel, D.; May, P.C.; Shapiro, M.; McCarthy, J.R.

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-Alanine dipeptides as MC4R agonists
pp. 4341-4344(4)
Authors: Ruel, R.; Herpin, T.F.; Iben, L.; Luo, G.; Martel, A.; Mason, H.; Mattson, G.; Poirier, B.; Ruediger, E.H.; Shi, D.; Thibault, C.; Yu, G.; Antal Zimanyi, I.; Poindexter, G.S.; Macor, J.E.

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New cerebrosides from Euphorbia peplis L.: antimicrobial activity evaluation
pp. 4345-4350(6)
Authors: Cateni, F.; Zilic, J.; Falsone, G.; Scialino, G.; Banfi, E.

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DAPI derivative: A fluorescent DNA dye that Can be covalently attached to biomolecules
pp. 4351-4354(4)
Authors: Li, M.; Wu, R.S.; Tsai, J.S.C.

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Successful shape-Based virtual screening: The discovery of a potent inhibitor of the type I TGF receptor kinase (TRI)
pp. 4355-4359(5)
Authors: Singh, J.; Chuaqui, C.E.; Boriack-Sjodin, P.A.; Lee, W.; Pontz, T.; Corbley, M.J.; Cheung, H.; Arduini, R.M.; Mead, J.N.; Newman, M.N.; Papadatos, J.L.; Bowes, S.; Josiah, S.; Ling, L.E.

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4-Methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the Farnesyltransferase inhibitor ZARNESTRA(TM)
pp. 4361-4364(4)
Authors: Angibaud, P.; Saha, A.K.; Bourdrez, X.; End, D.W.; Freyne, E.; Lezouret, P.; Mannens, G.; Mevellec, L.; Meyer, C.; Pilatte, I.; Poncelet, V.; Roux, B.; Smets, G.; van Dun, J.; Venet, M.; Wouters, W.

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Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors
pp. 4365-4369(5)
Authors: Angibaud, P.; Bourdrez, X.; End, D.W.; Freyne, E.; Janicot, M.; Lezouret, P.; Ligny, Y.; Mannens, G.; Damsch, S.; Mevellec, L.; Meyer, C.; Muller, P.; Pilatte, I.; Poncelet, V.; Roux, B.; Smets, G.; van Dun, J.; van Remoortere, P.; Venet, M.; Wouters, W.

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Synthesis and antiviral evaluation of 3-hydroxy-2-methylpyridin-4-one dideoxynucleoside derivatives
pp. 4371-4374(4)
Authors: Barral, K.; Hider, R.C.; Balzarini, J.; Neyts, J.; de Clercq, E.; Camplo, M.

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3D-QSAR Studies on natural acetylcholinesterase inhibitors of Sarcococca saligna by comparative molecular field analysis (CoMFA)
pp. 4375-4380(6)
Authors: Zaheer-ul-Haq; Wellenzohn, B.; Tonmunphean, S.; Khalid, A.; Choudhary, M.I.; Rode, B.M.

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Heterocyclic aminopyrrolidine derivatives as melatoninergic agents
pp. 4381-4384(4)
Authors: Sun, L.; Chen, J.; Mattson, R.J.; Epperson, J.R.; Deskus, J.A.; Li, W.; Takaki, K.; Hodges, D.B.; Iben, L.; Mahle, C.D.; Ortiz, A.; Molstad, D.; Ryan, E.; Yeleswaram, K.; Xu, C.; Luo, G.

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Novel 3,4-Dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a
pp. 4385-4388(4)
Authors: Rosauer, K.G.; Ogawa, A.K.; Willoughby, C.A.; Ellsworth, K.P.; Geissler, W.M.; Myers, R.W.; Deng, Q.; Chapman, K.T.; Harris, G.; Moller, D.E.

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Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects
pp. 4389-4393(5)
Authors: Suh Y.-G.; Lee, Y.; Min, K.; Park, O.; Seung, H.; Kim, H.; Park, H.; Choi, J.; Lee, J.; Kang, S.; Oh, U.; Koo, J.; Joo, Y.; Kim, S.; Kim, J.K.; Park, Y.

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Antibacterial and antiproliferative activity of cationic fullerene derivatives
pp. 4395-4397(3)
Authors: Mashino, T.; Nishikawa, D.; Takahashi, K.; Usui, N.; Yamori, T.; Seki, M.; Endo, T.; Mochizuki, M.

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Synthesis and biological activity of novel 1-Methylcarbapenems with oxyiminopyrrolidinylamide moiety
pp. 4399-4403(5)
Authors: Lee, J.H.; Lee, K.S.; Kang, Y.K.; Yoo, K.H.; Shin, K.J.; Kim, D.C.; Kong, J.Y.; Lee, Y.; Lee, S.J.; Kim, D.J.

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Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity
pp. 4405-4408(4)
Authors: Minutolo, F.; Bertini, S.; Betti, L.; Danesi, R.; Gervasi, G.; Giannaccini, G.; Papi, C.; Placanica, G.; Barontini, S.; Rapposelli, S.; Macchia, M.

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Design, synthesis and biological activity of novel dimethyl-{2-[6-substituted-indol-1-yl]-ethyl}-amine as potent, selective, and orally-Bioavailable 5-HT1D agonists
pp. 4409-4413(5)
Authors: Isaac, M.; Slassi, M.; Xin, T.; Arora, J.; O'Brien, A.; Edwards, L.; MacLean, N.; Wilson, J.; Demschyshyn, L.; Labrie, P.; Naismith, A.; Maddaford, S.; Papac, D.; Harrison, S.; Wang, H.; Draper, S.; Tehim, A.

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Synthesis of non-immunosuppressive cyclophilin-Binding cyclosporin A derivatives as potential anti-HIV-1 drugs
pp. 4415-4419(5)
Authors: Evers, M.; Barriere, J.; Bashiardes, G.; Bousseau, A.; Carry, J.; Dereu, N.; Filoche, B.; Henin, Y.; Sable, S.; Vuilhorgne, M.; Mignani, S.

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Binding of -Carbolines at 5-HT2 serotonin receptors
pp. 4421-4425(5)
Authors: Grella, B.; Teitler, M.; Smith, C.; Herrick-Davis, K.; Glennon, R.A.

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1-Aryl-6,7-methylenedioxy-3H-quinazolin-4-ones as anticonvulsant agents
pp. 4427-4430(4)
Authors: Zappala, M.; Grasso, S.; Micale, N.; Zuccala, G.; Menniti, F.S.; Ferreri, G.; de Sarro, G.; de Micheli, C.

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Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype
pp. 4431-4435(5)
Authors: Ujjainwalla, F.; Warner, D.; Walsh, T.F.; Wyvratt, M.J.; Zhou, C.; Yang, L.; Kalyani, R.N.; MacNeil, T.; van der Ploeg, L.H.T.; Rosenblum, C.I.; Tang, R.; Vongs, A.; Weinberg, D.H.; Goulet, M.T.

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Synthesis and Anti-HIV properties of new water-soluble bis-functionalized[60]fullerene derivatives
pp. 4437-4440(4)
Authors: Bosi, S.; Da Ros, T.; Spalluto, G.; Balzarini, J.; Prato, M.

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O-N Intramolecular acyl migration strategy in water-soluble prodrugs of taxoids
pp. 4441-4444(4)
Authors: Skwarczynski, M.; Sohma, Y.; Kimura, M.; Hayashi, Y.; Kimura, T.; Kiso, Y.

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Potent anti-metastatic activity of dimeric sesquiterpene thioalkaloids from the rhizome of Nuphar pumilum
pp. 4445-4449(5)
Authors: Matsuda, H.; Morikawa, T.; Oda, M.; Asao, Y.; Yoshikawa, M.

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Synthesis of new 3-Arylisoquinolinamines: effect on topoisomerase I inhibition and cytotoxicity
pp. 4451-4454(4)
Authors: Cho W.-J.; Min, S.Y.; Le, T.N.; Kim, T.S.

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Synthesis and evaluation of optically pure dioxolanes as inhibitors of hepatitis C virus RNA replication
pp. 4455-4458(4)
Authors: Bera, S.; Malik, L.; Bhat, B.; Carroll, S.S.; MacCoss, M.; Olsen, D.B.; Tomassini, J.E.; Eldrup, A.B.

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trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines: A novel class of -Selective opioid antagonists
pp. 4459-4462(4)
Authors: Le Bourdonnec, B.; Belanger, S.; Cassel, J.A.; Stabley, G.J.; DeHaven, R.N.; Dolle, R.E.

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Ureas of 5-aminopyrazole and 2-aminothiazole inhibit growth of gram-positive bacteria
pp. 4463-4466(4)
Authors: Kane, J.L.; Hirth, B.H.; Liang, B.; Gourlie, B.B.; Nahill, S.; Barsomian, G.

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Tripeptidyl-peptidase II (TPP II) inhibitory activity of (S)-2,3-dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a systematic SAR evaluation. Part 2
pp. 4467-4471(5)
Authors: Breslin, H.J.; Miskowski, T.A.; Kukla, M.J.; de Winter, H.L.; Somers, M.V.F.; Roevens, P.W.M.; Kavash, R.W.

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1,3-Dihydrobenzo[c]furan nucleoside analogues: additional studies of the thymine derivative
pp. 4473-4475(3)
Authors: Egron, D.; Perigaud, C.; Gosselin, G.; Aubertin, A.; Faraj, A.; Selouane, M.; Postel, D.; Len, C.

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Duloxetine (Cymbalta(TM)), a dual inhibitor of serotonin and norepinephrine reuptake
pp. 4477-4480(4)
Authors: Bymaster, F.P.; Beedle, E.E.; Findlay, J.; Gallagher, P.T.; Krushinski, J.H.; Mitchell, S.; Robertson, D.W.; Thompson, D.C.; Wallace, L.; Wong, D.T.

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Conicamin, a novel histamine antagonist from the mediterranean tunicate Aplidium conicum
pp. 4481-4483(3)
Authors: Aiello, A.; Borrelli, F.; Capasso, R.; Fattorusso, E.; Luciano, P.; Menna, M.

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Exploration of the bicyclo[3.3.1]nonane system as a template for the development of new ligands for the estrogen receptor
pp. 4485-4488(4)
Authors: Muthyala, R.S.; Carlson, K.E.; Katzenellenbogen, J.A.

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Novel mechanism of inhibiting -Lactamases by sulfonylation using -Sultams
pp. 4489-4492(4)
Authors: Page, M.I.; Hinchliffe, P.S.; Wood, J.M.; Harding, L.P.; Laws, A.P.

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Microbial transformation of baccatin VI and 1-Hydroxy baccatin I by aspergillus niger
pp. 4493-4496(4)
Authors: Shen Y.-C.; Lo, K.; Lin, C.; Chakraborty, R.

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N-Acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist
pp. 4497-4499(3)
Authors: Hirose, M.; Egashira, S.; Goto, Y.; Hashihayata, T.; Ohtake, N.; Iwaasa, H.; Hata, M.; Fukami, T.; Kanatani, A.; Yamada, K.

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Structure-activity relationships of indole cytosolic phospholipase A2α inhibitors: substrate mimetics
pp. 4501-4504(4)
Authors: McKew, J.C.; Lovering, F.; Clark, J.D.; Bemis, J.; Xiang, Y.; Shen, M.; Zhang, W.; Alvarez, J.C.; Joseph-McCarthy, D.

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Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence
pp. 4505-4509(5)
Authors: Holder, J.R.; Bauzo, R.M.; Xiang, Z.; Scott, J.; Haskell-Luevano, C.

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Novel bicyclic furanopyrimidines with dual anti-VZV and -HCMV activity
pp. 4511-4513(3)
Authors: McGuigan, C.; Brancale, A.; Andrei, G.; Snoeck, R.; de Clercq, E.; Balzarini, J.

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Corrigendum to ''Bone-Targeted Src Kinase Inhibitors: Novel Pyrrolo- and Pyrazolopyrimidine Analogues''[Bioorg. Med. Chem. Lett. 13 (2003) 3063]
pp. 4519-4519(1)
Authors: Sundaramoorthi, R.; Shakespeare, W.C.; Keenan, T.P.; Metcalf, C.A.; Wang, Y.; Mani, U.; Merry, T.; Liu, S.; Bohacek, R.S.; Narula, S.S.; Dalgarno, D.C.; van Schravendijk, M.R.; Violette, S.M.; Liou, S.; Adams, S.; Ram, M.K.; Keats, J.A.; Weigle, M.; Sawyer, T.K.

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Erratum to ''Aryloxazolidinediones: Identification of Potent Orally Active PPAR Dual α/ Agonists'' - [Bioorg. Med. Chem. Lett. 13 (2003) 3541]
pp. 4521-4521(1)
Authors: Desai, R.C.; Gratale, D.F.; Han, W.; Koyama, H.; Metzger, E.; Lombardo, V.K.; MacNaul, K.L.; Doebber, T.W.; Berger, J.P.; Leung, K.; Franklin, R.; Moller, D.E.; Heck, J.V.; Sahoo, S.P.

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