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Volume 10; Issue 11

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Bioorganic & Medicinal Chemistry Letters
Volume 10; Issue 11

Bioorganic & Medicinal Chemistry Letters

Volume 10; Issue 11

1

Synthesis and in vitro antibacterial activity of 3-[N-methyl-N-(3-methyl-1,3-thiazolium-2-yl)amino]methyl cephalosporin derivatives

Sung Hoon Kim, Hyenju Son, Ghilsoo Nam, Dae Yoon Chi, Joong Hyup Kim

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 126 KB

english, 2000

2

Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani

Kelly Chibale, Mark Visser, Vanessa Yardley, Simon L. Croft, Alan H. Fairlamb

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 130 KB

english, 2000

3

Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds

Andrew Spaltenstein, Merrick R Almond, William J Bock, Darryl G Cleary, Eric S Furfine, Richard J Hazen, Wieslaw M Kazmierski, Francesco G Salituro, Roger D Tung, Lois L Wright

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 152 KB

english, 2000

4

Prediction of drug solubility from Monte Carlo simulations

William L. Jorgensen, Erin M. Duffy

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 112 KB

english, 2000

5

Carbacyclic peptide mimetics as VCAM–VLA-4 antagonists

Jefferson Tilley, Gerry Kaplan, Nader Fotouhi, Barry Wolitzky, Karen Rowan

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 141 KB

english, 2000

6

The design and synthesis of potent cyclic peptide VCAM–VLA-4 antagonists incorporating an achiral Asp-Pro mimetic

Nader Fotouhi, Pramod Joshi, David Fry, Charles Cook, Jefferson W Tilley, Gerry Kaplan, Angela Hanglow, Karen Rowan, Virginia Schwinge, Barry Wolitzky

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 164 KB

english, 2000

7

Cyclic thioether peptide mimetics as VCAM–VLA-4 antagonists

Nader Fotouhi, Pramod Joshi, Jefferson W. Tilley, Karen Rowan, Virginia Schwinge, Barry Wolitzky

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 162 KB

english, 2000

8

Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists

Heinrich Rueeger, Pascal Rigollier, Yasuchika Yamaguchi, Tibur Schmidlin, Walter Schilling, Leoluca Criscione, Steven Whitebread, Michele Chiesi, Mary W Walker, Dale Dhanoa, Imadul Islam, Jack Zhang,

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 308 KB

english, 2000

9

β-Casomorphins: substitution of phenylalanine with β-homo phenylalanine increases the μ-type opioid receptor affinity

Luigi Longobardo, Dominique Melck, Rosa Siciliano, Antonello Santini, Vincenzo Di Marzo, Giancarlo Cammarota

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 150 KB

english, 2000

10

9-Benzylpurines with inhibitory activity against Mycobacterium tuberculosis

Anne Kristin Bakkestuen, Lise-Lotte Gundersen, Geir Langli, Fusheng Liu, Jens M.J Nolsøe

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 125 KB

english, 2000

11

Bicyclic nucleoside inhibitors of Varicella-Zoster Virus (VZV): the effect of a terminal halogen substitution in the side-chain

Andrea Brancale, Christopher McGuigan, Graciela Andrei, Robert Snoeck, Erik De Clercq, Jan Balzarini

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 119 KB

english, 2000

12

Mass spectrometry reveals elastase inhibitors from the reactive centre loop of α1-antitrypsin

Penny A Wright, Adam A Rostom, Carol V Robinson, Christopher J Schofield *

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 103 KB

english, 2000

13

Synthesis of glycosylated polyethylenimine with reduced toxicity and high transfecting efficiency

Françoise Leclercq, Catherine Dubertret, Bruno Pitard, Daniel Scherman, Jean Herscovici

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 429 KB

english, 2000

14

Squalamine analogues as potential anti-trypanosomal and anti-leishmanial compounds

Soghra Khabnadideh, Choon Leei Tan, Simon L Croft, Howard Kendrick, Vanessa Yardley, Ian H Gilbert

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 130 KB

english, 2000

15

(+)-4-Phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist

Fabrizio Gasparini, Werner Inderbitzin, Eric Francotte, Gabrielle Lecis, Paul Richert, Zorica Dragic, Rainer Kuhn, Peter J Flor

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 162 KB

english, 2000

16

The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD 170292

N. Bernad, B.G.M. Burgaud, D.C. Horwell, R.A. Lewthwaite, J. Martinez, M.C. Pritchard

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 166 KB

english, 2000

17

Conformationally-restricted ligands for the histamine H1 receptor

Christopher Upton, Richard H. Osborne, Mohammad Jaffar

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 100 KB

english, 2000

18

SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors

Laszlo Revesz, Franco E Di Padova, Thomas Buhl, Roland Feifel, Hermann Gram, Peter Hiestand, Ute Manning, Alfred G Zimmerlin

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 161 KB

english, 2000

19

The synthesis and in vitro cytotoxic studies of novel oxa-spermidine derivatives and homologues

Vladimir A Kuksa, Valentin A Pavlov, Paul Kong Thoo Lin

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 113 KB

english, 2000

20

‘Double-drugs’— A new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker

Hikaru Matsumoto, Tomonori Hamawaki, Hisashi Ota, Tooru Kimura, Toshiyuki Goto, Kouichi Sano, Yoshio Hayashi, Yoshiaki Kiso

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 200 KB

english, 2000

21

Synthesis and structure–activity relationships of quaternary ammonium cephalosporins with 3-pyrazolylpyridinium derivatives

Kwan Young Chang, Sung Hoon Kim, Ghilsoo Nam, Jae Hong Seo, Joong Hyup Kim, Deok-Chan Ha

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 154 KB

english, 2000

22

Cytotoxic halogenoacrylic derivatives of distamycin A

Paolo Cozzi, Italo Beria, Marina Caldarelli, Laura Capolongo, Cristina Geroni, Nicola Mongelli

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 145 KB

english, 2000

23

Cytotoxic α-bromoacrylic derivatives of distamycin analogues modified at the amidino moiety

Paolo Cozzi, Italo Beria, Marina Caldarelli, Cristina Geroni, Nicola Mongelli, Giulia Pennella

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 158 KB

english, 2000

24

The basal SAR of a novel insulin receptor activator

Harold B. Wood Jr., Regina Black, Gino Salituro, Deborah Szalkowski, Zhihua Li, Yan Zhang, David E. Moller, Bei Zhang, A.Brian Jones

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 188 KB

english, 2000

25

Synthesis and evaluation of geldanamycin–testosterone hybrids

Scott D Kuduk, Christina R Harris, Fuzhong F Zheng, Laura Sepp-Lorenzino, Quathek Ouerfelli, Neal Rosen, Samuel J Danishefsky

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 160 KB

english, 2000

26

4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity

James B Thomas, Robert N Atkinson, Richard B Rothman, Jason P Burgess, S.Wayne Mascarella, Christina M Dersch, Heng Xu, F.Ivy Carroll

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 131 KB

english, 2000

27

Nucleotide libraries as a source of biologically relevant chemical diversity: solution-phase synthesis

Wenqiang Zhou, Sathya Upendran, Arlène Roland, Yi Jin, Radhakrishnan P. Iyer

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 170 KB

english, 2000

28

Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. Part 6: Further focus on the contracted C4′-side chain analogues

Kumiko Takeuchi, Todd J. Kohn, Richard W. Harper, Ho-Shen Lin, Donetta S. Gifford-Moore, Michael E. Richett, Daniel J. Sall, Gerry F. Smith, Minsheng Zhang

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 141 KB

english, 2000

29

COBRA-1, A rationally-designed epoxy-THF containing compound with potent tubulin depolymerizing activity as a novel anticancer agent

Shyi-Tai Jan, Chen Mao, Alexei O Vassilev, Christopher S Navara, Fatih M Uckun

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 451 KB

english, 2000

30

Substrate and stereochemical specificity of the organophosphorus acid anhydrolase from Alteromonas sp. JD6.5 toward p-nitrophenyl phosphotriesters

Craig M. Hill, Feiyue Wu, Tu-Chen Cheng, Joseph J. DeFrank, Frank M. Raushel

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 137 KB

english, 2000

31

Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity

Willard Lew, Huiwei Wu, Xiaowu Chen, Bradford J Graves, Paul A Escarpe, Holly L MacArthur, Dirk B Mendel, Choung U Kim

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 336 KB

english, 2000

32

Synthesis and activity studies of conformationally restricted α-ketoamide factor Xa inhibitors

Joseph Cacciola, John M. Fevig, Pieter F.W. Stouten, Richard S. Alexander, Robert M. Knabb, Ruth R. Wexler

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 498 KB

english, 2000

33

Methaqualone derivatives are potent noncompetitive AMPA receptor antagonists

B.L Chenard, F.S Menniti, M.J Pagnozzi, K.D Shenk, F.E Ewing, W.M Welch

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 124 KB

english, 2000

34

Hepatitis C viral IRES inhibition by phenazine and phenazine-like molecules

Wuyi Wang, Patrice Préville, Nicolas Morin, Samir Mounir, Weizhong Cai, M.Arshad Siddiqui

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 152 KB

english, 2000

35

A focused compound library of novel N-(7-indolyl)benzenesulfonamides for the discovery of potent cell cycle inhibitors

Takashi Owa, Tatsuo Okauchi, Kentaro Yoshimatsu, Naoko Hata Sugi, Yoichi Ozawa, Takeshi Nagasu, Nozomu Koyanagi, Tadashi Okabe, Kyosuke Kitoh, Hiroshi Yoshino

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 204 KB

english, 2000

36

Immunomodulatory activity of hexapeptides related to proline rich peptide from colostrum

B Kundu, A Puri, G Singh, R Sahai, L.M Tripathi, V.M.L Srivastava

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 81 KB

english, 2000

37

Total synthesis of pyrrolizidines 223H′, 239K′, 265H′, and 267H′ found in Madagascan frogs (Mantella) and their affinities for nicotinic acetylcholine receptor

Hiroki Takahata, Seiki Takahashi, Nehad Azer, Amira T. Eldefrawi, Mohyee E. Eldefrawi

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 152 KB

english, 2000

38

Facile synthesis of N-Fmoc-serine-S-GlcNAc: a potential molecular probe for the functional study of O-GlcNAc

Yuki Ohnishi, Mie Ichikawa, Yoshitaka Ichikawa

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 149 KB

english, 2000

39

Functionalized nucleoside 5′-triphosphates for in vitro selection of new catalytic ribonucleic acids

Jasenka Matulic-Adamic, Andrew T Daniher, Alexander Karpeisky, Peter Haeberli, David Sweedler, Leonid Beigelman

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 189 KB

english, 2000

40

Discovery of a potent, non-triketone type inhibitor of 4-hydroxyphenylpyruvate dioxygenase

Shean-Woei Lin, Yun-Loung Lin, Tzu-Ching Lin, Ding-Yah Yang

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2000

Langue:

english

Fichier:

PDF, 98 KB

english, 2000