Frontiers in Medicinal Chemistry

Volume 2

by

Atta-ur-Rahman , Allen B. Reitz

DOI: 10.2174/97816080520591050201
eISBN: 978-1-60805-205-9, 2005
ISBN: 978-1-60805-673-6
ISSN: 1567-2042

  
  




Frontiers in Medicinal Chemistry is a book series devoted to the review of area...[view complete introduction]
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Table of Contents

Editorial , Pp. iv- (1)

Allen B. Reitz, Atta-ur-Rahman, Cheryl P. Kordik and M. Iqbal Choudhary

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Contributors , Pp. viii-xiii (6)

Allen B. Reitz, Atta-ur-Rahman, Cheryl P. Kordik and M. Iqbal Choudhary

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Novel Inhibitors of HIV Integrase: The Discovery of Potential Anti-HIV Therapeutic Agents , Pp. 3-20 (18)

Vasu Nair

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Macrolide Antibiotics: Binding Site, Mechanism of Action, Resistance , Pp. 21-35 (15)

Marne Gaynor and Alexander S. Mankin

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Potential New Targets for Antithrombotic Therapy , Pp. 37-48 (12)

Andras Gruber and Stephen R. Hanson

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Potent and Selective A2A Adenosine Receptor Antagonists: Recent Improvement , Pp. 49-62 (14)

Barbara Cacciari, Giorgia Pastorin, Stefano Moro and Giampiero Spalluto

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Updating the Dual Role of Brain Nitric Oxide in Neurodegeneration/Neuroprotection: Understanding Molecular Mechanisms to Devise Drug Approaches , Pp. 63-109 (47)

Antonio Contestabile, Barbara Monti, Andrea Contestabile and Elisabetta Ciani

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Effect of Genetic Background on Ionotropic Glutamate Receptor and Neurotrophin Biology: Synaptic Connectivity and Function in Neurological Disease , Pp. 111-132 (22)

Gregory N. Barnes and John T. Slevin

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Medical Marijuana in CNS Disorders , Pp. 133-159 (27)

Alison J. Drysdale and Bettina Platt

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Obesity and Diabetes Gene Discovery Approaches , Pp. 161-182 (22)

Ken Walder, David Segal, Jeremy Jowett, John Blangero and Greg R. Collier

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Understanding the Molecular Mechanism of Action of Estrogen Receptor Modulators , Pp. 183-231 (49)

Mary J. Meegan and David G. Lloyd

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Recent Advances in Peroxisome Proliferator- Activated Receptor Science , Pp. 233-251 (19)

Barry G. Shearer and William J. Hoekstra

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Recent Developments in the Synthesis and Evaluation of Glucose Analog Inhibitors of Glycogen Phosphorylases as Potential Antidiabetic Agents , Pp. 253-272 (20)

Laszlo Somsak, Veronika Nagy, Zsuzsa Hadady, Nora Felfoldi, Tibor Docsa and Pal Gergely

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Regulation by Nicotine of Food Intake and Body Weight: Implications for Obesity Treatment , Pp. 273-297 (25)

Ming D. Li, Justin K. Kane and Ozlen Konu

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Histone Deacetylase Inhibitors: From Chromatin Remodelling to Experimental Cancer Therapeutics , Pp. 299-315 (17)

Janine Arts, Stefanie de Schepper and Kristof Van Emelen

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Radiogenetic Therapy Using Radiation-Responsive Gene Promoters , Pp. 317-330 (14)

Brian Marples, Olga Greco, Michael C. Joiner and Simon D. Scott

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Inhibitors of Farnesyltransferase and Geranylgeranyltransferase-I for Antitumor Therapy: Substrate-Based Design, Conformational Constraint and Biological Activity , Pp. 331-355 (25)

Christopher J. Dinsmore and Ian M. Bell

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Enediyne Natural Products: Biosynthesis and Prospect Towards Engineering Novel Antitumor Agents , Pp. 357-369 (13)

Ben Shen, Wen Liu and Koichi Nonaka

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Heparin Derivatives and Semisynthetic Biotechnological Heparins as Angiogenesis Inhibitors , Pp. 371-391 (21)

Marco Presta, Daria Leali, Helena Stabile, Roberto Ronca, Maura Camozzi, Emanuela Moroni, Stefania Nicoli, Sandra Liekens and Marco

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VIP and Drug Design 2004 , Pp. 393-415 (23)

Illana Gozes and Sharon Furman

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Chemical Genomics-Based Target Mining and Validation of Biologically Active Small Molecules , Pp. 417-430 (14)

Ho Jeong Kwon

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Ethnobotany and Natural Products: The Search for New Molecules, New Treatments of Old Diseases or a Better Understanding of Indigenous Cultures? , Pp. 431-450 (20)

Michael Heinrich

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Natural Killer T Cells as Targets for Therapeutic Intervention in Autoimmune Diseases , Pp. 451-484 (34)

Michael T. Wilson and Luc Van Kaer

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Combinatorial Synthesis of Small Molecule Libraries by Microwave Technology , Pp. 485-510 (26)

Chung-Ming Sun

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Pharmacophore Discovery - Lessons Learned , Pp. 511-532 (22)

John H. van Drie

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Drug Discovery Today , Pp. 533-543 (11)

Oliver Schwardt, Brian Cutting, Hartmuth Kolb and Beat Ernst

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Theoretical Property Predictions , Pp. 545-570 (26)

David J. Livingston

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Prediction of Drug Metabolism: The Case of Cytochrome P450 2D6 , Pp. 571-586 (16)

Nico P.E. Vermeulen

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Subject Index to Volume 2 , Pp. 587-606 (20)

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List of Contributors

Co-Editor(s):
Atta-ur-Rahman
H.E.J. Research Institute of Chemistry, University of Karachi
Karachi, 75270
Pakistan


Allen B. Reitz
Johnson & Johnson Pharmaceutical Research and Development, Spring House
Pennsylvania , 19477
USA




Associate Editor(s):
M. Iqbal Choudhary
H.E.J. Research Institute of Chemistry, University of Karachi
Karachi, 75270
Pakistan


Cheryl P. Kordik
Johnson & Johnson Pharmaceutical Research and Development, Spring House
Pennsylvania , 19477
USA




Editorial Advisory Board:
P.R. Bernstein
University of Delaware
Newark
DE
USA


C. Bor-Luen
National Taiwan University, Taipei
Taiwan
R.O.C.


R. Efremov
M.M. Shemyakin & Yu.A. Ovchinnikov Institute of Bioorganic Chemistry
Moscow
Russia


C. Garcia-Echeverria
Sanofi-Aventis
Paris
France


D. Hadjipavlou-Litina
Arristotle Universith of Thessaloniki
Thessaloniki
Greece


D. Heymann
University of Nantes
Nantes
France


D.A. Jans
Nuclear Signaling Laboratory, Monash University
Australia


G.B. Mahady
University of Illinois at Chicago
Chicago
IL
USA


B. Malawska
Jagiellonian University Collegium Medicum
Kraków
Poland


C. Philippe
Sciences and Technologies University of Lille
Lille
France




Contributor(s):
Janine Arts
Oncology Discovery Research, Johnson & Johnson Pharmaceutical Research and Development
Turnhoutseweg 30
Beerse, 2340
Belgium


Gregory N. Barnes
Developmental Neurobiology Laboratory, Department of Neurology
L441, Wing D, KY Clinic, 704 South Limestone
Lexington
KY , 40536
USA


Ian M. Bell
Department of Medicinal Chemistry
Merck Research Laboratories
West Point
PA , 19486
USA


John Blangero
Department of Genetics
Southwest Foundation for Biomedical Research
San Antonio, 78245
USA


Barbara Cacciari
Dipartimento di Scienze Farmaceutiche
Università di Ferrara
Via Fossato di Mortasa 17/19
Ferrara, I-44100
Italy


Maura Camozzi
Unit of General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology
School of Medicine, University of Brescia
Brescia, 25123
Italy


Elisabetta Ciani
Department of Biology and Department of Human and General Physiology
University of Bologna, Via Selmi 3
Bologna, 40126
Italy


Greg R. Collier
Metabolic Research Unit
School of Health Sciences, Deakin University
ChemGenex Pharmaceuticals
Geelong, VIC 3217
Australia


Antonio Contestabil
Department of Biology and Department of Human and General Physiology
University of Bologna
Via Selmi 3
Bologna, 40126
Italy


Andrea Contestabile
Department of Biology and Department of Human and General Physiology
University of Bologna
Via Selmi 3
Bologna, 40126
Italy


Brian Cutting
Institute of Molecular Pharmacy, Pharmacenter
University of Basel, Klingelbergstrasse 50
Basel
CH, 4056
Switzerland


Christopher J. Dinsmore
Department of Medicinal Chemistry
Merck Research Laboratories
West Point
PA , 19486
USA


Tibor Docsa
Signalling and Apoptosis Research Group of the Hungarian Academy of Sciences
Research Center for Molecular Medicine, Medical and Health Science Center
University of Debrecen, Bem tér 18/B
Debrecen, H-4026
Hungary


John H. van Drie
Vertex Pharmaceuticals
130 Waverly St.
Cambridge
MA , 02139
USA


Alison J. Drysdale
Department of Biomedical Sciences
Institute of Medical Sciences
Foresterhill, Aberdeen
Scotland, AB25 2ZD
UK


Kristof Van Emelen
Department of Medicinal Chemistry
Johnson & Johnson Pharmaceutical Research and Development
Turnhoutseweg 30
Beerse, 2340
Belgium


Beat Ernst
Institute of Molecular Pharmacy, Pharmacenter
University of Basel, Klingelbergstrasse 50
Bem tér 18/B
Basel
CH, 4056
Switzerland


Nóra Felföldi
Department of Organic Chemistry, Faculty of Science
University of Debrecen
Egyetem tér 1, POB 20
Debrecen
CH, H-4010
Hungary


Sharon Furman
Department of Clinical Biochemistry, Sackler Faculty of Medicine
Tel Aviv University
Tel Aviv, 69978
Israel


Marne Gaynor
Center for Pharmaceutical Biotechnology - M/C 870
University of Illinois
900 S. Ashland Ave.
Chicago
IL , 60607
USA


Pál Gergely
Department of Medical Chemistry
Research Center for Molecular Medicine, Medical and Health Science Center
University of Debrecen, Bem tér 18/B
Debrecen, H-4026
Hungary


Illana Gozes
Department of Clinical Biochemistry
Sackler Faculty of Medicine, Tel Aviv University
Tel Aviv, 69978
Israel


Olga Greco
Department of Radiation Oncology
Karmanos Cancer Institute and Wayne State University
Hudson Webber Building, Room 824, 4100 John R
Detroit
MI , 48201-2013
USA


Andras Gruber
Department of Biomedical Engineering
OGI School of Science and Engineering, Oregon Health and Science University
20000 N.W. Walker Road, Beaverton, Portland
Oregon, 97006-8921
USA


Zsuzsa Hadady
Department of Organic Chemistry
Faculty of Science, University of Debrecen
Egyetem tér 1, POB 20
Debrecen, H-4010
Hungary


Stephen R. Hanson
Department of Biomedical Engineering
OGI School of Science and Engineering, Oregon Health and Science University
20000 N.W. Walker Road, Beaverton, Portland
Oregon, 97006-8921
USA


Michael Heinrich
Centre for Pharmacognosy and Phytotherapy
The School of Pharmacy, University of London
29-39 Brunswick Square
London, WC1N 1AX
UK


William J. Hoekstra
GlaxoSmithKline, Five Moore Drive
Research Triangle Park
London
NC , 27709-3398
USA


Michael C. Joiner
Department of Radiation Oncology
Karmanos Cancer Institute and Wayne State University
Hudson Webber Building, Room 824, 4100 John R
Detroit
MI , 48201-2013
USA


Jeremy Jowett
International Diabetes Institute
Caulfield, VIC 3062
Australia


Justin K. Kane
Program in Genomics and Bioinformatics on Drug Addiction, Department of Psychiatry
University of Texas Health Science Center
San Antonio
TX , 78229
USA


Luc Van Kaer
Department of Microbiology and Immunology
Vanderbilt University School of Medicine
Tennessee , 37232-0295
USA


Hartmuth Kolb
Department of Chemistry
The Scripps Research Institute
10550 North Torrey Pines Road
La Jolla
CA , 92037
USA


Ozlen Konu
Program in Genomics and Bioinformatics on Drug Addiction
Department of Psychiatry, University of Texas Health Science Center
San Antonio
TX , 78229
USA


Ho Jeong Kwon
Chemical Genomics National Research Laboratory, Department of Bioscience and Biotechnology
Institute of Bioscience, Sejong University
98 Kunja-dong, Kwangjin-gu
Seoul , 143-747
Korea


Daria Leali
Unit of General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology
School of Medicine, University of Brescia
Brescia, 25123
Italy


Ming D. Li
Program in Genomics and Bioinformatics on Drug Addiction, Department of Psychiatry
University of Texas Health Science Center
San Antonio
TX , 78229
USA


Sandra Liekens
Present address: Rega Institute for Medical Research
Katholieke Universiteit Leuven
Leuven, B-3000
Belgium


Wen Liu
Division of Pharmaceutical Sciences
University of Wisconsin, Madison
Seoul
WI , 53705
USA


David J. Livingstone
ChemQuest, Delamere House, 1 Royal Crescent, Sandown, Isle of Wight, PO36 8LZ
Centre for Molecular design, University of Portsmouth
Portsmouth
Hants, PO1 2DY
UK


David G. Lloyd
Department of Biochemistry
Trinity College Dublin
Ireland


Alexander S. Mankin
Center for Pharmaceutical Biotechnology – M/C 870
University of Illinois
900 S. Ashland Ave.
Chicago
IL , 60607
USA


Brian Marples
Department of Radiation Oncology
Karmanos Cancer Institute and Wayne State University
Hudson Webber Building, Room 824, 4100 John R
Detroit
MI, 48201-2013
USA


Mary J. Meegan
School of Pharmacy, Trinity College Dublin
Ireland


Barbara Monti
Department of Biology and Department of Human and General Physiology
University of Bologna, Via Selmi 3
Bologna, 40126
Italy


Stefano Moro
Molecular Modeling Section, Dipartimento di Scienze Farmaceutiche
Università di Padova
Via Marzolo 5
Padova, I-35131
Italy


Emanuela Moroni
Unit of General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology
School of Medicine, University of Brescia
Brescia, 25123
Italy


Veronika Nagy
Department of Organic Chemistry
Faculty of Science, University of Debrecen
Egyetem tér 1, POB 20
Debrecen, H-4010
Hungary


Vasu Nair
Department of Pharmaceutical and Biomedical Sciences
Center for Drug Discovery, The University of Georgia
Athens
GA , 30606
USA


Stefania Nicoli
Unit of General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology
School of Medicine, University of Brescia
Brescia, 25123
Italy


Koichi Nonaka
Division of Pharmaceutical Sciences
University of Wisconsin
Madison
WI , 53705
USA


Giorgia Pastorin
Dipartimento di Scienze Farmaceutiche
Università di Trieste, Piazzale Europa 1
Trieste, I-34127
Italy


Bettina Platt
Department of Biomedical Sciences
Institute of Medical Sciences
Foresterhill, Aberdeen
Scotland, AB25 2ZD
UK


Marco Presta
Unit of General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology
School of Medicine, University of Brescia
Brescia, 25123
Italy


Roberto Ronca
Unit of General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology
School of Medicine, University of Brescia
Brescia, 25123
Italy


Marco Rusnati
Unit of General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology
School of Medicine, University of Brescia
Brescia, 25123
Italy


Stefanie de Schepper
Oncology Discovery Research
Johnson & Johnson Pharmaceutical Research and Development
Turnhoutseweg 30
Beerse, 2340
Belgium


Oliver Schwardt
Institute of Molecular Pharmacy, Pharmacenter
University of Basel
Klingelbergstrasse 50
Basel
CH, 4056
Switzerland


Simon D. Scott
Department of Radiation Oncology
Karmanos Cancer Institute and Wayne State University
Hudson Webber Building, Room 824, 4100 John R
Detroit
MI , 48201-2013
USA


David Segal
Metabolic Research Unit
School of Health Sciences, Deakin University
Pigdons Road
Waurn Ponds, VIC 3217
Australia


Barry G. Shearer
GlaxoSmithKline
Five Moore Drive, Research Triangle Park
Waurn Ponds
NC , 27709-3398
USA


Ben Shen
Division of Pharmaceutical Sciences and Department of Chemistry
University of Wisconsin
Madison
WI , 53705
USA


John T. Slevin
Developmental Neurobiology Laboratory, Department of Neurology
L441, Wing D, KY Clinic, 704 South Limestone
Lexington
KY , 40536
USA


László Somsák
Department of Organic Chemistry
Faculty of Science, University of Debrecen
Egyetem tér 1, POB 20
Debrecen, H-4010
Hungary


Giampiero Spalluto
Dipartimento di Scienze Farmaceutiche
Università di Trieste
Piazzale Europa 1
Trieste, I-34127
Italy


Helena Stabile
Unit of General Pathology and Immunology, Department of Biomedical Sciences and Biotechnology
School of Medicine, University of Brescia
Brescia, 25123
Italy


Chung-Ming Sun
Laboratory of Combinatorial Drug Discovery
National Dong Hwa University, Shou-Feng
Hualien , 974
Taiwan


Nico P.E. Vermeulen
LACDR - Section of Molecular Toxicology, Department of Chemistry and Pharmacochemistry
Vrije Universiteit
De Boelelaan 1083, 1081 HV
Amsterdam
The Netherlands


Ken Walder
Metabolic Research Unit
School of Health Sciences, Deakin University
Pigdons Road, VIC
Waurn Ponds, 3217
Australia


Michael T. Wilson
Department of Microbiology and Immunology
Vanderbilt University School of Medicine
Rudolph Light Hall, Room 811, Nashville
Tennessee , 37232-0295
USA




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