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COMMUNICATIONS TO THE EDITOR
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3919-3922
| Syntheses of trans-5- Oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-Oxo-hexahydro-furo[3,2-b]pyrroles (Pyrrolidine trans-Lactams and trans-Lactones): New Pharmacophores for Elastase Inhibition
Simon J. F. Macdonald,
David J. Belton,
Doreen M. Buckley,
Julie E. Spooner,
Michael S. Anson,
Lee A. Harrison,
Keith Mills,
Richard J. Upton,
Michael D. Dowle,
Robin A. Smith,
Christopher R. Molloy, and
Catherine Risley
[Full Article -
PDF] |
EXPEDITED ARTICLES
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3923-3927
| Structure-Based Design of Cathepsin K Inhibitors Containing a Benzyloxy-Substituted Benzoyl Peptidomimetic
Scott K. Thompson,
Ward W. Smith,
Baoguang Zhao,
Stacie M. Halbert,
Thaddeus A. Tomaszek,
David G. Tew,
Mark A. Levy,
Cheryl A. Janson,
Karla J. D'Alessio,
Michael S. McQueney,
Jeff Kurdyla,
Christopher S. Jones,
Renee L. DesJarlais,
Sherin S. Abdel-Meguid, and
Daniel F. Veber
[Full Article -
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ARTICLES
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3928-3939
| Investigations of Neurotrophic Inhibitors of FK506 Binding Protein via Monte Carlo Simulations
Michelle L. Lamb and
William L. Jorgensen
[Full Article -
PDF] |
3940-3947
| N-[ -(Tetralin-1-yl)alkyl] Derivatives of 3,3-Dimethylpiperidine Are Highly Potent and Selective  1 or 2 Ligands
Francesco Berardi,
Sergio Santoro,
Roberto Perrone,
Vincenzo Tortorella,
Stefano Govoni, and
Laura Lucchi
[Full Article -
PDF] |
3948-3960
| Geometrically and Conformationally Restrained Cinnamoyl Compounds as Inhibitors of HIV-1 Integrase: Synthesis, Biological Evaluation, and Molecular Modeling
Marino Artico,
Roberto Di Santo,
Roberta Costi,
Ettore Novellino,
Giovanni Greco,
Silvio Massa,
Enzo Tramontano,
Maria E. Marongiu,
Antonella De Montis, and
Paolo La Colla
[Full Article -
PDF] |
3961-3971
| Structure-Based Design of  -Lactamase Inhibitors. 1. Synthesis and Evaluation of Bridged Monobactams
Ingrid Heinze-Krauss,
Peter Angehrn,
Robert L. Charnas,
Klaus Gubernator,
Eva-Maria Gutknecht,
Christian Hubschwerlen,
Malgosia Kania,
Christian Oefner,
Malcolm G. P. Page,
Satoshi Sogabe,
Jean-Luc Specklin, and
Fritz Winkler
[Full Article -
PDF] |
3972-3975
| Structure-Based Design of -Lactamase Inhibitors. 2. Synthesis and Evaluation of Bridged Sulfactams and Oxamazins
Christian Hubschwerlen,
Peter Angehrn,
Klaus Gubernator,
Malcolm G. P. Page, and
Jean-Luc Specklin
[Full Article -
PDF] |
3976-3986
| Acetylcholinesterase Inhibitors: Synthesis and Structure-Activity Relationships of -[N-Methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl Derivatives
Angela Rampa,
Alessandra Bisi,
Piero Valenti,
Maurizio Recanatini,
Andrea Cavalli,
Vincenza Andrisano,
Vanni Cavrini,
Lorena Fin,
Alessandro Buriani, and
Pietro Giusti
[Full Article -
PDF] |
3987-3993
| A Novel Class of Adenosine A3 Receptor Ligands. 1. 3-(2-Pyridinyl)isoquinoline Derivatives
Jacqueline E. van Muijlwijk-Koezen,
Henk Timmerman,
Regina Link,
Henk van der Goot, and
Adriaan P. IJzerman
[Full Article -
PDF] |
3994-4000
| A Novel Class of Adenosine A3 Receptor Ligands. 2. Structure Affinity Profile of a Series of Isoquinoline and Quinazoline Compounds
Jacqueline E. van Muijlwijk-Koezen,
Henk Timmerman,
Regina Link,
Henk van der Goot, and
Adriaan P. IJzerman
[Full Article -
PDF] |
4001-4011
| Substituted 4-Acylpyrazoles and 4-Acylpyrazolones: Synthesis and Multidrug Resistance-Modulating Activity
Peter Chiba,
Wolfgang Holzer,
Marion Landau,
Gerhard Bechmann,
Karin Lorenz,
Brigitte Plagens,
Manuela Hitzler,
Elisabeth Richter, and
Gerhard Ecker
[Full Article -
PDF] |
4012-4020
| 4-(-Arylvinyl)-3-(-arylvinylketo)-1-ethyl-4-piperidinols and Related Compounds: A Novel Class of Cytotoxic and Anticancer Agents
Jonathan R. Dimmock,
Sarvesh C. Vashishtha,
J. Wilson Quail,
Uma Pugazhenthi,
Zbigniew Zimpel,
Athena M. Sudom,
Theresa M. Allen,
Grace Y. Kao,
Jan Balzarini, and
Erik De Clercq
[Full Article -
PDF] |
4021-4035
| Design, Synthesis, and Biological Activities of New Thieno[3,2-d]pyrimidines as Selective Type 4 Phosphodiesterase Inhibitors
María I. Crespo,
Lluís Pagès,
Armando Vega,
Victor Segarra,
Manel López,
Teresa Doménech,
Montserrat Miralpeix,
Jordi Beleta,
Hamish Ryder, and
José M. Palacios
[Full Article - PDF] |
4036-4052
| New Platelet Fibrinogen Receptor Glycoprotein IIb-IIIa Antagonists: Orally Active Series of N-Alkylated Amidines with a 6,6-Bicyclic Template
Kunio Okumura,
Toshiyuki Shimazaki,
Yoji Aoki, and
Hiroyuki Yamashita
, Eishi Tanaka and
Shinichi Banba
, Kouhei Yazawa,
Kenji Kibayashi, and
Hitoshi Banno
[Full Article - PDF] |
4053-4061
| A Novel Class of Orally Active Non-Peptide Bradykinin B2 Receptor Antagonists. 2. Overcoming the Species Difference between Guinea Pig and Man
Yoshito Abe,
Hiroshi Kayakiri,
Shigeki Satoh,
Takayuki Inoue,
Yuki Sawada,
Noriaki Inamura,
Masayuki Asano,
Chie Hatori,
Hiroe Sawai,
Teruo Oku, and
Hirokazu Tanaka
[Full Article - PDF] |
4062-4079
| A Novel Class of Orally Active Non-Peptide Bradykinin B2 Receptor Antagonists. 3. Discovering Bioisosteres of the Imidazo[1,2-a]pyridine Moiety
Yoshito Abe,
Hiroshi Kayakiri,
Shigeki Satoh,
Takayuki Inoue,
Yuki Sawada,
Noriaki Inamura,
Masayuki Asano,
Ichiro Aramori,
Chie Hatori,
Hiroe Sawai,
Teruo Oku, and
Hirokazu Tanaka
[Full Article - PDF] |
4080-4100
| Synthesis and Antibacterial Activity of Ketolides (6-O-Methyl-3-oxoerythromycin Derivatives): A New Class of Antibacterials Highly Potent Against Macrolide-Resistant and -Susceptible Respiratory Pathogens
Constantin Agouridas,
Alexis Denis,
Jean-Michel Auger,
Yannick Benedetti,
Alain Bonnefoy,
François Bretin,
Jean-François Chantot,
Arlette Dussarat,
Claude Fromentin,
Solange Gouin D'Ambrières,
Sylvette Lachaud,
Patrick Laurin,
Odile Le Martret,
Véronique Loyau, and
Nicole Tessot
[Full Article - PDF] |
4101-4108
| Synthesis and Antimalarial Activities of Fluoroalkyl Derivatives of Dihydroartemisinin
Truong Thi Thanh Nga,
Céline Ménage,
Jean-Pierre Bégué,
Danièle Bonnet-Delpon, and
Jean-Charles Gantier
, Bruno Pradines and
Jean-Claude Doury
, Truong Dinh Thac
[Full Article - PDF] |
4109-4117
| Novel 1,1,3-Trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine Derivatives as Non-Nucleoside Reverse Transcriptase Inhibitors That Inhibit Human Immunodeficiency Virus Type 1 Replication
Esther Arranz,
Juan A. Díaz,
Simon T. Ingate,
Myriam Witvrouw,
Christophe Pannecouque,
Jan Balzarini,
Erik De Clercq, and
Salvador Vega
[Full Article - PDF] |
4118-4129
| Novel, Highly Potent Aldose Reductase Inhibitors: (R)-(-)-2-(4-Bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine- 4-spiro-3'-pyrrolidine-1,2',3,5'-tetrone (AS-3201) and Its Congeners
Toshiyuki Negoro,
Makoto Murata,
Shozo Ueda,
Buichi Fujitani,
Yoshiyuki Ono,
Akemi Kuromiya,
Masanobu Komiya,
Kenji Suzuki, and
Jun-ichi Matsumoto
[Full Article - PDF] |
4130-4142
| Predictive Models for GABAA/Benzodiazepine Receptor Subtypes: Studies of Quantitative Structure-Activity Relationships for Imidazobenzodiazepines at Five Recombinant GABAA/Benzodiazepine Receptor Subtypes [ x3 2 (x = 1-3, 5, and 6)] via Comparative Molecular Field Analysis
Qi Huang,
Ruiyan Liu,
Puwen Zhang,
Xiaohui He,
Ruth McKernan,
Tong Gan,
Dennis W. Bennett, and
James M. Cook
[Full Article - PDF] |
4143-4149
| N-Substituted 9-Methyl-5-(3-hydroxyphenyl)morphans Are Opioid Receptor Pure Antagonists
James B. Thomas,
Xiaoling Zheng,
S. Wayne Mascarella,
Richard B. Rothman,
Christina M. Dersch,
John S. Partilla,
Judith L. Flippen-Anderson,
Clifford F. George,
Buddy E. Cantrell,
Dennis M. Zimmerman, and
F. Ivy Carroll
[Full Article - PDF] |
4150-4160
| Universal Template Approach to Drug Design: Polyamines as Selective Muscarinic Receptor Antagonists
Maria L. Bolognesi,
Anna Minarini,
Roberta Budriesi,
Silvia Cacciaguerra,
Alberto Chiarini,
Santi Spampinato,
Vincenzo Tumiatti, and
Carlo Melchiorre
[Full Article - PDF] |
NOTES
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4161-4164
| Halogenated Chalcones with High-Affinity Binding to P-Glycoprotein: Potential Modulators of Multidrug Resistance
Frédéric Bois,
Chantal Beney,
Ahcène Boumendjel,
Anne-Marie Mariotte,
Gwenaëlle Conseil, and
Attilio Di Pietro
[Full Article - PDF] |
4165-4170
| N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: Synthesis and Adrenergic and Dopaminergic Activity Studies
Nikos Tagmatarchis,
Kyriaki Thermos, and
Haralambos E. Katerinopoulos
[Full Article - PDF] |
4171-4176
| 4-Alkynylphenyl Imidazolylpropyl Ethers as Selective Histamine H3-Receptor Antagonists with High Oral Central Nervous System Activity
Michael Krause,
Xavier Ligneau,
Holger Stark,
Monique Garbarg,
Jean-Charles Schwartz, and
Walter Schunack
[Full Article - PDF] |
4177-4180
| 7-Arylidenenaltrexones as Selective  1 Opioid Receptor Antagonists
Shigenori Ohkawa and
Philip S. Portoghese
[Full Article - PDF] |