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COMMUNICATIONS TO THE EDITOR
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2439-2441
| 1-[2(R)-(2-Amino-2-methylpropionylamino)-3-(1H-indol-3-yl)propionyl]-3- benzylpiperidine-3(S)-carboxylic Acid Ethyl Ester (L-163,540): A Potent, Orally Bioavailable, and Short-Duration Growth Hormone Secretagogue
Lihu Yang,
Greg Morriello,
Arthur A. Patchett,
Kwan Leung,
Tom Jacks,
Kang Cheng,
Klaus D. Schleim,
William Feeney,
Wanda W.-S. Chan,
Shuet-Hing L. Chiu, and
Roy G. Smith
[Full Article -
PDF] |
2442-2444
| 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]- [1,4]benzodiazepin-10(11H)-ylcarbonyl)-3- chlorophenyl]benzamide (VPA-985): An Orally Active Arginine Vasopressin Antagonist with Selectivity for V2 Receptors
J. Donald Albright,
Marvin F. Reich,
Efren G. Delos Santos,
John P. Dusza,
Fuk-Wah Sum,
Aranapakam M.Venkatesan,
Joseph Coupet,
Peter S. Chan,
Xun Ru,
Hossein Mazandarani, and
Trina Bailey
[Full Article -
PDF] |
EXPEDITED ARTICLES
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2445-2450
| Substituted Halogenated Arylsulfonamides: A New Class of  Receptor Binding Tumor Imaging Agents
Christy S. John,
Benjamin B. Lim,
Bertold J. Vilner,
Brian C. Geyer, and
Wayne D. Bowen
[Full Article -
PDF] |
2451-2460
| Structure-Activity Relationship Studies of Novel Carbocyclic Influenza Neuraminidase Inhibitors
Choung U. Kim,
Willard Lew,
Matthew A. Williams,
Huiwei Wu,
Lijun Zhang,
Xiaowu Chen,
Paul A. Escarpe,
Dirk B. Mendel,
W. Graeme Laver, and
Raymond C. Stevens
[Full Article -
PDF] |
ARTICLES
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2461-2480
| Inhibition of Human Neutrophil Elastase. 4. Design, Synthesis, X-ray Crystallographic Analysis, and Structure-Activity Relationships for a Series of P2-Modified, Orally Active Peptidyl Pentafluoroethyl Ketones
Robert J. Cregge,
Sherrie L. Durham,
Robert A. Farr,
Steven L. Gallion,
C. Michelle Hare,
Robert V. Hoffman,
Michael J. Janusz,
Hwa-Ok Kim,
Jack R. Koehl,
Shujaath Mehdi,
William A. Metz,
Norton P. Peet,
John T. Pelton,
Herman A. Schreuder,
Shyam Sunder, and
Chantal Tardif
[Full Article -
PDF] |
2481-2491
| New Chemical Descriptors Relevant for the Design of Biologically Active Peptides. A Multivariate Characterization of 87 Amino Acids
Maria Sandberg,
Lennart Eriksson,
Jörgen Jonsson,
Michael Sjöström, and
Svante Wold
[Full Article -
PDF] |
2492-2502
| Design of a New Class of Orally Active Fibrinogen Receptor Antagonists
Scott I. Klein,
Bruce F. Molino,
Mark Czekaj,
Charles J. Gardner,
Valeria Chu,
Karen Brown,
Ralph D. Sabatino,
Jeffrey S. Bostwick,
Charles Kasiewski,
Ross Bentley,
Vincent Windisch,
Mark Perrone,
Christopher T. Dunwiddie, and
Robert J. Leadley
[Full Article -
PDF] |
2503-2512
| Pharmacophores Incorporating Numerous Excluded Volumes Defined by X-ray Crystallographic Structure in Three-Dimensional Database Searching: Application to the Thyroid Hormone Receptor
Paulette A. Greenidge,
Bo Carlsson,
Lars-Göran Bladh, and
Mikael Gillner
[Full Article -
PDF] |
2513-2523
| Heteroaryl Analogues of AMPA. 2. Synthesis, Absolute Stereochemistry, Photochemistry, and Structure-Activity Relationships
Erik Falch,
Lotte Brehm,
Ivan Mikkelsen,
Tommy N. Johansen,
Niels Skjærbæk,
Birgitte Nielsen,
Tine B. Stensb l,
Bjarke Ebert, and
Povl Krogsgaard-Larsen
[Full Article -
PDF] |
2524-2536
| Design and Synthesis of m1-Selective Muscarinic Agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-Methoxyphenyl)-2-propynyl)- oxime Maleate (CI-1017), a Functionally m1-Selective Muscarinic Agonist
Haile Tecle,
Stephen D. Barrett,
David J. Lauffer,
Corinne Augelli-Szafran,
Mark R. Brann,
Michael J. Callahan,
Bradley. W. Caprathe,
Robert E. Davis,
Patricia D. Doyle,
David Eubanks,
William Lipiniski,
Tara Mirzadegan,
Walter H. Moos,
D. W. Moreland,
Carrie B. Nelson,
Michael R. Pavia,
Charlotte Raby,
Roy D. Schwarz,
Carolyn J. Spencer,
Anthony J. Thomas, and
Juan C. Jaen
[Full Article -
PDF] |
2537-2552
| Synthesis and Evaluation of Analogues of the Partial Agonist 6-(Propyloxy)-4-(methoxymethyl)- -carboline-3-carboxylic Acid Ethyl Ester (6-PBC) and the Full Agonist 6-(Benzyloxy)-4-(methoxymethyl)-- carboline-3-carboxylic Acid Ethyl Ester (Zk 93423) at Wild Type and Recombinant GABAA Receptors
Eric D. Cox,
Hernando Diaz-Arauzo,
Qi Huang,
Mundla S. Reddy,
Chunrong Ma,
Brad Harris,
Ruth McKernan,
Phil Skolnick, and
James M. Cook
[Full Article -
PDF] |
2553-2564
| Three-Dimensional Quantitative Similarity-Activity Relationships (3D QSiAR) from SEAL Similarity Matrices
Hugo Kubinyi,
Fred A. Hamprecht, and
Thomas Mietzner
[Full Article -
PDF] |
2565-2571
| Homonojirimycin Isomers and N-Alkylated Homonojirimycins: Structural and Conformational Basis of Inhibition of Glycosidases
Naoki Asano,
Makoto Nishida,
Atsushi Kato,
Haruhisa Kizu,
Katsuhiko Matsui,
Yutaka Shimada,
Takashi Itoh,
Masanori Baba,
Alison A. Watson,
Robert J. Nash,
Paul M. de Q. Lilley,
David J. Watkin, and
George W. J. Fleet
[Full Article -
PDF] |
2572-2578
| Carbocyclic Analogues of the Potent Cytidine Deaminase Inhibitor 1-(-D-Ribofuranosyl)-1,2-dihydropyrimidin-2-one (Zebularine)
Lak Shin Jeong,
Greg Buenger,
John J. McCormack,
David A. Cooney,
Zhang Hao, and
Victor E. Marquez
[Full Article -
PDF] |
2579-2587
| Synthesis and Evaluation of Peptidyl Michael Acceptors That Inactivate Human Rhinovirus 3C Protease and Inhibit Virus Replication
Jian-she Kong,
Shankar Venkatraman,
Kelly Furness,
Sanjay Nimkar,
Timothy A. Shepherd,
Q. May Wang,
Jeffrey Aubé, and
Robert P. Hanzlik
[Full Article -
PDF] |
2588-2603
| Synthesis and Biological Evaluations of 3-Substituted Indolin-2-ones: A Novel Class of Tyrosine Kinase Inhibitors That Exhibit Selectivity toward Particular Receptor Tyrosine Kinases
Li Sun,
Ngoc Tran,
Flora Tang,
Harald App,
Peter Hirth,
Gerald McMahon, and
Cho Tang
[Full Article -
PDF] |
2604-2613
| Neurosteroid Analogues. 6. The Synthesis and GABAA Receptor Pharmacology of Enantiomers of Dehydroepiandrosterone Sulfate, Pregnenolone Sulfate, and (3 ,5)-3-Hydroxypregnan-20-one Sulfate
Kent R. Nilsson,
Charles F. Zorumski, and
Douglas F. Covey
[Full Article -
PDF] |
2614-2620
| Minimal-Size, Constrained Corticotropin-Releasing Factor Agonists with i-(i+3) Glu-Lys and Lys-Glu Bridges
Jean Rivier,
Sabine L. Lahrichi,
Jozsef Gulyas,
Judit Erchegyi,
Steven C. Koerber,
A. Grey Craig,
Anne Corrigan,
Catherine Rivier, and
Wylie Vale
[Full Article -
PDF] |
2621-2625
| Synthesis of 7,8-(Methylenedioxy)-1-phenyl-3,5-dihydro-4H-2,3-benzodiazepin- 4-ones as Novel and Potent Noncompetitive AMPA Receptor Antagonists
Yan Wang,
Christopher S. Konkoy,
Victor I. Ilyin,
Kimberly E. Vanover,
Richard B. Carter,
Eckard Weber,
John F. W. Keana,
Richard M. Woodward, and
Sui Xiong Cai
[Full Article - PDF] |
NOTES
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2626-2630
| In Vitro Platelet-Activating Factor Receptor Binding Inhibitory Activity of Pinusolide Derivatives: A Structure-Activity Study
Byung Hoon Han,
Hyun Ok Yang,
Young-Hwa Kang,
Dae-Yeon Suh,
Hyun Jung Go,
Wan-Jin Song,
Yong Chul Kim, and
Man Ki Park
[Full Article -
PDF] |
2631-2635
| Synthesis and Biological Activity of a Novel Methylamine-Bridged Enkephalin Analogue (MABE): A New Route to Cyclic Peptides and Peptidomimetics
Kevin Shreder,
Li Zhang,
Trunghau Dang,
Tony L. Yaksh,
Hiroshi Umeno,
Robert DeHaven,
Jeffrey Daubert, and
Murray Goodman
[Full Article -
PDF] |
2636-2642
| Nitroaromatic Amino Acids as Inhibitors of Neuronal Nitric Oxide Synthase
Marlon Cowart,
Elizabeth A. Kowaluk,
Jerome F. Daanen,
Kathy L. Kohlhaas,
Karen M. Alexander,
Frank L. Wagenaar, and
James F. Kerwin, Jr.
[Full Article - PDF] |
2643-2650
| Identification of a Dihydropyridine as a Potent 1a Adrenoceptor-Selective Antagonist That Inhibits Phenylephrine-Induced Contraction of the Human Prostate
Wai C. Wong,
George Chiu,
John M. Wetzel,
Mohammad R. Marzabadi,
Dhanapalan Nagarathnam,
Diana Wang,
James Fang,
Shou Wu Miao,
Xingfang Hong,
Carlos Forray,
Pierre J.-J. Vaysse,
Theresa A. Branchek, and
Charles Gluchowski
, Rui Tang and
Herbert Lepor
[Full Article - PDF] |
2651-2656
| N-Arylalkyl Pseudopeptide Inhibitors of Farnesyltransferase
S. Jane deSolms,
Elizabeth A. Giuliani,
Samuel L. Graham,
Kenneth S. Koblan,
Nancy E. Kohl,
Scott D. Mosser,
Allen I. Oliff,
David L. Pompliano,
Elaine Rands,
Thomas H. Scholz,
Catherine M. Wiscount,
Jackson B. Gibbs, and
Robert L. Smith
[Full Article - PDF] |
2657-2660
| 14-Desoxy Analogues of Naltrindole and 7-Spiroindanyloxymorphone: The Role of the 14-Hydroxy Group at  Opioid Receptors
Tushar A. Kshirsagar,
Xinqin Fang, and
Philip S. Portoghese
[Full Article - PDF] |
BOOK REVIEWS
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2661-2661
| Oxford Dictionary of Biochemistry and Molecular Biology Edited by A. D. Smith, S. P. Datta, G. H. Smith, P. N. Campbell, R. Bentley, and H. A. McKenzie. Oxford University Press, Oxford. 1997. xi + pp. 20.5 x 26 cm. ISBN 0-19-854768-4. $60.00.
Bruce L. Currie
[Full Article - PDF] |
2661-2661
| Affinity Separations. A Practical Approach Edited by Paul Matejtschuk. Oxford University Press, New York. 1997. xix + 253 pp. 15.5 x 23.5 cm. ISBN 0-19-963550-1. $55.00.
Michael W. Duffel
[Full Article - PDF] |
2661-2662
| The Impact of Stereochemistry on Drug Development and Use Edited by Hassan Y. Aboul-Enein and Irving W. Wainer. John Wiley & Sons, New York. 1997. xxvii + 695 pp. 16 x 24 cm. ISBN 0471596442. $99.00.
John L. Neumeyer
[Full Article - PDF] |