Journal of Medicinal Chemistry
Volume 41, Issue 22 (October 22, 1998)
Copyright © 1998 American Chemical Society

Click [Full Article - PDF] to display or print the full article page image in PDF.

COMMUNICATIONS TO THE EDITOR

4181-4185

Synthesis and Modeling Studies of a Potent Conformationally Rigid Muscarinic Agonist: 1-Azabicyclo[2.2.1]heptanespirofuranone Edwin S. C. Wu, Alexander Kover, and Simon F. Semus [Full Article - PDF]

4186-4189

Acetylcholinesterase Noncovalent Inhibitors Based on a Polyamine Backbone for Potential Use against Alzheimer's Disease Carlo Melchiorre, Vincenza Andrisano, Maria L. Bolognesi, Roberta Budriesi, Andrea Cavalli, Vanni Cavrini, Michela Rosini, Vincenzo Tumiatti, and Maurizio Recanatini [Full Article - PDF]

4190-4195

Discovery of a Novel, Potent, and Orally Active Nonpeptide Antagonist of the Human Luteinizing Hormone-Releasing Hormone (LHRH) Receptor Nobuo Cho, Masataka Harada, Toshihiro Imaeda, Takashi Imada, Hirokazu Matsumoto, Yoji Hayase, Satoshi Sasaki, Shuichi Furuya, Nobuhiro Suzuki, Shoichi Okubo, Kazuhiro Ogi, Satoshi Endo, Haruo Onda, and Masahiko Fujino [Full Article - PDF]

4196-4198

6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2,3-b]pyridine (RWJ 68354): A Potent and Selective p38 Kinase Inhibitor James R. Henry, Kenneth C. Rupert, John H. Dodd, Ignatius J. Turchi, Scott A. Wadsworth, Druie E. Cavender, Bohumila Fahmy, Gilbert C. Olini, Janet E. Davis, J. Lee Pellegrino-Gensey, Peter H. Schafer, and John J. Siekierka [Full Article - PDF]

EXPEDITED ARTICLES

4199-4206

Synthesis and Evaluation of N-[11C]Methylated Analogues of Epibatidine as Tracers for Positron Emission Tomographic Studies of Nicotinic Acetylcholine Receptors Andrew G. Horti, Ursula Scheffel, Alane S. Kimes, John L. Musachio, Hayden T. Ravert, William B. Mathews, Yougen Zhan, Paige A. Finley, Edythe D. London, and Robert F. Dannals [Full Article - PDF]

ARTICLES

4207-4215

Derivation of a Pharmacophore Model for Anandamide Using Constrained Conformational Searching and Comparative Molecular Field Analysis Weida Tong, Elizabeth R. Collantes, and William J. Welsh , Barbara A. Berglund and Allyn C. Howlett [Full Article - PDF]

4216-4223

Novel Cyclic Compounds as Potent Phosphodiesterase 4 Inhibitors Wei He, Fu-Chih Huang, Barbara Hanney, John Souness, Bruce Miller, Guyan Liang, Jon Mason, and Stevan Djuric [Full Article - PDF]

4224-4231

In Vitro and in Vivo Activities of Oligodeoxynucleotide-Based Thrombin Inhibitors Containing Neutral Formacetal Linkages Gong-Xin He, John P. Williams, Michael J. Postich, S. Swaminathan, Regan G. Shea, Terry Terhorst, Veronica S. Law, Cheri T. Mao, Cathy Sueoka, Steven Coutré, and Norbert Bischofberger [Full Article - PDF]

4232-4239

Axially Chiral N-Benzyl-N,7-dimethyl-5-phenyl-1,7-naphthyridine-6-carboxamide Derivatives as Tachykinin NK1 Receptor Antagonists: Determination of the Absolute Stereochemical Requirements Yoshinori Ikeura, Yuji Ishichi, Toshimasa Tanaka, Akira Fujishima, Mika Murabayashi, Mitsuru Kawada, Takenori Ishimaru, Izumi Kamo, Takayuki Doi, and Hideaki Natsugari [Full Article - PDF]

4240-4250

Design of Benzamidine-Type Inhibitors of Factor Xa Bernhard Gabriel, Milton T. Stubbs, Andreas Bergner, Jörg Hauptmann, Wolfram Bode, Jörg Stürzebecher, and Luis Moroder [Full Article - PDF]

4251-4260

Metabolites of the Angiotensin II Antagonist Tasosartan: The Importance of a Second Acidic Group John W. Ellingboe, Michael D. Collini, Dominick Quagliato, James Chen, Madelene Antane, Jean Schmid, Dale Hartupee, Valerie White, C. Hyung Park, Tarak Tanikella, and Jehan F. Bagli [Full Article - PDF]

4261-4272

Quantitative Structure-Activity Relationships of 2,4-Diamino-5-(2-X-benzyl)pyrimidines versus Bacterial and Avian Dihydrofolate Reductase Cynthia Dias Selassie, Wei-Xi Gan, Lara S. Kallander, and Teri E. Klein [Full Article - PDF]

4273-4278

Design of New Topoisomerase II Inhibitors Based upon a Quinobenzoxazine Self-Assembly Model Qingping Zeng, Yan Kwok, Sean M. Kerwin, Gina Mangold, and Laurence H. Hurley [Full Article - PDF]

4279-4287

Studies on Selectin Blockers. 7. Structure-Activity Relationships of Sialyl Lewis X Mimetics Based on Modified Ser-Glu Dipeptides Takahiro Tsukida, Hideki Moriyama, Kiriko Kurokawa, Toshio Achiha, Yoshimasa Inoue, and Hirosato Kondo [Full Article - PDF]

4288-4300

Potent and Selective Non-Cysteine-Containing Inhibitors of Protein Farnesyltransferase David J. Augeri, Stephen J. O'Connor, Dave Janowick, Bruce Szczepankiewicz, Gerry Sullivan, John Larsen, Douglas Kalvin, Jerry Cohen, Edward Devine, Haichao Zhang, Sajeev Cherian, Badr Saeed, Shi-Chung Ng, and Saul Rosenberg [Full Article - PDF]

4301-4308

Synthesis of Peptide Aldehyde Derivatives as Selective Inhibitors of Human Cathepsin L and Their Inhibitory Effect on Bone Resorption Tsuneo Yasuma, Satoru Oi, Nobuo Choh, Toshiyuki Nomura, Naoki Furuyama, Atsushi Nishimura, Yukio Fujisawa, and Takashi Sohda [Full Article - PDF]

4309-4316

Novel Calcium Antagonists with Both Calcium Overload Inhibition and Antioxidant Activity. 1. 2-(3,5-Di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones Tatsuya Kato, Tomokazu Ozaki, Kazuhiko Tamura, Yoshiyuki Suzuki, Michitaka Akima, and Nobuhiro Ohi [Full Article - PDF]

4317-4328

Bis-Cationic Heteroaromatics as Macrofilaricides: Synthesis of Bis-Amidine and Bis-Guanylhydrazone Derivatives of Substituted Imidazo[1,2-a]pyridines Richard J. Sundberg, Sujay Biswas, Krishna Kumar Murthi, and Donna Rowe , John W. McCall and Michael T. Dzimianski [Full Article - PDF]

4329-4342

Design of Peptidomimetics That Inhibit the Association of Phosphatidylinositol 3-Kinase with Platelet-Derived Growth Factor- Receptor and Possess Cellular Activity Scott R. Eaton, Wayne L. Cody, Annette M. Doherty, Debra R. Holland, Robert L. Panek, Gina H. Lu, Tawny K. Dahring, and David R. Rose [Full Article - PDF]

4343-4353

5-Substituted Pyrimidines with a 1,5-Anhydro-2,3-dideoxy-D-arabino-hexitol Moiety at N-1: Synthesis, Antiviral Activity, Conformational Analysis, and Interaction with Viral Thymidine Kinase Tomasz Ostrowski, Berthold Wroblowski, Roger Busson, Jozef Rozenski, Erik De Clercq, Matthew S. Bennett, John N. Champness, William C. Summers, Mark R. Sanderson, and Piet Herdewijn [Full Article - PDF]

4354-4359

5-Benzylidene 1,2-Dihydrochromeno[3,4-f]quinolines, A Novel Class of Nonsteroidal Human Progesterone Receptor Agonists Christopher M. Tegley, Lin Zhi, Keith B. Marschke, Marco M. Gottardis, Qinchuan Yang, and Todd K. Jones [Full Article - PDF]

4360-4364

Bisquinolines. 2. Antimalarial N,N-Bis(7-chloroquinolin-4-yl)heteroalkanediamines Jonathan L. Vennerstrom, Arba L. Ager, Jr., Arnulf Dorn, Steven L. Andersen, Lucia Gerena, Robert G. Ridley, and Wilbur K. Milhous [Full Article - PDF]

4365-4377

Synthesis and Tyrosine Kinase Inhibitory Activity of a Series of 2-Amino-8H-pyrido[2,3-d]pyrimidines: Identification of Potent, Selective Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitors Diane H. Boschelli, Zhipei Wu, Sylvester R. Klutchko, H. D. Hollis Showalter, James M. Hamby, Gina H. Lu, Terry C. Major, Tawny K. Dahring, Brian Batley, Robert L. Panek, Joan Keiser, Brian G. Hartl, Alan J. Kraker, Wayne D. Klohs, Bill J. Roberts, Sandra Patmore, William L. Elliott, Randy Steinkampf, Laura A. Bradford, Hussein Hallak, and Annette M. Doherty [Full Article - PDF]

4378-4384

Muscarinic Agonists with Antipsychotic-like Activity: Structure-Activity Relationships of 1,2,5-Thiadiazole Analogues with Functional Dopamine Antagonist Activity Per Sauerberg, Lone Jeppesen, Preben H. Olesen, Thger Rasmussen, Michael D. B. Swedberg, Malcolm J. Sheardown, Anders Fink-Jensen, Christian Thomsen, Henning Thgersen, Karin Rimvall, John S. Ward, David O. Calligaro, Neil W. DeLapp, Frank P. Bymaster, and Harlan E. Shannon [Full Article - PDF]

4385-4399

CoMFA-Based Prediction of Agonist Affinities at Recombinant D1 vs D2 Dopamine Receptors Richard E. Wilcox, Tom Tseng, Mi-Youn Kim Brusniak, Brett Ginsburg, Robert S. Pearlman, Martha Teeter, Curtiss DuRand, Stephanie Starr, and Kim A. Neve [Full Article - PDF]

4400-4407

Potent Cyano and Carboxamido Side-Chain Analogues of 1',1'-Dimethyl-8-Tetrahydrocannabinol Michael Singer, William J. Ryan, Bijali Saha, Billy R. Martin, and Raj K. Razdan [Full Article - PDF]

4408-4420

Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase. 3. Discovery of a Novel Series of N-Alkyl-N-[(fluorophenoxy)benzyl]-N'-arylureas with Weak Toxicological Effects on Adrenal Glands Akira Tanaka, Takeshi Terasawa, Hiroyuki Hagihara, Noriko Ishibe, Masae Sawada, Yuri Sakuma, Masaharu Hashimoto, Hisashi Takasugi, and Hirokazu Tanaka [Full Article - PDF]

NOTES

4421-4423

Bisphenols That Stimulate Cells To Release Alkali Metal Cations: A Structure-Activity Study Laszlo Hopp, Susan O. Megee, and John B. Lloyd [Full Article - PDF]

BOOK REVIEWS

4424-4424

Second Supplements to the Second Edition of Rodd's Chemistry of Carbon Compounds. Volume IV: Heterocyclic Compounds. Part C: Five-Membered Heterocyclic Compounds with Two Hetero-Atoms in the Ring from Groups V and VI of the Periodic Table; Part D: Five-Membered Heterocyclic Compounds with More Than Two Hetero-Atoms in the Ring Edited by M. Sainsbury. Elsevier, Amsterdam. 1998. xvi + 281 pp. 15.5 × 23 cm. ISBN-0-444-828702. $187.00. Arnold Martin [Full Article - PDF]

4424-4425

A Practical Guide to Combinatorial Chemistry Edited by A. W. Czarnik and S. H. DeWitt. American Chemical Society, Washington, D.C. 1997. xiv + 450 pp. 15.5 × 23.5 cm. ISBN 0-8412-3485. $89.95. Donald J. Kyle [Full Article - PDF]

4425-4425

Analytical Chemistry Edited by R. Kellner, J.-M. Mermet, M. Otto, and H. M. Widmer. Wiley-VCH, New York. 1998. xxv + 916 pp. 21.5 × 30 cm. ISBN 3-527-286101. $84.95. Jerry L. Born [Full Article - PDF]

4425-4426

High-Performance Capillary Electrophoresis Edited by Morteza G. Kahaledi. John Wiley & Sons, New York, NY. 1998. xxxii + 1047 pp. 16 × 24 cm. ISBN 0-471-148512. $150.00. Robert J. Linhardt [Full Article - PDF]

4426-4426

The Combinatorial Index By Barry A. Bunin. Academic Press, New York, NY. 1998. xvii + 322 pp. 18 × 26 cm. ISBN 0-12-141340-3. $79.95. Lester A. Mitscher [Full Article - PDF]

4426-4427

Practical Application of Computer-Aided Drug Design Edited by Paul S. Charifson. Marcel Dekker, Inc., New York, NY. 1997. x + 52 pp. 16 × 23.5 cm. ISBN 0-8247-9885-6. $150.00. Donald J. Abraham [Full Article - PDF]

4427-4428

The Laboratory Companion: A Practical Guide to Materials, Equipment, and Technique By Gary S. Coyne. John Wiley & Sons, New York. 1997. xviii + 527 pp. 18 × 26 cm. ISBN 0-4711-8422-5. $59.95. Thomas C. Boge [Full Article - PDF]

4428-4428

Emerging Drugs. The Prospect for Improved Medicines. Annual Executive Briefing. Volume 3. Edited by W. C. Bowman, J. D. Fitzgerald, and J. B. Taylor. Ashley Publications Ltd., London. 1998. vi + 397 pp. 21 x 29.54 cm. ISSN 1361-9195. $690.00. Joseph Weinstock [Full Article - PDF]