Volume 39; Issue 1

Journal of Medicinal Chemistry

Volume 39; Issue 1

1

Conformationally Constrained Analogues of Diacylglycerol. 11.1 Ultrapotent Protein Kinase C Ligands Based on a Chiral 5-Disubstituted Tetrahydro-2-furanone Template

Lee, Jeewoo, Wang, Shaomeng, Milne, George W. A., Sharma, Rajiv, Lewin, Nancy E., Blumberg, Peter M., Marquez, Victor E.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 308 KB

english, 1996

2

Binding of O-Alkyl Derivatives of Serotonin at Human 5-HT1Dβ Receptors

Glennon, Richard A., Hong, Seoung-Soo, Bondarev, Mikhail, Law, Ho, Dukat, Malgorzata, Rakhit, Suman, Power, Patricia, Fan, Ermei, Kinneau, Diana, Kamboj, Rajender

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 188 KB

english, 1996

3

Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure−Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor Receptor

Bridges, Alexander J., Zhou, Hairong, Cody, Donna R., Rewcastle, Gordon W., McMichael, Amy, Showalter, H. D. Hollis, Fry, David W., Kraker, Alan J., Denny, William A.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 302 KB

english, 1996

4

Structure−Activity Relationships in a Series of 2(1H)-Quinolones Bearing Different Acidic Function in the 3-Position: 6,7-Dichloro-2(1H)-oxoquinoline-3-phosphonic Acid, a New Potent and Selective AMPA/Kainate Antagonist with Neuroprotective Properties

Desos, Patrice, Lepagnol, Jean M., Morain, Philippe, Lestage, Pierre, Cordi, Alex A.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 462 KB

english, 1996

5

Substituted Xanthines, Pteridinediones, and Related Compounds as Potential Antiinflammatory Agents. Synthesis and Biological Evaluation of Inhibitors of Tumor Necrosis Factor α

Cottam, Howard B., Shih, Hsiencheng, Tehrani, Lida R., Wasson, D. Bruce, Carson, Dennis A.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 384 KB

english, 1996

6

Biarylcarboxylic Acids and -amides: Inhibition of Phosphodiesterase Type IV versus [ 3 H]Rolipram Binding Activity and Their Relationship to Emetic Behavior in the Ferret

Duplantier, Allen J., Biggers, Michael S., Chambers, Robert J., Cheng, John B., Cooper, Kelvin, Damon, David B., Eggler, James F., Kraus, Kenneth G., Marfat, Anthony, Masamune, Hiroko, Pillar, Joann S

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 201 KB

english, 1996

7

Binding of Arylpiperazines, (Aryloxy)propanolamines, and Tetrahydropyridylindoles to the 5-HT 1A Receptor: Contribution of the Molecular Lipophilicity Potential to Three-Dimensional Quantitative Structure−Affinity Relationship Models

Gaillard, Patrick, Carrupt, Pierre-Alain, Testa, Bernard, Schambel, Philippe

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 304 KB

english, 1996

8

Conformational Analysis of D 1 Dopamine Receptor Agonists: Pharmacophore Assessment and Receptor Mapping †

Mottola, David M., Laiter, Sergei, Watts, Val J., Tropsha, Alexander, Wyrick, Steven D., Nichols, David E., Mailman, Richard B.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 512 KB

english, 1996

9

Studies of Cardiotonic Agents. 8. Synthesis and Biological Activities of Optically Active 6-(4-(Benzylamino)-7-quinazolinyl)-4,5-dihydro-5-methyl- 3(2 H )-pyridazinone (KF15232)

Nomoto, Yuji, Takai, Haruki, Ohno, Tetsuji, Nagashima, Ken, Yao, Kozo, Yamada, Koji, Kubo, Kazuhiro, Ichimura, Michio, Mihara, Akira, Kase, Hiroshi

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 330 KB

english, 1996

10

(−)-Arctigenin as a Lead Structure for Inhibitors of Human Immunodeficiency Virus Type-1 Integrase

Eich, Eckart, Pertz, Heinz, Kaloga, Macki, Schulz, Jutta, Fesen, Mark R., Mazumder, Abhijit, Pommier, Yves

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 535 KB

english, 1996

11

Nonpeptide Angiotensin II Receptor Antagonists: Synthesis, Biological Activities, and Structure−Activity Relationships of Imidazole-5-carboxylic Acids Bearing Alkyl, Alkenyl, and Hydroxyalkyl Substituents at the 4-Position and Their Related Compounds

Yanagisawa, Hiroaki, Amemiya, Yoshiya, Kanazaki, Takuro, Shimoji, Yasuo, Fujimoto, Koichi, Kitahara, Yoshiko, Sada, Toshio, Mizuno, Makoto, Ikeda, Masahiro, Miyamoto, Shuichi, Furukawa, Youji, Koike,

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 846 KB

english, 1996

12

Potent Human Immunodeficiency Virus Type 1 Protease Inhibitors That Utilize Noncoded d -Amino Acids as P 2 /P 3 Ligands

Jungheim, Louis N., Shepherd, Timothy A., Baxter, Angela J., Burgess, Jeffrey, Hatch, Steven D., Lubbehusen, Penny, Wiskerchen, MaryAnn, Muesing, Mark A.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 475 KB

english, 1996

13

Cardioselective Antiischemic ATP-Sensitive Potassium Channel Openers. 4. Structure−Activity Studies on Benzopyranylcyanoguanidines: Replacement of the Benzopyran Portion

Atwal, Karnail S., Ferrara, Francis N., Ding, Charles Z., Grover, Gary J., Sleph, Paul G., Dzwonczyk, Steven, Baird, Anne J., Normandin, Diane E.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 481 KB

english, 1996

14

Discovery of the Hemifumarate and (α- l -Alanyloxy)methyl Ether as Prodrugs of an Antirheumatic Oxindole: Prodrugs for the Enolic OH Group

Robinson, Ralph P., Reiter, Lawrence A., Barth, Wayne E., Campeta, Anthony M., Cooper, Kelvin, Cronin, Brian J., Destito, Rosalina, Donahue, Kathleen M., Falkner, Fred C., Fiese, Eugene F., Johnson, D

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 247 KB

english, 1996

15

New σ and 5-HT 1A Receptor Ligands: ω-(Tetralin-1-yl)- n -alkylamine Derivatives

Berardi, Francesco, Colabufo, Nicola A., Giudice, Giuseppe, Perrone, Roberto, Tortorella, Vincenzo, Govoni, Stefano, Lucchi, Laura

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 224 KB

english, 1996

16

Effect of Linking Bridge Modifications on the Antipsychotic Profile of Some Phthalimide and Isoindolinone Derivatives

Norman, Mark H., Minick, Douglas J., Rigdon, Greg C.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 410 KB

english, 1996

17

3-Benzisothiazolylpiperazine Derivatives as Potential Atypical Antipsychotic Agents

Howard, Harry R., Lowe, John A., Seeger, Thomas F., Seymour, Patricia A., Zorn, Stevin H., Maloney, Patrick R., Ewing, Frank E., Newman, Michael E., Schmidt, Anne W., Furman, Jerome S., Robinson, Gwen

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 192 KB

english, 1996

18

Azole Phenoxy Hydroxyureas as Selective and Orally Active Inhibitors of 5-Lipoxygenase

Malamas, Michael S., Carlson, Richard P., Grimes, David, Howell, Ralph, Glaser, Keith, Gunawan, Iwan, Nelson, James A., Kanzelberger, Mira, Shah, Uresh, Hartman, David A.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 310 KB

english, 1996

19

Structure−Antigastrin Activity Relationships of New Spiroglumide Amido Acid Derivatives

Makovec, Francesco, Peris, Walter, Frigerio, Sandra, Giovanetti, Roberto, Letari, Ornella, Mennuni, Laura, Revel, Laura

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 326 KB

english, 1996

20

Synthesis and Antitumor Evaluation of a Highly Potent Cytotoxic DNA Cross-Linking Polyamine Analogue, 1,12-Diaziridinyl-4,9-diazadodecane

Li, Yanlong, Eiseman, Julie L., Sentz, Dorothy L., Rogers, Faye A., Pan, Su-Shu, Hu, Li-Tai, Egorin, Merrill J., Callery, Patrick S.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 94 KB

english, 1996

21

Design and Synthesis of Non-Peptide Ras CAAX Mimetics as Potent Farnesyltransferase Inhibitors

Qian, Yimin, Vogt, Andreas, Sebti, Saïd M., Hamilton, Andrew D.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 216 KB

english, 1996

22

The Squalestatins: Decarboxy and 4-Deoxy Analogues as Potent Squalene Synthase Inhibitors 1

Chan, Chuen, Andreotti, Daniele, Cox, Brian, Dymock, Brian W., Hutson, Julie L., Keeling, Suzanne E., McCarthy, Alun D., Procopiou, Panayiotis A., Ross, Barry C., Sareen, Meenu, Scicinski, Jan J., Sha

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 548 KB

english, 1996

23

N -Methyl- d -aspartic Acid Receptor Agonists: Resolution, Absolute Stereochemistry, and Pharmacology of the Enantiomers of 2-Amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic Acid

Madsen, Ulf, Frydenvang, Karla, Ebert, Bjarke, Johansen, Tommy N., Brehm, Lotte, Krogsgaard-Larsen, Povl

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 379 KB

english, 1996

24

Quinazoline Antifolate Thymidylate Synthase Inhibitors: γ-Linked l - d , d - d , and d - l Dipeptide Analogues of 2-Desamino-2-methyl- N 10 -propargyl-5,8-dideazafolic Acid (ICI 198583) †,‡

Bavetsias, Vassilios, Jackman, Ann L., Kimbell, Rosemary, Gibson, William, Boyle, F. Thomas, Bisset, Graham M. F.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

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PDF, 572 KB

english, 1996

25

Computer-Aided Molecular Design. Applications in Agrochemicals, Materials, and Pharmaceuticals Edited by C. Reynolds, M. Holloway, and H. Cox. American Chemical Society, Washington, DC. 1995. x + 428 pp. 15.5 × 23.5 cm. ISBN 0-8412-3160-5. $109.95.

Dixon, J. Scott

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 28 KB

english, 1996

26

To See the Obvious. By Arthur J. Birch. In Profiles, Pathways and Dreams Edited by Jeffrey I. Seeman. American Chemical Society, Washington, DC. 1995. xxviii + 269 pp. 15 × 23 cm. ISBN 0-8412-1840-4. $24.95.

Barton, Derek H. R.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 28 KB

english, 1996

27

Synthesis and Biological Evaluation of dl -4,4-Difluoroglutamic Acid and dl -γ,γ-Difluoromethotrexate

Tsukamoto, Takashi, Kitazume, Tomoya, McGuire, John J., Coward, James K.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 231 KB

english, 1996

28

Conformationally Constrained Analogues of Diacylglycerol. 12. 1 Ultrapotent Protein Kinase C Ligands Based on a Chiral 4,4-Disubstituted Heptono-1,4-lactone Template

Lee, Jeewoo, Sharma, Rajiv, Wang, Shaomeng, Milne, George W. A., Lewin, Nancy E., Szallasi, Zoltan, Blumberg, Peter M., George, Clifford, Marquez, Victor E.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 500 KB

english, 1996

29

Conformationally Constrained Analogues of Diacylglycerol. 10. Ultrapotent Protein Kinase C Ligands Based on a Racemic 5-Disubstituted Tetrahydro-2-furanone Template 1

Sharma, Rajiv, Lee, Jeewoo, Wang, Shaomeng, Milne, George W. A., Lewin, Nancy E., Blumberg, Peter M., Marquez, Victor E.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 462 KB

english, 1996

30

Theoretical Study of Inhibition of Adenosine Deaminase by (8 R )-Coformycin and (8 R )-Deoxycoformycin

Marrone, Tami J., Straatsma, T. P., Briggs, James M., Wilson, David K., Quiocho, Florante A., McCammon, J. Andrew

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 274 KB

english, 1996

31

Dibenzoxepinone Hydroxylamines and Hydroxamic Acids: Dual Inhibitors of Cyclooxygenase and 5-Lipoxygenase with Potent Topical Antiinflammatory Activity

Hamer, R. Richard L., Tegeler, John J., Kurtz, Ellen S., Allen, Richard C., Bailey, Steven C., Elliott, Mary Ellen, Hellyer, Luther, Helsley, Grover C., Przekop, Penelope, Freed, Brian S., White, John

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 223 KB

english, 1996

32

Diarylspiro[2.4]heptenes as Orally Active, Highly Selective Cyclooxygenase-2 Inhibitors: Synthesis and Structure−Activity Relationships

Huang, Horng-Chih, Li, James J., Garland, Danny J., Chamberlain, Timothy S., Reinhard, Emily J., Manning, Robert E., Seibert, Karen, Koboldt, Carol M., Gregory, Susan A., Anderson, Gary D., Veenhuizen

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 353 KB

english, 1996

33

The View from Inside the Receptor

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 27 KB

english, 1996

34

Synthesis and Biological Activity of Folic Acid and Methotrexate Analogues Containing l - threo -(2 S, 4 S )-4-Fluoroglutamic Acid and dl -3,3-Difluoroglutamic Acid

Hart, Barry P., Haile, William H., Licato, Nicholas J., Bolanowska, Wanda E., McGuire, John J., Coward, James K.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 425 KB

english, 1996

35

Development of Highly Potent Inhibitors of Ras Farnesyltransferase Possessing Cellular and in Vivo Activity

Leftheris, Katerina, Kline, Toni, Vite, Gregory D., Cho, Young H., Bhide, Rajeev S., Patel, Dinesh V., Patel, Manorama M., Schmidt, Robert J., Weller, Harold N., Andahazy, Mary L., Carboni, Joan M., G

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 415 KB

english, 1996

36

Synthesis and Structure−Activity Relationships of Phenylenebis(methylene)- Linked Bis-tetraazamacrocycles That Inhibit Human Immunodeficiency Virus Replication. 2. Effect of Heteroaromatic Linkers on the Activity of Bicyclams

Bridger, Gary J., Skerlj, Renato T., Padmanabhan, Sreenivasan, Martellucci, Stephen A., Henson, Geoffrey W., Abrams, Michael J., Joao, Heidi C., Witvrouw, Myriam, De Vreese, Karen, Pauwels, Rudi, De C

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 527 KB

english, 1996

37

High-Affinity Partial Agonist Imidazo[1,5- a ]quinoxaline Amides, Carbamates, and Ureas at the γ-Aminobutyric Acid A/Benzodiazepine Receptor Complex †

Jacobsen, E. Jon, TenBrink, Ruth E., Stelzer, Lindsay S., Belonga, Kenneth L., Carter, Donald B., Im, Haesook K., Im, Wha Bin, Sethy, Vimala H., Tang, Andy H., VonVoigtlander, Philip F., Petke, James

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 598 KB

english, 1996

38

Synthesis and Modeling Studies with Monocyclic Analogues of Mycophenolic Acid

Anderson, Wayne K., Boehm, Terri L., Makara, Gergely M., Swann, R. Thomas

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 345 KB

english, 1996

39

In Vitro and in Vivo Studies of Benzisoquinoline Ligands for the Brain Synaptic Vesicle Monoamine Transporter

Lee, Lihsueh C., Vander Borght, Thierry, Sherman, Phillip S., Frey, Kirk A., Kilbourn, Michael R.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 167 KB

english, 1996

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