Search Results - "Almond, Harold"

Thrombogenic Collagen-Mimetic Peptides: Self-Assembly of Triple Helix-Based Fibrils Driven by Hydrophobic Interactions by Cejas, Mabel A., Kinney, William A., Chen, Cailin, Vinter, Jeremy G., Almond, Harold R., Balss, Karin M., Maryanoff, Cynthia A., Schmidt, Ute, Breslav, Michael, Mahan, Andrew, Lacy, Eilyn, Maryanoff, Bruce E.

“…Collagens are integral structural proteins in animal tissues and play key functional roles in cellular modulation. We sought to discover collagen model…”
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Gaussian docking functions by McGann, Mark R., Almond, Harold R., Nicholls, Anthony, Grant, J. Andrew, Brown, Frank K.

“…A shape‐based Gaussian docking function is constructed which uses Gaussian functions to represent the shapes of individual atoms. A set of 20 trypsin…”
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Discovery of Potent, Selective, Orally Active, Nonpeptide Inhibitors of Human Mast Cell Chymase by Greco, Michael N, Hawkins, Michael J, Powell, Eugene T, Almond, Harold R, de Garavilla, Lawrence, Hall, Jeffrey, Minor, Lisa K, Wang, Yuanping, Corcoran, Thomas W, Di Cera, Enrico, Cantwell, Angelene M, Savvides, Savvas N, Damiano, Bruce P, Maryanoff, Bruce E

“…A series of β-carboxamido-phosphon(in)ic acids (2) was identified as a new structural motif for obtaining potent inhibitors of human mast cell chymase. For…”
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Structure-Function Analysis of Urotensin II and Its Use in the Construction of a Ligand-Receptor Working Model by Kinney, William A., Almond, Jr, Harold R., Qi, Jenson, Smith, Charles E., Santulli, Rosemary J., de Garavilla, Lawrence, Andrade-Gordon, Patricia, Cho, Daniel S., Everson, Anita M., Feinstein, Mark A., Leung, Perry A., Maryanoff, Bruce E.

“…The salient structural features of urotensin II (U II) required for stimulation of its G‐protein‐coupled receptor were obtained from biological evaluation of…”
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In-Depth Study of Tripeptide-Based α-Ketoheterocycles as Inhibitors of Thrombin. Effective Utilization of the S1‘ Subsite and Its Implications to Structure-Based Drug Design by Costanzo, Michael J, Almond, Harold R, Hecker, Leonard R, Schott, Mary R, Yabut, Stephen C, Zhang, Han-Cheng, Andrade-Gordon, Patricia, Corcoran, Thomas W, Giardino, Edward C, Kauffman, Jack A, Lewis, Joan M, de Garavilla, Lawrence, Haertlein, Barbara J, Maryanoff, Bruce E

“…Thrombin inhibitors are potentially useful in medicine for their anticoagulant and antithrombotic effects. We synthesized and evaluated diverse…”
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Potent, Small-Molecule Inhibitors of Human Mast Cell Tryptase. Antiasthmatic Action of a Dipeptide-Based Transition-State Analogue Containing a Benzothiazole Ketone by Costanzo, Michael J, Yabut, Stephen C, Almond, Harold R, Andrade-Gordon, Patricia, Corcoran, Thomas W, de Garavilla, Lawrence, Kauffman, Jack A, Abraham, William M, Recacha, Rosario, Chattopadhyay, Debashish, Maryanoff, Bruce E

“…Inhibitors of human mast cell tryptase (EC 3.4.21.59) have therapeutic potential for treating allergic or inflammatory disorders. We have investigated…”
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Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: Synthesis, SAR, and in vivo assessment by Luci, Diane K., Ghosh, Shyamali, Smith, Charles E., Qi, Jenson, Wang, Yuanping, Haertlein, Barbara, Parry, Tom J., Li, Jian, Almond, Harold R., Minor, Lisa K., Damiano, Bruce P., Kinney, William A., Maryanoff, Bruce E., Lawson, Edward C.

“…Various 4-phenylpiperidine-benzoxazin-3-ones were synthesized and biologically evaluated as urotensin-II (U-II) receptor antagonists. Compound 12i was…”
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Nonpeptidic, Noncovalent Inhibitors of the Cysteine Protease Cathepsin S by Thurmond, Robin L, Beavers, Mary Pat, Cai, Hui, Meduna, Steven P, Gustin, Darin J, Sun, Siquan, Almond, Harold J, Karlsson, Lars, Edwards, James P

“…The first nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S (CatS) are described. Electronic database searching using the program DOCK…”
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Nonpeptide Inhibitors of Cathepsin G:  Optimization of a Novel β-Ketophosphonic Acid Lead by Structure-Based Drug Design by Greco, Michael N, Hawkins, Michael J, Powell, Eugene T, Almond, Harold R, Corcoran, Thomas W, de Garavilla, Lawrence, Kauffman, Jack A, Recacha, Rosario, Chattopadhyay, Debashish, Andrade-Gordon, Patricia, Maryanoff, Bruce E

“…The serine protease cathepsin G (EC 3.4.21.20; Cat G), which is stored in the azurophilic granules of neutrophils (polymorphonuclear leukocytes) and released…”
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α2 Adrenoceptor Agonists as Potential Analgesic Agents. 3. Imidazolylmethylthiophenes by Boyd, Robert E, Rasmussen, C. Royce, Press, Jeffery B, Raffa, Robert B, Codd, Ellen E, Connelly, Charlene D, Li, Quan S, Martinez, Rebecca P, Lewis, Martin A, Almond, Harold R, Reitz, Allen B

“…A series of imidazolylmethylthiophenes has been prepared and evaluated as ligands for the α2 adrenoceptor. These compounds were tested in two animal models…”
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In-Depth Study of Tripeptide-Based α-Ketoheterocycles as Inhibitors of Thrombin. Effective Utilization of the S1‘ Subsite and Its Implications to Structure-Based Drug Design by Costanzo, Michael J, Almond, Harold R, Hecker, Leonard R, Schott, Mary R, Yabut, Stephen C, Zhang, Han-Cheng, Andrade-Gordon, Patricia, Corcoran, Thomas W, Giardino, Edward C, Kauffman, Jack A, Lewis, Joan M, de Garavilla, Lawrence, Haertlein, Barbara J, Maryanoff, Bruce E

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Stereoselective synthesis of β-aryl-β-amino esters by Cohen, Judith H, Abdel-Magid, Ahmed F, Almond, Harold R, Maryanoff, Cynthia A

“…An efficient stereoselective synthesis of β-aryl-β-amino esters via reduction of enantiomerically enriched N-( p-methoxy-α-methylbenzyl)enamines by catalytic…”
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Aroyl(aminoacyl)pyrroles, a New Class of Anticonvulsant Agents by Carson, John R, Carmosin, Richard J, Pitis, Philip M, Vaught, Jeffry L, Almond, Harold R, Stables, James P, Wolf, Harold H, Swinyard, Ewart A, White, H. Steve

“…2-Aroyl-4-(ω-aminoacyl)- (4) and 4-aroyl-2-(ω-aminoacyl)pyrroles (9) represent a new, structurally novel class of anticonvulsant agents. Compounds of type 4…”
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2-Substituted 1-azabicycloalkanes, a new class of non-opiate antinociceptive agents by Carson, John R, Carmosin, Richard J, Vaught, Jeffry L, Gardocki, Joseph F, Costanzo, Michael J, Raffa, Robert B, Almond, Harold R

“…2-Substituted 1-azabicycloalkanes (3- and 5-aryloctahydroindolizines 2 and 11, 3-cyclohexyloctahydroindolizine 12, 4-aryloctahydroquinolizines 13, and…”
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Stereochemistry and conformation of a nitrogen-containing, medium-sized ring: hexahydro-1-phenyl-3-benzazonine derivatives. High 1,4-diastereoselectivity in hydrogenation of an exocyclic alkene by Maryanoff, Bruce E, Almond, Harold R

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Stereospecific enammonium-iminium rearrangements in a benzo[a]quinolizidine system by Maryanoff, Bruce E, McComsey, David F, Leo, Gregory C, Almond, Harold R

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Dramatic reversal of diastereoselectivity in an N-acyliminium ion cyclization leading to hexahydropyrrolo[2,1-a]isoquinolines. A case of competing steric interactions by Maryanoff, Bruce E, McComsey, David F, Almond, Harold R, Mutter, Martin S, Bemis, Guy W, Whittle, Robert R, Olofson, R. A

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In-Depth Study of Tripeptide-Based α-Ketoheterocycles as Inhibitors of Thrombin. Effective Utilization of the S 1 ‘ Subsite and Its Implications to Structure-Based Drug Design by Costanzo, Michael J., Almond, Harold R., Hecker, Leonard R., Schott, Mary R., Yabut, Stephen C., Zhang, Han-Cheng, Andrade-Gordon, Patricia, Corcoran, Thomas W., Giardino, Edward C., Kauffman, Jack A., Lewis, Joan M., de Garavilla, Lawrence, Haertlein, Barbara J., Maryanoff, Bruce E.

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(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines:  Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitors with Broad Antiproliferative Activity against Tumor Cells by Ho, Chih Y, Ludovici, Donald W, Maharoof, Umar S. M, Mei, Jay, Sechler, Jan L, Tuman, Robert W, Strobel, Eric D, Andraka, Laura, Yen, Hwa-Kwo, Leo, Gregory, Li, Jian, Almond, Harold, Lu, Hong, DeVine, Ann, Tominovich, Rose M, Baker, Judith, Emanuel, Stuart, Gruninger, Robert H, Middleton, Steven A, Johnson, Dana L, Galemmo, Robert A

“…A series of (6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines has been optimized to preserve both potent kinase inhibition activity against the…”
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Detailed rate studies on the Wittig reaction of nonstabilized phosphorus ylides via phosphorus-31, proton, carbon-13 NMR spectroscopy. Insight into kinetic vs. thermodynamic control of stereochemistry by Maryanoff, Bruce E, Reitz, Allen B, Mutter, Martin S, Inners, Ruth R, Almond, Harold R

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