Search Results - "Kaltenbronn, James S"

Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites by Kaltenbronn, James S, Hudspeth, J. P, Lunney, E. A, Michniewicz, B. M, Nicolaides, E. D, Repine, J. T, Roark, W. H, Stier, M. A, Tinney, F. J

“…Renin inhibitors having 13 different isosteres connecting the P3 and P2 positions have been prepared. Synthetic routes and in vitro activity exhibited by these…”
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Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors by Doherty, Annette M, Sircar, Ila, Kornberg, Brian E, Quin, John, Winters, R. Thomas, Kaltenbronn, James S, Taylor, Michael D, Batley, Brian L, Rapundalo, Stephen R

“…A series of primate renin inhibitors containing difluorocarbinol and difluoroketone groups at the P1-P1' position have been synthesized and studied both in…”
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C-Terminal Modifications of Histidyl-N-benzylglycinamides To Give Improved Inhibition of Ras Farnesyltransferase, Cellular Activity, and Anticancer Activity in Mice by McNamara, Dennis J, Dobrusin, Ellen, Leonard, Daniele M, Shuler, Kevon R, Kaltenbronn, James S, Quin, John, Bur, Scott, Thomas, Charles E, Doherty, Annette M, Scholten, Jeffrey D, Zimmerman, Karen K, Gibbs, Barbara S, Gowan, Richard C, Latash, Michael P, Leopold, Wilbur R, Przybranowski, Sally A, Sebolt-Leopold, Judith S

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Design and Synthesis of Renin Inhibitors: Incorporation of Transition-State Isostere Side Chains That Span from the S1 to the S3 Binding Pockets and Examination of P3-Modified Renin Inhibitors by Shahripour, Aurash, Kaltenbronn, James S, Lunney, Elizabeth A, Steinbaugh, Bruce A, Hamby, James M, Hamilton, Harriet W, Sawyer, Tomi K, Humblet, Christine, Doherty, Annette M

“…A series of renin inhibitors were designed to examine the topography of the contiguous binding pocket of renin that is normally occupied by the P1 and P3 side…”
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Analyses of ligand binding in five endothiapepsin crystal complexes and their use in the design and evaluation of novel renin inhibitors by Lunney, Elizabeth A, Hamilton, Harriet W, Hodges, John C, Kaltenbronn, James S, Repine, Joseph T, Badasso, Mohammed, Cooper, Jon B, Dealwis, Chris, Wallace, Bonnie A

“…Five renin inhibitors were cocrystallized with endothiapepsin, a fungal enzyme homologous to renin. Crystal structures of inhibitor-bound complexes have…”
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CI-867, a new broad-spectrum semisynthetic penicillin by Kaltenbronn, J S, Haskell, T H, Doub, L, Knoble, J, DeJohn, D, Krolls, U, Jenesel, N, Huang, G G, Heifetz, C L, Fisher, M W

“…The synthesis and antimicrobial activity of a new semisynthetic penicillin are described. Both in vitro and in vivo, the compound shows promising antibacterial…”
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Structure-activity relationships of the potent combined endothelinA/endothelinB receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21 (PD 142893): development of endothelinB receptor selective antagonists by Cody, Wayne L, He, John X, DePue, Patricia L, Waite, Lisa A, Leonard, Daniele M, Sefler, Andrea M, Kaltenbronn, James S, Haleen, Stephen J, Walker, Donnelle M, Flynn, Michael A, Welch, Kathleen, Reynolds, Elwood E, Doherty, Annette M

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New inhibitors of human renin that contain novel replacements at the P2 site by Doherty, Annette M, Kaltenbronn, James S, Hudspeth, James P, Repine, Joseph T, Roark, William H, Sircar, Ila, Tinney, Frank J, Connolly, Cleo J, Hodges, John C

“…A series of renin inhibitors with novel modifications at the P2 site has been prepared. Structure-activity relationships reveal that for a particular P2…”
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Renin inhibitors containing .alpha.-heteroatom amino acids as P2 residues by Repine, Joseph T, Kaltenbronn, James S, Doherty, Annette M, Hamby, James M, Himmelsbach, Richard J, Kornberg, Brian E, Taylor, Michael D, Lunney, ELizabeth A, Humblet, Christine

“…A series of renin inhibitors having alpha-heteroatom amino acids as P2 substitutions has been prepared. Examples where the heteroatom is oxygen, sulfur, or…”
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Renin inhibitors containing esters at the P2-position. Oral activity in a derivative of methyl aminomalonate by Repine, Joseph T, Himmelsbach, Richard J, Hodges, John C, Kaltenbronn, James S, Sircar, Ila, Skeean, Richard W, Brennan, Sean T, Hurley, Timothy R, Lunney, Elizabeth

“…A series of renin inhibitors containing ester side chains at the P2 subsite are potent inhibitors of primate renin. Derivatives containing the diol isostere…”
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4- and 5-Aryl-1-naphthaleneacetic acids as antiinflammatory agents by Kaltenbronn, James S

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Antiinflammatory activity of isomeric phenylnaphthaleneacetic acids by Kaltenbronn, James S

“…The isomeric phenylnaphthaleneacetic acids were prepared and tested for antiinflammatory activity by the anti-UV-erythema method. High potency was exhibited by…”
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Synthesis of a Bromine-Rich Marine Antibiotic by Hanessian, Stephen, Kaltenbronn, James S

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4-(and 5-)(2-Thienyl)-1-naphthaleneacetic acids as antiinflammatory agents by Kaltenbronn, James S, Rhee, Tae O

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Semisynthetic penicillins and cephalosporins containing the substituted 6-vinyl-1,2-dihydro-2-oxo- and 1,4-dihydro-4-oxo-3-pyridinecarboxylic acid side chains. Synthesis and structure-activity relationships by DeJohn, D, Domagala, J M, Haskell, T H, Heifetz, C L, Huang, G G, Kaltenbronn, J S, Krolls, U

“…A series of penicillins and cephalosporins containing the substituted 6-vinyl-1,2-dihydro-2-oxo- and 1,4-dihydro-4-oxo-3-pyridinecarboxylic acid side chains…”
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5-Aryl-2-furanacetic acids by Kaltenbronn, James S, Rhee, Tae O

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Evaluation of Physicochemical Parameters Important to the Oral Bioavailability of Peptide-like Compounds: Implications for the Synthesis of Renin Inhibitors by Hamilton, Harriet W, Steinbaugh, Bruce A, Stewart, Barbra H, Chan, O. Helen, Schmid, Heidi L, Schroeder, Richard, Ryan, Michael J, Keiser, Joan, Taylor, Michael D

“…A series of radiolabeled compounds related to renin inhibitor structures was synthesized to represent a range of physicochemical properties. These compounds…”
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Functionalization of substituted 2(1H)- and 4(1H)-pyridones. III. The preparation of substituted 6-Vinyl-1,2-dihydro-2-oxo- and 1,4-dihydro-4-oxo-3-pyridinecarboxylic acids through the chemistry of pyridone dianions by Dejohn, Dana, Domagala, John M., Kaltenbronn, James S., Krolls, Uldis

“…The synthesis of various substituted 6‐vinyl‐1,2‐dihydro‐2‐oxo‐3‐pyridinecarboxylic acids from the dianions of…”
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