Search Results - "Breslin, HJ"

Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist/ µ opioid receptor antagonist by Wade, PR, Palmer, JM, McKenney, S, Kenigs, V, Chevalier, K, Moore, BA, Mabus, JR, Saunders, PR, Wallace, NH, Schneider, CR, Kimball, ES, Breslin, HJ, He, W, Hornby, PJ

“…BACKGROUND & PURPOSE Loperamide is a selective µ opioid receptor agonist acting locally in the gastrointestinal (GI) tract as an effective anti‐diarrhoeal but…”
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Novel triazole based inhibitors of Ras farnesyl transferase by Saha, Ashis K., Liu, Li, Simoneaux, Richard, DeCorte, Bart, Meyer, Christophe, Skrzat, Stacy, Breslin, Henry J., Kukla, Michael J., End, Dave W.

“…A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore ( 5) is described. These inhibitors were discovered…”
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Identification of potent phenyl imidazoles as opioid receptor agonists by Breslin, Henry J., Cai, Chaozhong, Miskowski, Tamara A., Coutinho, Santosh V., Zhang, Sui-Po, Hornby, Pamela, He, Wei

“…Using previously reported opioid receptor (OR) agonist analogs 4a– c as starting points, the structure–activity relationship (SAR) for their related series has…”
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A convenient, large-scale synthesis of 4′-carboxamido N-Boc-2′,6′-dimethyl- l-phenylalanines by Cai, Chaozhong, Breslin, Henry J., He, Wei

“…A large-scale synthesis of a series of 4′-carboxamido N-Boc-2′,6′-dimethyl- l-phenylalanines is described. This method features mild reaction conditions and…”
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Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives by Pauwels, Rudi, Andries, Koen, Desmyter, Jan, Schols, Dominique, Kukla, Michael J, Breslin, Henry J, Raeymaeckers, Alfons, Gelder, Jozef Van, Woestenborghs, Robert, Heykants, Jozef, Schellekens, Karel, Janssen, Marcel A. C, Clercq, Erik De, Janssen, Paul A. J

“…In the search for compounds active against human immunodeficiency virus (HIV), we have found that members of a novel series of…”
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Tripeptidyl-peptidase II (TPP II) inhibitory activity of (S)-2,3-dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a systematic SAR evaluation. Part 2 by BRESLIN, Henry J, MISKOWSKI, Tamara A, KUKLA, Michael J, DE WINTER, Hans L, SOMERS, Maria V. F, ROEVENS, Peter W. M, KAVASH, Robert W

“…We have systematically explored the structure-activity relationship (SAR) for a series of compounds 2 as inhibitors of tripeptidyl-peptidase II (TPP II), a…”
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Rationale, Design, and Synthesis of Novel Phenyl Imidazoles as Opioid Receptor Agonists for Gastrointestinal Disorders by Breslin, Henry J, Miskowski, Tamara A, Rafferty, Bryan M, Coutinho, Santosh V, Palmer, Jeffrey M, Wallace, Nathaniel H, Schneider, Craig R, Kimball, Edward S, Zhang, Sui-Po, Li, Jian, Colburn, Raymond W, Stone, Dennis J, Martinez, Rebecca P, He, Wei

“…A small series of novel, imidazoles 4 have been prepared that exhibit very good binding affinities for the δ and μ opioid receptors (ORs), as well as…”
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Synthesis and Anti-HIV-1 Activity of 4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) Derivatives. 3 by Breslin, Henry J, Kukla, Michael J, Ludovici, Donald W, Mohrbacher, Richard, Ho, Winston, Miranda, Milton, Rodgers, James D, Hitchens, T. Kevin, Leo, Gregory

“…4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2 (1H)-ones (TIBO), 1, have been shown to significantly inhibit HIV-1 replication in vitro by…”
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Design, Synthesis, and Tripeptidyl Peptidase II Inhibitory Activity of a Novel Series of (S)-2,3-Dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles by Breslin, Henry J, Miskowski, Tamara A, Kukla, Michael J, Leister, William H, De Winter, Hans L, Gauthier, Diane A, Somers, Maria V. F, Peeters, Daniëlle C. G, Roevens, Peter W. M

“…Butabindide, 1, was previously reported as a potent inhibitor (IC50 = 7 nM) of the serine protease enzyme tripeptidyl peptidase II (TPPII), an endogenous…”
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Synthesis and Anti-HIV-1 Activity of 4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TlBO) Derivatives. 4 by Ho, Winston, Kukla, Michael J, Breslin, Henry J, Ludovici, Donald W, Grous, Philip P, Diamond, Craig J, Miranda, Milton, Rodgers, James D, Ho, Chih Y

“…In previous papers, we have described the discovery of a new series of compounds, 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1 H)- ones,…”
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Synthesis and anti-HIV activity of 1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one (TBO) derivatives. truncated 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-ones (TIBO) analogues by Breslin, Henry J., Kukla, Michael J., Kromis, Teresa, Cullis, Heather, De Knaep, Fons, Pauwels, Rudi, Andries, Koen, De Clercq, Erik, Janssen, Marcel A.C., Janssen, Paul A.J.

“…4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-ones (TIBO), 1, have been shown to significantly inhibit HIV-1 replication, as reported in…”
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New tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione derivatives are potent inhibitors of human immunodeficiency virus type 1 replication and are synergistic with 2',3'-dideoxynucleoside analogs by PAUWELS, R, ANDRIES, K, JANSSEN, P. A. J, DEBYSER, Z, KUKLA, M. J, SCHOLS, D, BRESLIN, H. J, WOESTENBORGHS, R, DESMYTER, J, JANSSEN, M. A. C, DE CLERCQ, E

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives. 2 by Kukla, Michael J, Breslin, Henry J, Diamond, Craig J, Grous, Philip P, Ho, Chih Y, Miranda, Milton, Rodgers, James D, Sherrill, Ronald G, De Clercq, Erik, Pauwels, Rudi, Andries, Koen, Moens, Luc J, Janssen, Marcel A. C, Janssen, Paul A. J

“…In the first paper of this series a new structure with anti-HIV-1 activity was disclosed and analogues were synthesized to explore the structure-activity…”
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Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives by Kukla, Michael J, Breslin, Henry J, Pauwels, Rudi, Fedde, Cynthia L, Miranda, Milton, Scott, Malcolm K, Sherrill, Ronald G, Raeymaekers, Alfons, Van Gelder, Jozef

“…A series of 6-substituted 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin- 2(1H)-ones (9) have been synthesized and tested for their ability to…”
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A novel series of N-(1-aminoalkylidene)carboximidamides as potential hypoglycemic agents by BRESLIN, H. J, KUKLA, M. J, TUMAN, R. W, REBARCHAK, M. C, BOWDEN, C. R

“…Nitrogen heterocyclic carboximidamides, such as linogliride, 1a, have been shown to possess significant hypoglycemic activity and have shown clinical efficacy…”
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Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo [4,5,1-jk][1,4] benzodiazepin-2(1H)-one (TIBO) derivatives by Breslin, HJ, Kukla, MJ, Ludovici, D W, Mohrbacher, R, Ho, Winston, Miranda, M, Rodgers, J D, Hitchens, T K, Leo, G, Gauthier, DA, Ho, Chih Y, Scott, M K, De Clercq, E, Pauwels, R

“…4,5,6,7-Tetrahydro 5-methylimidazo[4,5,1-jk] [1,4]benzodiazepin-2(1H)-ones (TIBO), 1, have been shown to significantly inhibit HIV-1 replication in vitro by…”
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Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo [4,5,1-jk][1,4] benzodiazepin 2(1H)-one (TlBO) derivatives by Ho, Winston, Kukla, MJ, Breslin, HJ, Ludovici, D W, Grous, P P, Diamond, C J, Miranda, M, Rodgers, J D, Ho, Chih Y, De Clercq, E, Pauwels, R, Andries, K, Janssen, MAC, Janssen, PAJ

“…In previous papers, we have described the discovery of a new series of compounds, 4,5,6,7-tetrahydro 5-methylimidazo[4,5,1-jk][1,4] benzodiazepin-2(1H)-ones ,…”
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Polycyclic heterocycles from glutaraldehyde in one reaction by Kukla, Michael J, Breslin, Henry J

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Antihypertensive dihydropyridines with 1,4,4-trisubstitution by Kukla, Michael J, Breslin, Henry J, Gill, Alan

“…Dihydropyridines with 1,4,4-trisubstitution were synthesized and tested for antihypertensive activity in a spontaneously hypertensive rat model. This…”
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A new implant for retinal detachment surgery by BRESLIN, H J

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