Search Results - "Dickinson, Roger P"

A Potent, Selective Inhibitor of Matrix Metalloproteinase-3 for the Topical Treatment of Chronic Dermal Ulcers by Fray, M. Jonathan, Dickinson, Roger P, Huggins, John P, Occleston, Nicholas L

“…The pathology of chronic dermal ulcers is characterized by excessive proteolytic activity which degrades extracellular matrix (required for cell migration) and…”
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The design and synthesis of a novel series of indole derived selective ETA antagonists by RAWSON, David J, DACK, Kevin N, DICKINSON, Roger P, JAMES, Kim

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Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines by Fish, Paul V, Barber, Christopher G, Brown, David G, Butt, Richard, Collis, Michael G, Dickinson, Roger P, Henry, Brian T, Horne, Valerie A, Huggins, John P, King, Elizabeth, O'Gara, Margaret, McCleverty, Dawn, McIntosh, Fraser, Phillips, Christopher, Webster, Robert

“…1-Isoquinolinylguanidines were previously disclosed as potent and selective inhibitors of urokinase-type plasminogen activator (uPA). Further investigation of…”
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A novel series of highly selective inhibitors of MMP-3 by Whitlock, Gavin A., Dack, Kevin N., Dickinson, Roger P., Lewis, Mark L.

“…The design and synthesis of a series of highly selective hydroxamate inhibitors of MMP-3 is described. Substitution of a 4-biaryl piperidine sulfonamide core…”
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Absorption, Distribution, Metabolism, and Excretion Considerations in Selection of Orally Active Indole-Containing Endothelin Antagonist by WALKER, Donald K, DACK, Kevin N, DICKINSON, Roger P, FENNER, Katherine S, JAMES, Kim, RAWSON, David J, SMITH, Dennis A

“…A series of potent indole-containing endothelin antagonists were evaluated in rat pharmacokinetic studies as part of a rational drug design program. Early…”
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Thromboxane Modulating Agents. 3. 1H-Imidazol-1-ylalkyl- and 3-Pyridinylalkyl-Substituted 3-[2-[(Arylsulfonyl)amino]ethyl]benzenepropanoic Acid Derivatives as Dual Thromboxane Synthase Inhibitor/Thromboxane Receptor Antagonists by Dickinson, Roger P, Dack, Kevin N, Long, Clive J, Steele, John

“…The design of a series of dual thromboxane synthase inhibitor/thromboxane receptor antagonists based on a 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid…”
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Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-Isoquinolinylguanidines by Barber, Christopher G., Dickinson, Roger P., Fish, Paul V.

“…A series of 1-isoquinolinylguanidines are selective inhibitors of uPA. Compound 13j (UK-356,202) combines excellent potency and selectivity, and has been…”
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Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines by Barber, Christopher G, Dickinson, Roger P

“…Based on previous modeling predictions, a series of (3-substituted-5-chloro-2-pyridinyl)guanidines have been designed with good potency and selectivity for…”
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Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines by Barber, Christopher G, Dickinson, Roger P, Horne, Valerie A

“…The identification of 2-pyridinylguanidines (e.g., 27 and 28) as selective inhibitors of urokinase-type plasminogen activator (uPA) is described. The X-ray…”
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Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3′ group chirality by Fray, M.Jonathan, Burslem, M.Frank, Dickinson, RogerP

“…Structure–activity relationships are described for a series of succinyl hydroxamic acids 1a– o and their carboxylic acid analogues 2a– o as inhibitors of…”
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Selective thromboxane synthetase inhibitors. 3. 1H-Imidazol-1-yl-substituted benzo[b]furan-, benzo[b]thiophene- and indole-2- and 3-carboxylic acids by Cross, Peter E, Dickinson, Roger P, Parry, M. John, Randall, Michael J

“…The preparation of a series of 1H-imidazol-1-yl-substituted benzo[b]furan-, benzo[b]thiophene-, and indolecarboxylic acids is described. Most of the compounds…”
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Electrophysiologic properties of UK-66,914, a novel class III antiarrhythmic agent by Gwilt, M, Dalrymple, H W, Burges, R A, Blackburn, K J, Dickinson, R P, Cross, P E, Higgins, A J

“…A class III antiarrhythmic agent that preferentially increases the effective refractory period without altering conduction velocity holds considerable promise…”
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Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles by Cross, Peter E, Dickinson, Roger P, Parry, M. John, Randall, Michael J

“…1-(2-Phenoxyethyl)-1H-imidazole was found to be an inhibitor of thromboxane (TxA2) synthetase, but it also inhibited the adrenal cytochrome P-450 enzyme…”
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Selective thromboxane synthetase inhibitors. 2. 3-(1H-Imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogs by Cross, Peter E, Dickinson, Roger P, Parry, M. John, Randall, Michael J

“…The preparation of a series of 3-(1H-imidazol-1-ylmethyl)-1H-indole-1-alkanoic acids is described. Several compounds were found to be more potent thromboxane…”
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Selective thromboxane synthetase inhibitors. 4. 2-(1H-Imidazol-1-ylmethyl)benzo[b]furan-, -benzo[b]thiophene-, -indole- and -naphthalenecarboxylic acids by Cross, Peter E, Dickinson, Roger P, Parry, M. John, Randall, Michael J

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Promotion of carbohydrate oxidation in the heart by some phenylglyoxylic acids by Barnish, Ian T, Cross, Peter E, Danilewicz, John C, Dickinson, Roger P, Stopher, David A

“…A series of phenylglyoxylic acids is described, many of which are able to promote carbohydrate oxidation in muscle tissue, thereby favorably altering the…”
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Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 2. Imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamides by Barnish, Ian T, Cross, Peter E, Dickinson, Roger P, Gadsby, Brian, Parry, Michael J, Randall, Michael J, Sinclair, Ian W

“…A series of imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamide carbonic anhydrase inhibitors is described and their anticonvulsant activities are…”
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Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 3. 5-(Arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides by Barnish, Ian T, Cross, Peter E, Dickinson, Roger P, Parry, Michael J, Randall, Michael J

“…A series of 5-(arylthio)-, 5-(arylsulfinyl)-, and 5-(arylsulfonyl)thiophene-2-sulfonamides is described and anticonvulsant activities are listed for the…”
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Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (Stromelysin-1) by Fray, M.Jonathan, Dickinson, RogerP

“…Structure–activity relationships are described for a series of succinyl hydroxamic acids 4a– o as potent and selective inhibitors of matrix metalloprotease-3…”
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Novel antifungal 2-aryl-1-(1 H-1,2,4-triazol-1-yl)butan-2-ol derivatives with high activity against Aspergillus fumigatus by Dickinson, Roger P., Bell, Andrew S., Hitchcock, Christopher A., Narayanaswami, Subramaniyan, Ray, Stephen J., Richardson, Kenneth, Troke, Peter F.

“…Replacement of one triazole ring of fluconazole with 4-pyridinyl leads to an increase in activity against Aspergillus fumigatus. Introduction of an α-methyl…”
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