Search Results - "Watson, Nigel S."

Factor Xa Inhibitors:  S1 Binding Interactions of a Series of N-{(3S)-1-[(1S)-1-Methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides by Chan, Chuen, Borthwick, Alan D, Brown, David, Burns-Kurtis, Cynthia L, Campbell, Matthew, Chaudry, Laiq, Chung, Chun-wa, Convery, Máire A, Hamblin, J. Nicole, Johnstone, Lisa, Kelly, Henry A, Kleanthous, Savvas, Patikis, Angela, Patel, Champa, Pateman, Anthony J, Senger, Stefan, Shah, Gita P, Toomey, John R, Watson, Nigel S, Weston, Helen E, Whitworth, Caroline, Young, Robert J, Zhou, Ping

“…Factor Xa inhibitory activities for a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides with different P1…”
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Arylsulfonamides: A study of the relationship between activity and conformational preferences for a series of factor Xa inhibitors by Senger, Stefan, Convery, Máire A., Chan, Chuen, Watson, Nigel S.

“…Torsional scans of sulfonamide S–C bonds in small model systems of a series of arylsulfonamide factor Xa inhibitors were performed in order to investigate if…”
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Sulfonamide-related conformational effects and their importance in structure-based design by Senger, Stefan, Chan, Chuen, Convery, Máire A., Hubbard, Julia A., Shah, Gita P., Watson, Nigel S., Young, Robert J.

“…An example is presented where structural information combined with ab initio calculations clearly indicate that an observed difference in biological activity…”
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The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs by Watson, Nigel S., Adams, Carl, Belton, David, Brown, David, Burns-Kurtis, Cynthia L., Chaudry, Laiq, Chan, Chuen, Convery, Máire A., Davies, David E., Exall, Anne M., Harling, John D., Irvine, Stephanie, Irving, Wendy R., Kleanthous, Savvas, McLay, Iain M., Pateman, Anthony J., Patikis, Angela N., Roethke, Theresa J., Senger, Stefan, Stelman, Gary J., Toomey, John R., West, Robert I., Whittaker, Caroline, Zhou, Ping, Young, Robert J.

“…The discovery of potent and long-acting series of orally available factor Xa inhibitors with tetrahydroisoquinoline and benzazepine motifs is described. The…”
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Structure- and property-based design of factor Xa inhibitors: Pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs by Young, Robert J., Campbell, Matthew, Borthwick, Alan D., Brown, David, Burns-Kurtis, Cynthia L., Chan, Chuen, Convery, Máire A., Crowe, Miriam C., Dayal, Satish, Diallo, Hawa, Kelly, Henry A., Paul King, N., Kleanthous, Savvas, Mason, Andrew M., Mordaunt, Jackie E., Patel, Champa, Pateman, Anthony J., Senger, Stefan, Shah, Gita P., Smith, Paul W., Watson, Nigel S., Weston, Helen E., Zhou, Ping

“…The synthesis and profiles of a series of fXa inhibitors with acyclic alanyl amide P4 motifs is described, which includes potent examples showing highly…”
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Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs by Young, Robert J., Adams, Carl, Blows, Mike, Brown, David, Burns-Kurtis, Cynthia L., Chan, Chuen, Chaudry, Laiq, Convery, Máire A., Davies, David E., Exall, Anne M., Foster, Graham, Harling, John D., Hortense, Eric, Irvine, Stephanie, Irving, Wendy R., Jackson, Steve, Kleanthous, Savvas, Pateman, Anthony J., Patikis, Angela N., Roethka, Theresa J., Senger, Stefan, Stelman, Gary J., Toomey, John R., West, Robert I., Whittaker, Caroline, Zhou, Ping, Watson, Nigel S.

“…The discovery of potent series of orally available factor Xa inhibitors with aminoindane and phenylpyrrolidine motifs is described. The rational design,…”
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Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with biaryl P4 motifs by Young, Robert J., Borthwick, Alan D., Brown, David, Burns-Kurtis, Cynthia L., Campbell, Matthew, Chan, Chuen, Charbaut, Marie, Chung, Chun-wa, Convery, Máire A., Kelly, Henry A., Paul King, N., Kleanthous, Savvas, Mason, Andrew M., Pateman, Anthony J., Patikis, Angela N., Pinto, Ivan L., Pollard, Derek R., Senger, Stefan, Shah, Gita P., Toomey, John R., Watson, Nigel S., Weston, Helen E.

“…Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl…”
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Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs by Kleanthous, Savvas, Borthwick, Alan D., Brown, David, Burns-Kurtis, Cynthia L., Campbell, Matthew, Chaudry, Laiq, Chan, Chuen, Clarte, Marie-Olive, Convery, Máire A., Harling, John D., Hortense, Eric, Irving, Wendy R., Irvine, Stephanie, Pateman, Anthony J., Patikis, Angela N., Pinto, Ivan L., Pollard, Derek R., Roethka, Theresa J., Senger, Stefan, Shah, Gita P., Stelman, Gary J., Toomey, John R., Watson, Nigel S., West, Robert I., Whittaker, Caroline, Zhou, Ping, Young, Robert J.

“…The discovery of a potent series of orally available Factor Xa inhibitors with monoaryl P4 motifs is described. Structure and property based drug design was…”
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Structure and property based design of factor Xa inhibitors: Biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs by Young, Robert J., Borthwick, Alan D., Brown, David, Burns-Kurtis, Cynthia L., Campbell, Matthew, Chan, Chuen, Charbaut, Marie, Convery, Máire A., Diallo, Hawa, Hortense, Eric, Irving, Wendy R., Kelly, Henry A., King, N. Paul, Kleanthous, Savvas, Mason, Andrew M., Pateman, Anthony J., Patikis, Angela N., Pinto, Ivan L., Pollard, Derek R., Senger, Stefan, Shah, Gita P., Toomey, John R., Watson, Nigel S., Weston, Helen E., Zhou, Ping

“…Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic…”
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Selective and dual action orally active inhibitors of thrombin and factor Xa by Young, Robert J., Brown, David, Burns-Kurtis, Cynthia L., Chan, Chuen, Convery, Máire A., Hubbard, Julia A., Kelly, Henry A., Pateman, Anthony J., Patikis, Angela, Senger, Stefan, Shah, Gita P., Toomey, John R., Watson, Nigel S., Zhou, Ping

“…The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. The observed…”
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Antithrombotic Potential of GW813893: A Novel, Orally Active, Active-site Directed Factor Xa Inhibitor by Abboud, Melanie A, Needle, Saul J, Burns-Kurtis, Cynthia L, Valocik, Richard E, Koster, Paul F, Amour, Augustin J, Chan, Chuen, Brown, David, Chaudry, Laiq, Zhou, Ping, Patikis, Angela, Patel, Champa, Pateman, Anthony J, Young, Rob J, Watson, Nigel S, Toomey, John R

“…BACKGROUND:Factor Xa (FXa) has been a target of considerable interest for drug development efforts aimed at suppressing thrombosis. In this report, a new…”
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Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors by Watson, Nigel S., Brown, David, Campbell, Matthew, Chan, Chuen, Chaudry, Laiq, Convery, Máire A., Fenwick, Rebecca, Hamblin, J. Nicole, Haslam, Claudine, Kelly, Henry A., King, N. Paul, Kurtis, Cynthia L., Leach, Andrew R., Manchee, Gary R., Mason, Andrew M., Mitchell, Charlotte, Patel, Champa, Patel, Vipulkumar K., Senger, Stefan, Shah, Gita P., Weston, Helen E., Whitworth, Caroline, Young, Robert J.

“…The synthesis is reported of the potent, selective fXa inhibitor 24 which shows highly encouraging rat and dog pharmacokinetic profiles and excellent oral…”
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The squalestatins, novel inhibitors of squalene synthase produced by a species of Phoma. II. Structure elucidation by Sidebottom, P J, Highcock, R M, Lane, S J, Procopiou, P A, Watson, N S

“…Three novel fungal metabolites 1-3 isolated from cultures of a Phoma sp. C2932, are potent and selective inhibitors of squalene synthase. Their structures have…”
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Thrombin inhibitors based on [5,5] trans-fused indane lactams by Pass, Martin, Abu-Rabie, Said, Baxter, Andrew, Conroy, Richard, Coote, Steven J, Craven, Andrew P, Finch, Harry, Hindley, Seán, Kelly, Henry A, Lowdon, Andrew W, McDonald, Edward, Mitchell, William L, Pegg, Neil A, Procopiou, Pan A, Ramsden, Nigel G, Thomas, Rhian, Walker, Dawn A, Watson, Nigel S, Jhoti, Harren, Mooney, Christopher J, Tang, Chi-Man, Thomas, Pamela J, Parry, Simon, Patel, Champa

“…A series of trans-fused lactams containing the indane nucleus has been prepared. Compound 19 has much enhanced plasma stability compared with its lactone…”
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The squalestatins: Synthesis of c-4 carboxamide derivatives by Chan, Chuen, Scicinski, Jan J, Srikantha, Anton Rp, Watson, Nigel S

“…Synthesis of squalcstalin S1 C-4 carboxamide, 2, as well as related C-4 amides and C-4 hydroxymethyl derivatives possessing a C-3 hydroxymethyl group (15 and…”
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The Squalestatins:  Decarboxy and 4-Deoxy Analogues as Potent Squalene Synthase Inhibitors by 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, Sharratt, Peter J, Snowden, Michael A, Watson, Nigel S

“…Squalestatins without either the hydroxy group at C-4 or the carboxylic acid at C-3 or C-4 were prepared and evaluated for their ability to inhibit rat liver…”
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Inhibitors of cholesterol biosynthesis. 2. 3,5-Dihydroxy-7-(N-pyrrolyl)-6-heptenoates, a novel series of HMG-CoA reductase inhibitors by Procopiou, Panayiotis A, Draper, Christopher D, Hutson, Julie L, Inglis, Graham G. A, Ross, Barry C, Watson, Nigel S

“…A series of 7-[2,3-diaryl-5-(1-methylethyl)-1H-pyrrol-1-yl]-3,5- dihydroxy-6-heptenoates was prepared and evaluated for its ability to inhibit the enzyme…”
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The Squalestatins:  Inhibitors of Squalene Synthase. Enzyme Inhibitory Activities and in Vivo Evaluation of C3-Modified Analogues by Procopiou, Panayiotis A, Cox, Brian, Kirk, Barrie E, Lester, Michael G, McCarthy, Alun D, Sareen, Meenu, Sharratt, Peter J, Snowden, Michael A, Spooner, Stephen J, Watson, Nigel S, Widdowson, Julia

“…Squalestatin analogues modified at C3 were prepared and evaluated for their ability to inhibit rat liver microsomal squalene synthase in vitro. While the…”
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Squalestatin 1, a potent inhibitor of squalene synthase, which lowers serum cholesterol in vivo by BAXTER, A, FITZGERALD, B. J, WRIGHT, C, HUTSON, J. L, MCCARTHY, A. D, MOTTERAM, J. M, ROSS, B. C, SAPRA, M, SNOWDEN, M. A, WATSON, N. S, WILLIAMS, R. J

“…Squalestatin 1 is a member of a novel family of fermentation products isolated from a previously unknown Phoma species (Coelomycetes). Squalestatin 1 is a…”
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The squalestatins: tricyclic 3,4-β-lactone and 3,4-oxetane systems by Cox, Brian, Morley, Nicolas, Procopiou, Panayiotis A, Sharratt, Peter J, Watson, Nigel S, Wild, Deborah

“…Squalestatin 3,4-β-lactone-4,5-dimethyl ester ( 8) was reductively ring-opened to yield squalestatin 3-hydroxymethyl-4,5-dimethyl ester ( 6) using mild…”
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