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Gerald Smith

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Chemicals & Drugs

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Jeffry B Franciskovich; John J Masters; Wayne W Weber; Valentine J Klimkowski; Michael Chouinard; Philip Sipes; Lea M Johnson; David W Snyder; Marcia K Chastain; Trelia J Craft; Richard D Towner; Donetta Gifford-Moore; Larry L Froelich; Jeffrey K Smallwood; Ronald S Foster; Gerald F Smith; John W Liebeschuetz; Christopher W Murray; Stephen C Young
Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors.
Valentine J Klimkowski; Brian M Watson; Michael R Wiley; John W Liebeschuetz; Jeffry B Franciskovich; Jothirajah Marimuthu; Jolie A Bastian; Daniel J Sall; Jeffrey K Smallwood; Nikolay Y Chirgadze; Gerald F Smith; Ronald S Foster; Trelia J Craft; Philip Sipes; Marcia K Chastain; Scott M Sheehan
D-phenylglycinol-derived non-covalent factor Xa inhibitors: effect of non-peptidic S4 linkage elements on affinity and anticoagulant activity.
David Mendel; Angela L Marquart; Sajan Joseph; Philip Waid; Ying K Yee; Anne Louise Tebbe; Andrew M Ratz; David K Herron; Theodore Goodson; John J Masters; Jeffry B Franciskovich; Jennifer M Tinsley; Michael R Wiley; Leonard C Weir; Jeffrey A Kyle; Valentine J Klimkowski; Gerald F Smith; Richard D Towner; Larry L Froelich; John Buben; Trelia J Craft
Anthranilamide inhibitors of factor Xa.

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All Publications

2007: Jeffry B Franciskovich; John J Masters; Wayne W Weber; Valentine J Klimkowski; Michael Chouinard; Philip Sipes; Lea M Johnson; David W Snyder; Marcia K Chastain; Trelia J Craft; Richard D Towner; Donetta Gifford-Moore; Larry L Froelich; Jeffrey K Smallwood; Ronald S Foster; Gerald F Smith; John W Liebeschuetz; Christopher W Murray; Stephen C Young
Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(24):6910-3.
2007: Valentine J Klimkowski; Brian M Watson; Michael R Wiley; John W Liebeschuetz; Jeffry B Franciskovich; Jothirajah Marimuthu; Jolie A Bastian; Daniel J Sall; Jeffrey K Smallwood; Nikolay Y Chirgadze; Gerald F Smith; Ronald S Foster; Trelia J Craft; Philip Sipes; Marcia K Chastain; Scott M Sheehan
D-phenylglycinol-derived non-covalent factor Xa inhibitors: effect of non-peptidic S4 linkage elements on affinity and anticoagulant activity.
Bioorganic & medicinal chemistry letters 2007;17(21):5801-5.
2007: David Mendel; Angela L Marquart; Sajan Joseph; Philip Waid; Ying K Yee; Anne Louise Tebbe; Andrew M Ratz; David K Herron; Theodore Goodson; John J Masters; Jeffry B Franciskovich; Jennifer M Tinsley; Michael R Wiley; Leonard C Weir; Jeffrey A Kyle; Valentine J Klimkowski; Gerald F Smith; Richard D Towner; Larry L Froelich; John Buben; Trelia J Craft
Anthranilamide inhibitors of factor Xa.
Bioorganic & medicinal chemistry letters 2007;17(17):4832-6.
2006: Brian J Eastwood; Mark W Farmen; Philip W Iversen; Trelia J Craft; Jeffrey K Smallwood; Kim E Garbison; Neil DeLapp; Gerald F Smith
The minimum significant ratio: a statistical parameter to characterize the reproducibility of potency estimates from concentration-response assays and estimation by replicate-experiment studies.
Journal of biomolecular screening 2006;11(3):253-61.
2005: Jeffry B Franciskovich; John J Masters; Jennifer M Tinsley; Trelia J Craft; Larry L Froelich; Donetta Gifford-Moore; Valentine J Klimkowski; Jeffrey K Smallwood; Gerald F Smith; Tommy Smith; Richard R Towner; Leonard C Weir; Michael R Wiley
Investigation of factor Xa inhibitors containing non-amidine S1 elements.
Bioorganic & medicinal chemistry letters 2005;15(21):4838-41.
2003: Scott M Sheehan; John J Masters; Michael R Wiley; Stephen C Young; John W Liebeschuetz; Stuart D Jones; Christopher W Murray; Jeffry B Franciskovich; David B Engel; Wayne W Weber; Jothirajah Marimuthu; Jeffrey A Kyle; Jeffrey K Smallwood; Mark W Farmen; Gerald F Smith
A four component coupling strategy for the synthesis of D-phenylglycinamide-derived non-covalent factor Xa inhibitors.
Bioorganic & medicinal chemistry letters 2003;13(14):2255-9.
2000: Kumiko Takeuchi; Jolie A Bastian; Donetta Gifford-Moore; RW Harper; S C Miller; Jeffrey T Mullaney; Daniel J Sall; Gerald F Smith; M Zhang; Matthew J Fisher
1,2-Disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: a novel series of thrombin inhibitors.
Bioorganic & medicinal chemistry letters 2000;10(20):2347-51.
2000: Kumiko Takeuchi; Todd J Kohn; RW Harper; Ho-Shen Lin; Donetta Gifford-Moore; Michael E Richett; Daniel J Sall; Gerald F Smith; M Zhang
Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. Part 6: further focus on the contracted C4'-side chain analogues.
Bioorganic & medicinal chemistry letters 2000;10(11):1199-202.
2000: John J Masters; Jeffry B Franciskovich; Jennifer M Tinsley; C Campbell; J B Campbell; Trelia J Craft; Larry L Froelich; Donetta Gifford-Moore; L A Hay; David K Herron; Valentine J Klimkowski; K D Kurz; J T Metz; Andrew M Ratz; RT Shuman; Gerald F Smith; Tommy Smith; Richard D Towner; Michael R Wiley; A Wilson; Ying K Yee
Non-amidine-containing 1,2-dibenzamidobenzene inhibitors of human factor Xa with potent anticoagulant and antithrombotic activity.
Journal of medicinal chemistry 2000;43(11):2087-92.
2000: Michael R Wiley; Leonard C Weir; S Briggs; N A Bryan; John Buben; C Campbell; Nikolay Y Chirgadze; R C Conrad; Trelia J Craft; James V Ficorilli; Jeffry B Franciskovich; Larry L Froelich; Donetta Gifford-Moore; Theodore Goodson; David K Herron; Valentine J Klimkowski; K D Kurz; Jeffrey A Kyle; John J Masters; Andrew M Ratz; G Milot; RT Shuman; Tommy Smith; Gerald F Smith; Anne Louise Tebbe; Jennifer M Tinsley
Structure-based design of potent, amidine-derived inhibitors of factor Xa: evaluation of selectivity, anticoagulant activity, and antithrombotic activity.
Journal of medicinal chemistry 2000;43(5):883-99.
2000: Ying K Yee; Anne Louise Tebbe; J H Linebarger; Douglas W Beight; Trelia J Craft; Donetta Gifford-Moore; Theodore Goodson; David K Herron; Valentine J Klimkowski; Jeffrey A Kyle; J Scott Sawyer; Gerald F Smith; Jennifer M Tinsley; Richard D Towner; Leonard C Weir; Michael R Wiley
N(2)-Aroylanthranilamide inhibitors of human factor Xa.
Journal of medicinal chemistry 2000;43(5):873-82.
2000: David K Herron; Theodore Goodson; Michael R Wiley; Leonard C Weir; Jeffrey A Kyle; Ying K Yee; Anne Louise Tebbe; Jennifer M Tinsley; David Mendel; John J Masters; Jeffry B Franciskovich; J Scott Sawyer; Douglas W Beight; Andrew M Ratz; G Milot; S E Hall; Valentine J Klimkowski; James H Wikel; Brian J Eastwood; Richard D Towner; Donetta Gifford-Moore; Trelia J Craft; Gerald F Smith
1,2-Dibenzamidobenzene inhibitors of human factor Xa.
Journal of medicinal chemistry 2000;43(5):859-72.
2000: Daniel J Sall; D L Bailey; Jolie A Bastian; John Buben; Nikolay Y Chirgadze; Amy Clemens-Smith; ML Denney; Matthew J Fisher; Deborah D Giera; Donetta Gifford-Moore; RW Harper; Lea M Johnson; Valentine J Klimkowski; Todd J Kohn; Ho-Shen Lin; JR McCowan; Alan D Palkowitz; Michael E Richett; Gerald F Smith; David W Snyder; Kumiko Takeuchi; JE Toth; M Zhang
Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 5. Potency, efficacy, and pharmacokinetic properties of modified C-3 side chain derivatives.
Journal of medicinal chemistry 2000;43(4):649-63.
2000: Nikolay Y Chirgadze; Daniel J Sall; Stephen L Briggs; David Clawson; M Zhang; Gerald F Smith; Richard Schevitz
The crystal structures of human alpha-thrombin complexed with active site-directed diamino benzo[b]thiophene derivatives: a binding mode for a structurally novel class of inhibitors.
Protein science : a publication of the Protein Society 2000;9(1):29-36.
1999: Michael R Wiley; Leonard C Weir; Stephen L Briggs; Nikolay Y Chirgadze; David Clawson; Donetta Gifford-Moore; A L Schacht; Gerald F Smith; Vasu Vasudevan; LL Zornes; Valentine J Klimkowski
The design of potent, selective, non-covalent, peptide thrombin inhibitors utilizing imidazole as a S1 binding element.
Bioorganic & medicinal chemistry letters 1999;9(18):2767-72.
1999: M Zhang; D L Bailey; Jolie A Bastian; Stephen L Briggs; Nikolay Y Chirgadze; David Clawson; ML Denney; Donetta Gifford-Moore; RW Harper; Lea M Johnson; Valentine J Klimkowski; Todd J Kohn; Ho-Shen Lin; JR McCowan; Michael E Richett; Daniel J Sall; A J Smith; Gerald F Smith; David W Snyder; Kumiko Takeuchi; Barbara G Utterback; S C Yan
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.
Bioorganic & medicinal chemistry letters 1999;9(5):775-80.
1999: Kumiko Takeuchi; Todd J Kohn; Daniel J Sall; ML Denney; JR McCowan; Gerald F Smith; Donetta Gifford-Moore
Dibasic benzo[B]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 4. SAR studies on the conformationally restricted C3-side chain of hydroxybenzo[B]thiophenes.
Bioorganic & medicinal chemistry letters 1999;9(5):759-64.
1999: Jolie A Bastian; Nikolay Y Chirgadze; ML Denney; Donetta Gifford-Moore; Daniel J Sall; Gerald F Smith; James H Wikel
Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 3. Enhancing activity by imposing conformational restriction in the C-4" side chain.
Bioorganic & medicinal chemistry letters 1999;9(3):363-8.
1998: Daniel J Sall; Stephen L Briggs; Nikolay Y Chirgadze; David Clawson; Donetta Gifford-Moore; Valentine J Klimkowski; JR McCowan; Gerald F Smith; James H Wikel
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 2. Exploring interactions at the proximal (S2) binding site.
Bioorganic & medicinal chemistry letters 1998;8(18):2527-32.
1997: Daniel J Sall; Jolie A Bastian; Stephen L Briggs; John Buben; Nikolay Y Chirgadze; David Clawson; ML Denney; Deborah D Giera; Donetta Gifford-Moore; RW Harper; KL Hauser; Valentine J Klimkowski; Todd J Kohn; Ho-Shen Lin; JR McCowan; Alan D Palkowitz; Gerald F Smith; Kumiko Takeuchi; Kenneth J Thrasher; Jennifer M Tinsley; Barbara G Utterback; S C Yan; M Zhang
Dibasic benzo[b]thiophene derivatives as a novel class of active site-directed thrombin inhibitors. 1. Determination of the serine protease selectivity, structure-activity relationships, and binding orientation.
Journal of medicinal chemistry 1997;40(22):3489-93.
1997: Nikolay Y Chirgadze; Daniel J Sall; Valentine J Klimkowski; David Clawson; Stephen L Briggs; R Hermann; Gerald F Smith; Donetta Gifford-Moore; JP Wery
The crystal structure of human alpha-thrombin complexed with LY178550, a nonpeptidyl, active site-directed inhibitor.
Protein science : a publication of the Protein Society 1997;6(7):1412-7.
1995: R T Shuman; R B Rothenberger; C S Campbell; Gerald F Smith; Donetta Gifford-Moore; Jonathan Paschal; P D Gesellchen
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.
Journal of medicinal chemistry 1995;38(22):4446-53.
1993: R T Shuman; R B Rothenberger; C S Campbell; Gerald F Smith; Donetta Gifford-Moore; P D Gesellchen
Highly selective tripeptide thrombin inhibitors.
Journal of medicinal chemistry 1993;36(3):314-9.