Zobrazeno 1 - 10
of 52
pro vyhledávání: '"RONALD RUBIN"'
Autor:
Christie G. Brouillette, Steve Dunham, Karen Siegel, Mark E. Snow, Irina I. Protasevich, J. Ronald Rubin, Rocco Gogliotti
Publikováno v:
Biochemistry. 43:13380-13389
The antibacterial target enoyl-acyl carrier protein (ACP) reductase is a homotetrameric enzyme that catalyzes the last reductive step of fatty acid biosynthesis. In the present paper, four 2-(2-hydroxyphenoxy)phenol inhibitors, wherein the 4-position
Autor:
Ronald Rubin
An enormous amount of research effort has been directed toward elucidating the mechanism by which substances are extruded from cells; and reviews have been written and symposia held in order to systematize the plethora of evidence made available. How
Publikováno v:
Tetrahedron. 57:6579-6588
All four possible stereoisomers of the 3-carboxyl-4-isopropyl-pyrrolidine (4) were prepared and their stereochemistry was assigned unambiguously.
Addition reactions of allyl stannanes to an indolo[2′,3′:3,4]pyrido[1,2-b]isoquinoline imminium salt
Autor:
David T. Connor, Bruce D. Roth, Paul C. Unangst, Larry D. Bratton, Bharat K. Trivedi, J. Ronald Rubin
Publikováno v:
Journal of Heterocyclic Chemistry. 37:1081-1087
The addition of organometallic reagents to the 13b-position of the indolo[2′,3′:3,4]pyrido[1,2-b]isoquinoline imminium salt 4 is described. Reaction of 4 with tetraallyl tin in 2-methoxyethanol gave the allyl adduct 7 in moderate yield. Further e
Autor:
Christine Humblet, Jeremy E. Edmunds, and M. Arshad Siddiqui, ‡ Yves St-Denis, Debra R. Holland, Janet S. Plummer, Lakshmi S. Narasimhan, Stephen T. Rapundalo, J. Ronald Rubin
Publikováno v:
Journal of Medicinal Chemistry. 43:361-368
We have studied the thrombin and trypsin complexed structures of a pair of peptidomimetic thrombin inhibitors, containing different P1 fragments. The first has arginine as its P1 fragment, and the second contains the constrained arginine mimic (2S)-2
Autor:
A. Susser, Peter D. Winocour, John DiMaio, Debra R. Holland, M. Arshad Siddiqui, Kent A. Berryman, Sophie Levesque, Janet S. Plummer, D. Lafleur, Jeremy J. Edmunds, Scott R. Eaton, J. Ronald Rubin, Annette Marian Doherty, Cuiman Cai, Wayne L. Cody, Stephen T. Rapundalo, Lakshmi S. Narasimhan, Yves St-Denis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:835-840
The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors are described. We have explored the SAR around the P1' site. Modification of the P1' site has been found to affect potency and selectivity.
Publikováno v:
Tetrahedron. 55:1647-1656
The N-alkylation of primary nitrophenylsulfonamides followed by removal of the nitrophenylsulfonamide moiety under nucleophilic conditions to provide secondary amines has become an established literature procedure. Application of this methodology wit
Autor:
J. Ronald Rubin, Darin R. Kent, Debra R. Holland, John DiMaio, Yves St-Denis, Annette Marian Doherty, Sophie Levesque, Cuiman Cai, Peter D. Winocour, Jeremy J. Edmunds, M. Arshad Siddiqui, Lakshmi S. Narasimhan, Stephen T. Rapundalo, Janet S. Plummer, John X. He, Alan J. Susser, Kent A. Berryman, Wayne L. Cody
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3409-3414
The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors is described. We have explored the SAR with modifications to the P1 site. The introduction of arginine mimetics at the P1 site led to potent and selectiv
Autor:
Sophie Levesque, Kent A. Berryman, M. Arshad Siddiqui, Jeremy J. Edmunds, Peter D. Winocour, John DiMaio, Annette Marian Doherty, Yves St-Denis, C.E. Augelli-Szafran, Benoit Bachand, Lorraine Leblond, Lakshmi S. Narasimhan, J. Ronald Rubin, Micheline Tarazi, J.R. Penvose-Yi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3193-3198
Peptidomimetic inhibitors of general structure 1 have been prepared. Optimization of the binding affinities of these compounds through variation of the P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting ph
Publikováno v:
Tetrahedron Letters. 39:6111-6114
12b-Substituted indolo[2,3-a]quinolizidin-2-ones 5 are synthesized by treatment of Grignard reagents with O-acetyl iminium salt 4 generated by treating cyclic enaminoketone 3 with acetyl chloride. Subsequent Robinson annulation employing the Stork en