Search results for: Shankar Venkatraman

Items from 1 to 17 out of 17 results

article

Pharmacological characterization of the new bace1 inhibitor bi 1181181

Cornelia Dorner-Ciossek, Scott Hobson, Klaus Fuchs, Achim Sauer, more

Alzheimer's & Dementia: The Journal of the Alzheimer's Association > 2015 > 11 > 7 Supplement > P477

chapter

Uplink power control in LTE heterogeneous networks

Yuanye Wang, Shankar Venkatraman

2012 IEEE Globecom Workshops > 592 - 597

2012 IEEE Globecom Workshops (GC Wkshps)

Fractional path loss compensated power control (FPC) is adopted in LTE systems for the proper setting of User Equipment (UE) transmit power. The benefit of FPC has been extensively studied in homogeneous networks with only macro-cells. When additional small cells are co-channel deployed to form a heterogeneous networks (HetNet), new challenges are imposed to uplink power control. In this paper, we...

article

Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold

Peter D. Williams, Donnette D. Staas, Shankar Venkatraman, H. Marie Loughran, more

Bioorganic & Medicinal Chemistry Letters > 2010 > 20 > 22 > 6754-6757

Optimization studies using an HIV RNase H active site inhibitor containing a 1-hydroxy-1,8-naphthyridin-2(1H)-one core identified 4-position substituents that provided several potent and selective inhibitors. The best compound was potent and selective in biochemical assays (IC ₅₀ =0.045μM, HIV RT RNase H; 13μM, HIV RT-polymerase; 24μM, HIV integrase) and showed antiviral efficacy in a single-cycle...

article

Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3′,5′-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist

Shankar Venkatraman, Alec D. Lebsack, Kenneth Alves, Michael F. Gardner, more

Bioorganic & Medicinal Chemistry Letters > 2009 > 19 > 19 > 5803-5806

A series of prolyl-N-isonicotinoyl-(L)-4-aminophenylalanine derivatives substituted at the proline 4-position with cyclic amines was evaluated as VLA-4 antagonists. The ring size and presence or absence of fluorine affected potency and receptor occupancy. The analog with 3,3-difluoropiperidine at the proline 4-position (13) was the most potent compound and had very good duration of receptor occupancy...

article

The discovery of fused pyrrole carboxylic acids as novel, potent d-amino acid oxidase (DAO) inhibitors

Tim Sparey, Pravien Abeywickrema, Sarah Almond, Nick Brandon, more

Bioorganic & Medicinal Chemistry Letters > 2008 > 18 > 11 > 3386-3391

The ‘NMDA hypofunction hypothesis of schizophrenia’ can be tested in a number of ways. DAO is the enzyme primarily responsible for the metabolism of d-serine, a co-agonist for the NMDA receptor. We identified novel DAO inhibitors, in particular, acid 1, which demonstrated moderate potency for DAO in vitro and ex vivo, and raised plasma d-serine levels after dosing ip to rats. In parallel, analogues...

article

Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K

Eduardo L. Setti, Shankar Venkatraman, James T. Palmer, Xiaoming Xie, more

Bioorganic & Medicinal Chemistry Letters > 2006 > 16 > 16 > 4296-4299

The synthesis and biological profile of a novel series of potent and selective inhibitors of cysteine protease cathepsin K (Cat K) are described. Pharmacokinetic evaluation of 12 indicated that some members of this series could be suitable candidates to develop new orally active therapeutic agents for the treatment of osteoporosis.

article

Design and Synthesis of Tri-Ring P ₃ Benzamide-Containing Aminonitriles as Potent, Selective, Orally Effective Inhibitors of Cathepsin K

James T. Palmer, Clifford Bryant, Dan-Xiong Wang, Dana E. Davis, more

Journal of Medicinal Chemistry > 2005 > 48 > 24 > 7520 - 7534

article

Influence of acid surrogates toward potency of VLA-4 antagonist

Shankar Venkatraman, Jongwon Lim, Merryl Cramer, Michael F. Gardner, more

Bioorganic & Medicinal Chemistry Letters > 2005 > 15 > 18 > 4053-4056

A series of VLA-4 antagonist were synthesized wherein carboxylic acid was replaced by various acid surrogates. The effect of these acid surrogates toward potency was evaluated in a binding assay. A number of acid surrogates were potent antagonist of VLA-4, albeit significantly less potent than the corresponding carboxylic acid. Heterocyclic acid surrogate, oxadiazolidinone 3, demonstrated an improved...

article

Erratum to “An activity-based probe for the determination of cysteine cathepsin protease activities in whole cells” [Anal. Biochem. 335 (2004) 218–227]

Jean-Pierre Falgueyret, W. Cameron Black, Wanda Cromlish, Sylvie Desmarais, more

Analytical Biochemistry > 2005 > 340 > 2 > 380

article

An activity-based probe for the determination of cysteine cathepsin protease activities in whole cells

Jean-Pierre Falgueyret, W. Cameron Black, Wanda Cromlish, Sylvie Desmarais, more

Analytical Biochemistry > 2004 > 335 > 2 > 218-227

We describe a novel diazomethylketone-containing irreversible inhibitor (BIL-DMK) which is specific for a subset of pharmaceutically important cysteine cathepsin proteases. BIL-DMK rapidly inactivates cathepsins B, F, K, L, S, and V in isolated enzyme assays and labels cathepsins in whole cells. The presence of catalytically active cathepsins B, L, and K or S was demonstrated using radioiodinated...

article

Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the α ₂ δ-1 subunit of voltage gated calcium channel

Alec D. Lebsack, Janet Gunzner, Bowei Wang, Richard Pracitto, more

Bioorganic & Medicinal Chemistry Letters > 2004 > 14 > 10 > 2463-2467

We have identified and synthesized a series of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to α ₂ δ-1 subunit of voltage gated calcium channels. Structure-activity relationship studies directed toward improving the potency and physical properties of 2 lead to the discovery of 20 (IC ₅ ₀ =15nM) and (S)-22 (IC ₅ ₀ =30nM). A potent and selective...

article

Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives as high-affinity ligands of the α2δ subunit of voltage-gated calcium channels

Tao Hu, Brian A Stearns, Brian T Campbell, Jeannie M Arruda, more

Bioorganic & Medicinal Chemistry Letters > 2004 > 14 > 9 > 2031-2034

A novel class of 2H-pyrrolo[3,4-c]pyridazine ligands of the α₂δ subunit of voltage-gated calcium channels is described. Compound 4a with high affinity toward α₂δ was identified through structure–activity relationship studies of the lead compound. Tritiated ligand [³H]-4b was synthesized to demonstrate that this ligand binds to the same site as Gabapentin toward α₂δ subunit of voltage-gated calcium...

article

N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the α ₂ δ subunit of voltage gated calcium channels

Jongwon Lim, Nicholas Stock, Richard Pracitto, Julia K. Boueres, more

Bioorganic & Medicinal Chemistry Letters > 2004 > 14 > 8 > 1913-1916

A series of N-acridin-9-yl-butane-1,4-diamines were found to be high-affinity ligands of the α ₂ δ subunit of voltage gated calcium channels. The SAR studies of butane-1,4-diamine side chain resulted in the identification of compound 10 (IC ₅ ₀ =9 nM), which is more potent than gabapentin (IC ₅ ₀ =27 nM). Partial saturation of the acridine ring was also pursued and...

article

A Novel Class of Nonpeptidic Biaryl Inhibitors of Human Cathepsin K

Joël Robichaud, Renata Oballa, Peppi Prasit, Jean-Pierre Falgueyret, more

Journal of Medicinal Chemistry > 2003 > 46 > 17 > 3709 - 3727

article

Novel route to the synthesis of peptides containing 2-amino-1′-hydroxymethyl ketones and their application as cathepsin K inhibitors

Rohan V Mendonca, Shankar Venkatraman, James T Palmer

Bioorganic & Medicinal Chemistry Letters > 2002 > 12 > 20 > 2887-2891

Cathepsin K is highly expressed in human osteoclasts, and is implicated in bone resorption. This makes it an attractive target for the treatment of osteoporosis. Peptides containing 2-amino-1′-hydroxymethyl ketones and 2-amino-1′-alkoxymethyl ketones were discovered as potent inhibitors of cathepsin K. A novel synthetic route was devised to facilitate rapid elucidation of the SAR of these inhibitors...

article

Design, synthesis, and evaluation of azapeptides as substrates and inhibitors for human rhinovirus 3C protease

Shankar Venkatraman, Jian-she Kong, Sanjay Nimkar, Q. May Wang, more

Bioorganic & Medicinal Chemistry Letters > 1999 > 9 > 4 > 577-580

A series of azapeptides was prepared and assessed as inhibitors of the human rhinovirus 3C protease. Boc-VLFaQ-OPh was a slow-turnover substrate that gave transient (ca. 1-2 h) inhibition as it underwent hydrolysis. Boc-VLFaG-OPh gave very slow but essentially irreversible inhibition.

article

The crystal structure of a novel product from the acid-catalyzed condensation of 1-benzylindole with acetone

Wayland E. Noland, Michael J. Konkel, Susan J. Fanburg, Shankar Venkatraman, more

Journal of Chemical Crystallography > 1999 > 29 > 1 > 9-14

The acid-catalyzed condensation of 1-benzylindole with acetone in the presence of N-phenylmaleimide gave a tetrahydrocarbazole, (4,5,10,10b-tetrahydro-5-methyl-2-phenyl-10-(phenylmethyl)pyrrolo[3,4-a]carbazole-1,3[2H, 3aH]-dione (1), as the major product and a novel spiro compound, 1′,3,4,4′-tetrahydro-1′,1′,3,3-tetramethyl-4,4′-bis(phenylmethyl)-1,3′(2H, 2′H)-spiro[cyclopent[b]indole] (2), as the...

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