Search Results - "SHENVI, Ashok"

Preclinical pharmacology and pharmacokinetics of AZD3783, a selective 5-hydroxytryptamine 1B receptor antagonist by Zhang, Minli, Zhou, Diansong, Wang, Yi, Maier, Donna L, Widzowski, Daniel V, Sobotka-Briner, Cynthia D, Brockel, Becky J, Potts, William M, Shenvi, Ashok B, Bernstein, Peter R, Pierson, M Edward

“…The preclinical pharmacology and pharmacokinetic properties of (2R)-6-methoxy-8-(4-methylpiperazin-1-yl)-N-(4-morpholin-4-ylphenyl)chromane-2-carboxamide…”
Get more information

The mechanism of gamma-secretase: multiple inhibitor binding sites for transition state analogs and small molecule inhibitors by Tian, Gaochao, Ghanekar, Smita V, Aharony, David, Shenvi, Ashok B, Jacobs, Robert T, Liu, Xiaodong, Greenberg, Barry D

“…Transition state analogs pepstatin methylester (PME) and L685458 have been shown to inhibit gamma-secretase non-competitively (Tian, G., Sobotka-Briner, C.,…”
Get full text

Calculation and application of activity discriminants in lead optimization by Luo, Xincai, Krumrine, Jennifer R., Shenvi, Ashok B., Pierson, M. Edward, Bernstein, Peter R.

“…[Display omitted] ▶ Predict activities of in vitro (pharmacological, DMPK, and safety) assays. ▶ Emulate how medicinal chemists perform SAR analysis and…”
Get full text

Design, Synthesis, and SAR of Tachykinin Antagonists:  Modulation of Balance in NK1/NK2 Receptor Antagonist Activity by Albert, Jeffrey S, Aharony, David, Andisik, Donald, Barthlow, Herbert, Bernstein, Peter R, Bialecki, Russell A, Dedinas, Robert, Dembofsky, Bruce T, Hill, Daniel, Kirkland, Karin, Koether, Gerard M, Kosmider, Benedict J, Ohnmacht, Cyrus, Palmer, William, Potts, William, Rumsey, William, Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Warwick, Paul J, Russell, Keith

“…Through optimization of compounds based on the dual NK1/NK2 antagonist ZD6021, it was found that alteration of two key regions could modulate the balance of…”
Get full text

Recent advances in neurokinin receptor antagonists by Shenvi, Ashok B

Get more information

Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors by Rumsey, W L, Aharony, D, Bialecki, R A, Abbott, B M, Barthlow, H G, Caccese, R, Ghanekar, S, Lengel, D, McCarthy, M, Wenrich, B, Undem, B, Ohnmacht, C, Shenvi, A, Albert, J S, Brown, F, Bernstein, P R, Russell, K

“…The tachykinins, substance P, neurokinin A, and neurokinin B, have been implicated in many diseases. The present study evaluated the pharmacological properties…”
Get more information

Nitrogen-15 NMR spectroscopy of the catalytic-triad histidine of a serine protease in peptide boronic acid inhibitor complexes by Bachovchin, William W, Wong, Winona Y. L, Farr-Jones, Shauna, Shenvi, Ashok B, Kettner, Charles A

“…15N NMR spectroscopy was used to examine the active-site histidyl residue of alpha-lytic protease in peptide boronic acid inhibitor complexes. Two distinct…”
Get full text

Serine protease mechanism: structure of an inhibitory complex of .alpha.-lytic protease and a tightly bound peptide boronic acid by Bone, Roger, Shenvi, Ashok B, Kettner, Charles A, Agard, David A

“…The structure of the complex formed between alpha-lytic protease, a serine protease secreted by Lysobacter enzymogenes, and…”
Get full text

alpha.-Aminoboronic acid derivatives: effective inhibitors of aminopeptidases by Shenvi, Ashok B

“…alpha-Aminoboronic acids and their derivatives have been synthesized as stable white solids. These compounds are effective inhibitors of human enkephalin…”
Get full text

Convenient synthesis of 3-methyl-2,3,4,4a.alpha.,5,6,7,7a.alpha.-octahydro-1H-benzofuro[3,2-e]isoquinoline by Shenvi, Ashok B, Ciganek, Engelbert

Get full text

The Mechanism of γ-Secretase by Tian, Gaochao, Ghanekar, Smita V., Aharony, David, Shenvi, Ashok B., Jacobs, Robert T., Liu, Xiaodong, Greenberg, Barry D.

“…Transition state analogs pepstatin methylester (PME) and L685458 have been shown to inhibit γ-secretase non-competitively (Tian, G., Sobotka-Briner, C., Zysk,…”
Get full text

Discovery of novel, orally active dual NK1/NK2 antagonists by BERNSTEIN, Peter R, AHARONY, David, KOSMIDER, Benedict J, KIRKLAND, Karin, OHNMACHT, Cyrus J, POTTS, William, RUMSEY, William L, LIHONG SHEN, SHENVI, Ashok, SHERWOOD, Scott, STOLLMAN, David, RUSSELL, Keith, ALBERT, Jeffrey S, ANDISIK, Donald, BARTHLOW, Herbert G, BIALECKI, Russell, DAVENPORT, Timothy, DEDINAS, Robert F, DEMBOFSKY, Bruce T, KOETHER, Gerard

“…Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK1 and NK2…”
Get full text

Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity by Albert, Jeffrey S, Aharony, David, Andisik, Donald, Barthlow, Herbert, Bernstein, Peter R, Bialecki, Russell A, Dedinas, Robert, Dembofsky, Bruce T, Hill, Daniel, Kirkland, Karin, Koether, Gerard M, Kosmider, Benedict J, Ohnmacht, Cyrus, Palmer, William, Potts, William, Rumsey, William, Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Warwick, Paul J, Russell, Keith

“…Through optimization of compounds based on the dual NK(1)/NK(2) antagonist ZD6021, it was found that alteration of two key regions could modulate the balance…”
Get full text

Design, Synthesis, and SAR of Tachykinin Antagonists:  Modulation of Balance in NK 1 /NK 2 Receptor Antagonist Activity by Albert, Jeffrey S., Aharony, David, Andisik, Donald, Barthlow, Herbert, Bernstein, Peter R., Bialecki, Russell A., Dedinas, Robert, Dembofsky, Bruce T., Hill, Daniel, Kirkland, Karin, Koether, Gerard M., Kosmider, Benedict J., Ohnmacht, Cyrus, Palmer, William, Potts, William, Rumsey, William, Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Warwick, Paul J., Russell, Keith

Get full text

Discovery of novel, orally active dual NK 1/NK 2 antagonists by Bernstein, Peter R., Aharony, David, Albert, Jeffrey S., Andisik, Donald, Barthlow, Herbert G., Bialecki, Russell, Davenport, Timothy, Dedinas, Robert F., Dembofsky, Bruce T., Koether, Gerard, Kosmider, Benedict J., Kirkland, Karin, Ohnmacht, Cyrus J., Potts, William, Rumsey, William L., Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Stollman, David, Russell, Keith

“…Exploration of the SAR around selective NK 2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK 1 and…”
Get full text

4-Alkylpiperidines related to SR-48968: Potent antagonists of the neurokinin-2 (NK 2) receptor by Jacobs, Robert T., Shenvi, Ashok B., Mauger, Russell C., Ulatowski, Terrance G., Aharony, David, Buckner, Carl K.

“…A series of 4-alkylpiperidine derivatives related to the potent neurokinin-2 (NK 2) receptor antagonist SR-48968 ( 1) is described. Simple aliphatic…”
Get full text

The use of α-aminoboronic acid derivatives to stabilize peptide drugs during their intranasal absorption by HUSSAIN, M. A, SHENVI, A. B, ROWE, S. M, SHEFTER, E

“…alpha-Aminoboronic acid derivatives, potent and reversible inhibitors of aminopeptidases, were tested nasally in situ in rats for stabilizing externally…”
Get full text

Convenient synthesis of 3-methyl-2,3,4,4aα,5,6,7,7aα-octahydro-1H-benzofuro[3,2-e]isoquinoline by SHENVI, A. B, CIGANEK, E

Get full text

The Mechanism of γ-Secretase by Gaochao Tian, Smita V. Ghanekar, David Aharony, Ashok B. Shenvi, Robert T. Jacobs, Xiaodong Liu, Barry D. Greenberg

“…Transition state analogs pepstatin methylester (PME) and L685458 have been shown to inhibit γ-secretase non-competitively (Tian, G., Sobotka-Briner, C., Zysk,…”
Get full text

Recovery of rat nasal mucosa from the effects of aminopeptidase inhibitors by Hussain, M A, Koval, C A, Shenvi, A B, Aungst, B J

“…Aminopeptidase inhibitors may be useful for improving the systemic bioavailability of peptide drugs administered nasally or by other routes. Preferably, their…”
Get more information