Výsledky vyhledávání - "Piyasena Hewawasam"

Creation of a new class of radiosensitizers for glioblastoma based on the mibefradil pharmacophore

Autor: Sateja Paradkar, Adam Hendricson, Mark Plummer, Ranjini K. Sundaram, James Herrington, Denton Hoyer, Ranjit S. Bindra, Yulia V. Surovtseva, Piyasena Hewawasam

Publikováno v: Oncotarget

Glioblastoma (GBM) is the most common primary malignant tumor of the central nervous system with a dismal prognosis. Locoregional failure is common despite high doses of radiation therapy, which has prompted great interest in developing novel strateg

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54b96f25b0746c867fcdee576b3c9434
https://doi.org/10.18632/oncotarget.27933

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Resensitizing daclatasvir-resistant hepatitis C variants by allosteric modulation of NS5A

Publikováno v: Nature. 527:245-248

The drug daclatasvir (DCV), which inhibits the hepatitis C virus (HCV) non-structural protein 5A (NS5A), can successfully reduce viral load in patients; here, a combination of DCV and an NS5A analogue is shown to enhance DCV potency on multiple genot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df8acddb1fd05737cb9a5be1809c6380
https://doi.org/10.1038/nature15711

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A practical and efficient synthesis of 6-carboalkoxy-13-cycloalkyl-5H-indolo[2,1-a][2]benzazepine-10-carboxylic acid derivatives

Autor: Robert G. Gentles, Piyasena Hewawasam, Yong Tu, Thomas W. Hudyma, Nicholas A. Meanwell, John F. Kadow, Xiaofan Zhang

Publikováno v: Tetrahedron Letters. 55:1148-1153

A convenient and practical synthesis of 6-carboalkoxy-13-cycloalkyl-5 H -indolo[2,1- a ][2]benzazepine-10-carboxylic acid derivatives ( 6 ) has been developed. The key step in the synthesis utilizes an intramolecular tandem reaction sequence of a Mic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4a1aa68f0423ecc0ed990dcc538fe1f3
https://doi.org/10.1016/j.tetlet.2013.12.085

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Discovery and preclinical evaluation of potent, orally bioavailable, metabolically stable cyclopropylindolobenzazepine acylsulfonamides as thumb site 1 inhibitors of the hepatitis c virus NS5B RNA-dependent, RNA polymerase

Autor: Nicholas A. Meanwell, John F. Kadow, Piyasena Hewawasam, Julie A. Lemm, Karen Rigat, Min Gao, Yong Tu, Dawn D. Parker, Jay O. Knipe, Susan B. Roberts, Umesh Hanumegowda

Publikováno v: Bioorganicmedicinal chemistry letters. 26(3)

Herein, we describe the synthesis, antiviral structure-activity relationships (SAR), metabolic stability, and pharmacokinetic (PK) properties for a series of cyclopropylindolobenzazepine acylsulfonamide HCV NS5B polymerase inhibitors. Optimization of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::feb3f65ec1b8c8b3bc263bc873273490
https://pubmed.ncbi.nlm.nih.gov/26747393

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Synergistic Activity of Combined NS5A Inhibitors

Autor: Peter T. Nower, Lopez Omar D, Susan B. Roberts, Min Gao, Chunfu Wang, Jin-Hua Sun, Makonen Belema, Yong Tu, Mark I. Cockett, Nicholas A. Meanwell, Robert A. Fridell, Piyasena Hewawasam, Donald R. O'Boyle

Publikováno v: Antimicrobial agents and chemotherapy. 60(3)

Daclatasvir (DCV) is a first-in-class hepatitis C virus (HCV) nonstructural 5A replication complex inhibitor (NS5A RCI) that is clinically effective in interferon-free combinations with direct-acting antivirals (DAAs) targeting alternate HCV proteins

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f406f4f547da355dc19343f87b558215
https://pubmed.ncbi.nlm.nih.gov/26711745

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Effect of 4-(5-Chloro-2-hydroxyphenyl)-3-(2-hydroxyethyl)-6-(trifluoromethyl)-quinolin-2(1H)-one (BMS-223131), a Novel Opener of Large Conductance Ca2+-Activated K+ (Maxi-K) Channels on Normal and Stress-Aggravated Colonic Motility and Visceral Nociception

Autor: Piyasena Hewawasam, Robert A. Myers, Nicholas J. Lodge, Kimberly Newberry, Shaun Langdon, Alicia V. Lee, Digavalli V. Sivarao, Laura J. Signor, Mary Jane Plym

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 313:840-847

We evaluated the effects of 4-(5-chloro-2-hydroxyphenyl)-3-(2-hydroxyethyl)-6-(trifluoromethyl)-quinolin-2(1H)-one (BMS-223131), an opener of large conductance Ca(2+)-activated potassium (maxi-K) channels, on normal and stress-exacerbated colonic mot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6b8a9a219eafe737e533d6c78c27fc68
https://doi.org/10.1124/jpet.104.079285

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The synthesis and structure–activity relationships of 3-amino-4-benzylquinolin-2-ones

Autor: Joanne T. Natale, John E. Starrett, Piyasena Hewawasam, Valentin K. Gribkoff, Min Ding, Christopher G. Boissard, Sarita W Yeola, Nathan Chen, Steven I. Dworetzky

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:1615-1618

3-Amino-4-benzylquinolin-2-ones have been identified as a novel class of KCNQ2 channel openers. Synthesis and SAR is described along with their electrophysiological evaluation as activators of the cloned m KCNQ2 channel expressed in Xenopus laevis oo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4947a4b4aad6acaab3b34b31f5971cf5
https://doi.org/10.1016/j.bmcl.2004.01.073

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The synthesis and structure–activity relationships of 4-aryl-3-aminoquinolin-2-ones: a new class of calcium-Dependent, large conductance, potassium (maxi-K) channel openers targeted for post-stroke neuroprotection

Autor: Piyasena Hewawasam, Wenhong Fan, Christopher G. Boissard, Jay O. Knipe, Valentin K. Gribkoff, Sandra L. Moon, John E. Starrett

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:1779-1783

A series of 4-aryl-3-aminoquinoline-2-one derivatives was synthesized and evaluated as activators of the cloned maxi-K channel mSlo (hSlo) expressed in Xenopus laevis oocytes using electrophysiological methods. A brain penetrable activator of maxi-K

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ba7532ff76b999d59c5cc8e5e4a214a
https://doi.org/10.1016/s0960-894x(02)00240-8

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The synthesis and characterization of BMS-204352 (MaxiPost™) and related 3-fluorooxindoles as openers of maxi-K potassium channels

Autor: Piyasena Hewawasam, Steven I. Dworetzky, Yadagiri Pendri, Lorraine Pajor, Qi Gao, Valentin K. Gribkoff, John E. Starrett, Martinez Eduardo J, Joanne T. Trojnacki, Debra J. Post-Munson, Christopher G. Boissard, Krishnaswamy Yeleswaram, Robert K. Perrone, Nicholas A. Meanwell, Jay O. Knipe

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:1023-1026

3-Aryl-3-fluorooxindoles can be efficiently synthesized in two steps by the addition of an aryl Grignard to an isatin, followed by treatment with DAST. Oxindole 1 (BMS-204352; MaxiPost) can be isolated using chiral HPLC or prepared by employing chira

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9a56228112f2fba1136e1270d9daa2a
https://doi.org/10.1016/s0960-894x(02)00101-4

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