Search Results - "HEWAWASAM, Piyasena"

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 by Hewawasam, Piyasena, Fan, Wenhong, Knipe, Jay, Moon, Sandra L, Boissard, Christopher G, Gribkoff, Valentin K, Starrett, John E

“…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…”
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The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels by HEWAWASAM, Piyasena, GRIBKOFF, Valentin K, PAJOR, Lorraine M, KNIPE, Jay, QI GAO, PERRONE, Robert, STARRETT, John E, PENDRI, Yadagiri, DWORETZKY, Steven I, MEANWELL, Nicholas A, MARTINEZ, Eduardo, BOISSARD, Christopher G, POST-MUNSON, Debra J, TROJNACKI, Joanne T, YELESWARAM, Krishnaswamy

“…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…”
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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 by Sivarao, Digavalli V, Newberry, Kimberly, Langdon, Shaun, Lee, Alicia V, Hewawasam, Piyasena, Plym, Mary Jane, Signor, Laura, Myers, Robert, Lodge, Nicholas J

“…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…”
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Synthesis of water-Soluble prodrugs of BMS-191011: A maxi-K channel opener targeted for post-stroke neuroprotection by Hewawasam, Piyasena, Ding, Min, Chen, Nathan, King, Dalton, Knipe, Jay, Pajor, Lorraine, Ortiz, Astrid, Gribkoff, Valentin K., Starrett, John

“…A variety of water-soluble prodrugs of BMS-191011 was synthesized and evaluated for solution state stability and rate of conversion to BMS-191011 in rat and…”
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Discovery and Early Clinical Evaluation of BMS-605339, a Potent and Orally Efficacious Tripeptidic Acylsulfonamide NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection by Scola, Paul M., Wang, Alan Xiangdong, Good, Andrew C., Sun, Li-Qiang, Combrink, Keith D., Campbell, Jeffrey A., Chen, Jie, Tu, Yong, Sin, Ny, Venables, Brian L., Sit, Sing-Yuen, Chen, Yan, Cocuzza, Anthony, Bilder, Donna M., D’Andrea, Stanley, Zheng, Barbara, Hewawasam, Piyasena, Ding, Min, Thuring, Jan, Li, Jianqing, Hernandez, Dennis, Yu, Fei, Falk, Paul, Zhai, Guangzhi, Sheaffer, Amy K., Chen, Chaoqun, Lee, Min S., Barry, Diana, Knipe, Jay O., Li, Wenying, Han, Yong-Hae, Jenkins, Susan, Gesenberg, Christoph, Gao, Qi, Sinz, Michael W., Santone, Kenneth S., Zvyaga, Tatyana, Rajamani, Ramkumar, Klei, Herbert E., Colonno, Richard J., Grasela, Dennis M., Hughes, Eric, Chien, Caly, Adams, Stephen, Levesque, Paul C., Li, Danshi, Zhu, Jialong, Meanwell, Nicholas A., McPhee, Fiona

“…The discovery of BMS-605339 (35), a tripeptidic inhibitor of the NS3/4A enzyme, is described. This compound incorporates a cyclopropyl­acylsulfonamide moiety…”
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The Discovery of Asunaprevir (BMS-650032), An Orally Efficacious NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection by Scola, Paul M., Sun, Li-Qiang, Wang, Alan Xiangdong, Chen, Jie, Sin, Ny, Venables, Brian L., Sit, Sing-Yuen, Chen, Yan, Cocuzza, Anthony, Bilder, Donna M., D’Andrea, Stanley V., Zheng, Barbara, Hewawasam, Piyasena, Tu, Yong, Friborg, Jacques, Falk, Paul, Hernandez, Dennis, Levine, Steven, Chen, Chaoqun, Yu, Fei, Sheaffer, Amy K., Zhai, Guangzhi, Barry, Diana, Knipe, Jay O., Han, Yong-Hae, Schartman, Richard, Donoso, Maria, Mosure, Kathy, Sinz, Michael W., Zvyaga, Tatyana, Good, Andrew C., Rajamani, Ramkumar, Kish, Kevin, Tredup, Jeffrey, Klei, Herbert E., Gao, Qi, Mueller, Luciano, Colonno, Richard J., Grasela, Dennis M., Adams, Stephen P., Loy, James, Levesque, Paul C., Sun, Huabin, Shi, Hong, Sun, Lucy, Warner, William, Li, Danshi, Zhu, Jialong, Meanwell, Nicholas A., McPhee, Fiona

“…The discovery of asunaprevir (BMS-650032, 24) is described. This tripeptidic acylsulfonamide inhibitor of the NS3/4A enzyme is currently in phase III clinical…”
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Creation of a new class of radiosensitizers for glioblastoma based on the mibefradil pharmacophore by Paradkar, Sateja, Herrington, James, Hendricson, Adam, Hewawasam, Piyasena, Plummer, Mark, Hoyer, Denton, Sundaram, Ranjini K, Surovtseva, Yulia V, Bindra, Ranjit S

“…Glioblastoma (GBM) is the most common primary malignant tumor of the central nervous system with a dismal prognosis. Locoregional failure is common despite…”
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Resensitizing daclatasvir-resistant hepatitis C variants by allosteric modulation of NS5A by Sun, Jin-Hua, O’Boyle II, Donald R., Fridell, Robert A., Langley, David R., Wang, Chunfu, Roberts, Susan B., Nower, Peter, Johnson, Benjamin M., Moulin, Frederic, Nophsker, Michelle J., Wang, Ying-Kai, Liu, Mengping, Rigat, Karen, Tu, Yong, Hewawasam, Piyasena, Kadow, John, Meanwell, Nicholas A., Cockett, Mark, Lemm, Julie A., Kramer, Melissa, Belema, Makonen, Gao, Min

“…The drug daclatasvir (DCV), which inhibits the hepatitis C virus (HCV) non-structural protein 5A (NS5A), can successfully reduce viral load in patients; here,…”
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Discovery and Preclinical Characterization of the Cyclopropylindolobenzazepine BMS-791325, A Potent Allosteric Inhibitor of the Hepatitis C Virus NS5B Polymerase by Gentles, Robert G., Ding, Min, Bender, John A., Bergstrom, Carl P., Grant-Young, Katharine, Hewawasam, Piyasena, Hudyma, Thomas, Martin, Scott, Nickel, Andrew, Regueiro-Ren, Alicia, Tu, Yong, Yang, Zhong, Yeung, Kap-Sun, Zheng, Xiaofan, Chao, Sam, Sun, Jung-Hui, Beno, Brett R., Camac, Daniel M., Chang, Chong-Hwan, Gao, Mian, Morin, Paul E., Sheriff, Steven, Tredup, Jeff, Wan, John, Witmer, Mark R., Xie, Dianlin, Hanumegowda, Umesh, Knipe, Jay, Mosure, Kathy, Santone, Kenneth S., Parker, Dawn D., Zhuo, Xiaoliang, Lemm, Julie, Liu, Mengping, Pelosi, Lenore, Rigat, Karen, Voss, Stacey, Wang, Yi, Wang, Ying-Kai, Colonno, Richard J., Gao, Min, Roberts, Susan B., Gao, Qi, Ng, Alicia, Meanwell, Nicholas A, Kadow, John F.

“…Described herein are structure–activity relationship studies that resulted in the optimization of the activity of members of a class of cyclopropyl-fused…”
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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 by Hewawasam, Piyasena, Tu, Yong, Hudyma, Thomas W., Zhang, Xiaofan, Gentles, Robert G., Kadow, John F., Meanwell, Nicholas A.

“…[Display omitted] A convenient and practical synthesis of 6-carboalkoxy-13-cycloalkyl-5H-indolo[2,1-a][2]benzazepine-10-carboxylic acid derivatives (6) has…”
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A practical and efficient synthesis of 6-carboalkoxy-13-cycloalkyl-5H-indolo[2,1-a][2]benzazepine-10-carb o xylic acid derivatives by Hewawasam, Piyasena, Tu, Yong, Hudyma, Thomas, Zhang, Xiaofan, Gentles, Robert, Kadow, John, Meanwell, Nicholas

“…A convenient and practical synthesis of 6-carboalkoxy-13-cycloalkyl-5H-indolo[2,1-a][2]benzazepine-10-carb o xylic acid derivatives (6) has been developed. The…”
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Synergistic Activity of Combined NS5A Inhibitors by O'Boyle, 2nd, Donald R, Nower, Peter T, Gao, Min, Fridell, Robert, Wang, Chunfu, Hewawasam, Piyasena, Lopez, Omar, Tu, Yong, Meanwell, Nicholas A, Belema, Makonen, Roberts, Susan B, Cockett, Mark, Sun, Jin-Hua

“…Daclatasvir (DCV) is a first-in-class hepatitis C virus (HCV) nonstructural 5A replication complex inhibitor (NS5A RCI) that is clinically effective in…”
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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 by Hewawasam, Piyasena, Tu, Yong, Gao, Min, Hanumegowda, Umesh, Knipe, Jay, Lemm, Julie A., Parker, Dawn D., Rigat, Karen L., Roberts, Susan B., Meanwell, Nicholas A., Kadow, John F.

“…[Display omitted] Herein, we describe the synthesis, antiviral structure–activity relationships (SAR), metabolic stability, and pharmacokinetic (PK) properties…”
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Synthesis and Structure−Activity Relationships of 3-Aryloxindoles:  A New Class of Calcium-Dependent, Large Conductance Potassium (Maxi-K) Channel Openers with Neuroprotective Properties by Hewawasam, Piyasena, Erway, Matthew, Moon, Sandra L, Knipe, Jay, Weiner, Harvey, Boissard, Christopher G, Post-Munson, Debra J, Gao, Qi, Huang, Stella, Gribkoff, Valentin K, Meanwell, Nicholas A

“…A series of 3-aryloxindole derivatives were synthesized and evaluated as activators of the cloned maxi-K channel mSlo expressed in Xenopus laevis oocytes using…”
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Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels by Gribkoff, Valentin K, Starrett, John E, Dworetzky, Steven I, Hewawasam, Piyasena, Boissard, Christopher G, Cook, Deborah A, Frantz, Stephen W, Heman, Karen, Hibbard, Jeffrey R, Huston, Kevin, Johnson, Graham, Krishnan, Bala S, Kinney, Gene G, Lombardo, Lynn A, Meanwell, Nicholas A, Molinoff, Perry B, Myers, Robert A, Moon, Sandra L, Ortiz, Astrid, Pajor, Lorraine, Pieschl, Rick L, Post-Munson, Debra J, Signor, Laura J, Srinivas, Nugehally, Taber, Matthew T, Thalody, George, Trojnacki, Joanne T, Wiener, Harvey, Yeleswaram, Krishnaswamy, Yeola, Sarita W

“…During ischemic stroke, neurons at risk are exposed to pathologically high levels of intracellular calcium (Ca++), initiating a fatal biochemical cascade. To…”
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Inhibitors of blood platelet cAMP phosphodiesterase. 4. Structural variation of the side-chain terminus of water-soluble 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives by Meanwell, Nicholas A, Hewawasam, Piyasena, Thomas, Jeanine A, Wright, J. J. Kim, Russell, John W, Gamberdella, Marianne, Goldenberg, Harold J, Seiler, Steven M, Zavoico, George B

“…1-(Cyclohexylmethyl)-4-[4-[(2,3-dihydro-2-oxo-1H-imidazo[4,5-b] quinolin-7-yl)oxy]-1-oxobutyl]piperazine (2) was previously identified as a potent,…”
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Regiospecific preparation of the benz[b]xanthen-12-one ring system. Total synthesis of bikaverin by Hauser, Frank M, Hewawasam, Piyasena, Baghdanov, Vaceli M

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Stereospecific syntheses of (E)-1,3-disubstituted dienes by Hauser, Frank M, Tommasi, Ruben, Hewawasam, Piyasena, Rho, Young S

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4-Aryl-3-(hydroxyalkyl)quinolin-2-ones:  Novel Maxi-K Channel Opening Relaxants of Corporal Smooth Muscle Targeted for Erectile Dysfunction by Hewawasam, Piyasena, Fan, Wenhong, Ding, Min, Flint, Kim, Cook, Deborah, Goggins, Gregory D, Myers, Robert A, Gribkoff, Valentin K, Boissard, Christopher G, Dworetzky, Steven I, Starrett, John E, Lodge, Nicholas J

“…Novel 4-aryl-3-(hydroxyalkyl)quinoline-2-one derivatives were prepared and evaluated as openers of the cloned maxi-K channel hSlo expressed in Xenopus laevis…”
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3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction by BOY, Kenneth M, GUERNON, Jason M, STARRETT, John E, SIT, Sing-Yuen, XIE, Kai, HEWAWASAM, Piyasena, BOISSARD, Christopher G, DWORETZKY, Steven I, NATALE, Joanne, GRIBKOFF, Valentin K, LODGE, Nicholas

“…A series of Maxi-K openers for the treatment of erectile dysfunction based on the 3-thio-quinolinone core is described. Significant levels of channel opening…”
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