Search Results - "Zadjura, Lisa"

Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 5. An Evolution from Indole to Azaindoles Leading to the Discovery of 1-(4-Benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a Drug Candidate That Demonstrates Antiviral Activity in HIV-1-Infected Subjects by Wang, Tao, Yin, Zhiwei, Zhang, Zhongxing, Bender, John A, Yang, Zhong, Johnson, Graham, Yang, Zheng, Zadjura, Lisa M, D’Arienzo, Celia J, DiGiugno Parker, Dawn, Gesenberg, Christophe, Yamanaka, Gregory A, Gong, Yi-Fei, Ho, Hsu-Tso, Fang, Hua, Zhou, Nannan, McAuliffe, Brian V, Eggers, Betsy J, Fan, Li, Nowicka-Sans, Beata, Dicker, Ira B, Gao, Qi, Colonno, Richard J, Lin, Pin-Fang, Meanwell, Nicholas A, Kadow, John F

“…Azaindole derivatives derived from the screening lead 1-(4-benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione (1) were prepared and characterized to…”
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A Small Molecule HIV-1 Inhibitor That Targets the HIV-1 Envelope and Inhibits CD4 Receptor Binding by Lin, Pin-Fang, Blair, Wade, Wang, Tao, Spicer, Timothy, Guo, Qi, Zhou, Nannan, Gong, Yi-Fei, H. -G. Heidi Wang, Rose, Ronald, Yamanaka, Gregory, Robinson, Brett, Li, Chang-Ben, Fridell, Robert, Deminie, Carol, Demers, Gwendeline, Yang, Zheng, Zadjura, Lisa, Meanwell, Nicholas, Colonno, Richard

“…BMS-378806 is a recently discovered small molecule HIV-1 inhibitor that blocks viral entrance to cells. The compound exhibits potent inhibitory activity…”
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Inhibitors of HIV-1 attachment. Part 7: Indole-7-carboxamides as potent and orally bioavailable antiviral agents by Yeung, Kap-Sun, Qiu, Zhilei, Xue, Quifen, Fang, Haiquan, Yang, Zheng, Zadjura, Lisa, D’Arienzo, Celia J., Eggers, Betsy J., Riccardi, Keith, Shi, Pei-Yong, Gong, Yi-Fei, Browning, Marc R., Gao, Qi, Hansel, Steven, Santone, Kenneth, Lin, Ping-Fang, Meanwell, Nicholas A., Kadow, John F.

“…Optimization of the early lead compound 1 with various carboxamide substitution at the C7 position provided heteroaryl carboxamide analogs (e.g., 35) that…”
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Discovery of 4-Benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806):  A Novel HIV-1 Attachment Inhibitor That Interferes with CD4-gp120 Interactions by Wang, Tao, Zhang, Zhongxing, Wallace, Owen B, Deshpande, Milind, Fang, Haiquan, Yang, Zheng, Zadjura, Lisa M, Tweedie, Donald L, Huang, Stella, Zhao, Fang, Ranadive, Sunanda, Robinson, Brett S, Gong, Yi-Fei, Ricarrdi, Keith, Spicer, Timothy P, Deminie, Carol, Rose, Ronald, Wang, Hwei-Gene Heidi, Blair, Wade S, Shi, Pei-Yong, Lin, Pin-fang, Colonno, Richard J, Meanwell, Nicholas A

“…Indole derivative 1 interferes with the interaction of the HIV surface protein gp120 with the host cell receptor CD4. The 4-fluoro derivative 2 exhibited…”
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Inhibitors of HIV-1 attachment. Part 8: The effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors by Yeung, Kap-Sun, Qiu, Zhilei, Yin, Zhiwei, Trehan, Ashok, Fang, Haiquan, Pearce, Bradley, Yang, Zheng, Zadjura, Lisa, D’Arienzo, Celia J., Riccardi, Keith, Shi, Pei-Yong, Spicer, Timothy P., Gong, Yi-Fei, Browning, Marc R., Hansel, Steven, Santone, Kenneth, Barker, Jonathan, Coulter, Thomas, Lin, Ping-Fang, Meanwell, Nicholas A., Kadow, John F.

“…Optimization of the early lead compound 2 with heteroaryl substitution at the C7 position identified inhibitors with picomolar inhibitory activity. These…”
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Inhibitors of HIV-1 attachment. Part 4: A study of the effect of piperazine substitution patterns on antiviral potency in the context of indole-based derivatives by Wang, Tao, Kadow, John F., Zhang, Zhongxing, Yin, Zhiwei, Gao, Qi, Wu, Dedong, Parker, Dawn DiGiugno, Yang, Zheng, Zadjura, Lisa, Robinson, Brett A., Gong, Yi-Fei, Blair, Wade S., Shi, Pei-Yong, Yamanaka, Gregory, Lin, Pin-Fang, Meanwell, Nicholas A.

“…4-Fluoro- and 4-methoxy-1-(4-benzoylpiperazin-1-yl)-2-(1 H-indol-3-yl)ethane-1,2-dione ( 2 and 3, respectively) have been characterized as potent inhibitors of…”
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Inhibitors of HIV-1 attachment. Part 2: An initial survey of indole substitution patterns by MEANWELL, Nicholas A, WALLACE, Owen B, YEUNG, Kap-Sun, ZHILEI QIU, WRIGHT, J. J. Kim, ZHENG YANG, ZADJURA, Lisa, TWEEDIE, Donald L, YEOLA, Suresh, FANG ZHAO, RANADIVE, Sunanda, ROBINSON, Brett A, HAIQUAN FANG, GONG, Yi-Fei, WANG, Hwei-Gene Heidi, BLAIR, Wade S, SHI, Pei-Yong, COLONNO, Richard J, LIN, Pin-Fang, WANG, Henry, DESHPANDE, Milind, TAO WANG, ZHIWEI YIN, ZHONGXING ZHANG, PEARCE, Bradley C, JAMES, Jennifer

“…The effects of introducing simple halogen, alkyl, and alkoxy substituents to the 4, 5, 6 and 7 positions of…”
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Orally Active Fusion Inhibitor of Respiratory Syncytial Virus by Cianci, Christopher, Yu, Kuo-Long, Combrink, Keith, Sin, Ny, Pearce, Bradley, Wang, Alan, Civiello, Rita, Voss, Stacey, Luo, Guangxiang, Kadow, Kathy, Genovesi, Eugene V, Venables, Brian, Gulgeze, Hatice, Trehan, Ashok, James, Jennifer, Lamb, Lucinda, Medina, Ivette, Roach, Julia, Yang, Zheng, Zadjura, Lisa, Colonno, Richard, Clark, Junius, Meanwell, Nicholas, Krystal, Mark

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Utilization of in vitro Caco-2 permeability and liver microsomal half-life screens in discovering BMS-488043, a novel HIV-1 attachment inhibitor with improved pharmacokinetic properties by Yang, Zheng, Zadjura, Lisa M, Marino, Anthony M, D'Arienzo, Celia J, Malinowski, Jacek, Gesenberg, Christoph, Lin, Pin-Fang, Colonno, Richard J, Wang, Tao, Kadow, John F, Meanwell, Nicholas A, Hansel, Steven B

“…Optimizing pharmacokinetic properties to improve oral exposure is a common theme in modern drug discovery. In the present work, in vitro Caco-2 permeability…”
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Oral Efficacy of a Respiratory Syncytial Virus Inhibitor in Rodent Models of Infection by CIANCI, Christopher, GENOVESI, Eugene V, COMBRINK, Keith, ZHUFANG LI, COLONNO, Richard, MEANWELL, Nicholas, CLARK, Junius, KRYSTAL, Mark, LAMB, Lucinda, MEDINA, Ivette, ZHENG YANG, ZADJURA, Lisa, HYEKYUNG YANG, D'ARIENZO, Celia, NY SIN, YU, Kuo-Long

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Inhibitors of HIV-1 attachment. Part 9: An assessment of oral prodrug approaches to improve the plasma exposure of a tetrazole-containing derivative by Yeung, Kap-Sun, Qiu, Zhilei, Yang, Zheng, Zadjura, Lisa, D’Arienzo, Celia J., Browning, Marc R., Hansel, Steven, Huang, Xiaohua Stella, Eggers, Betsy J., Riccardi, Keith, Lin, Ping-Fang, Meanwell, Nicholas A., Kadow, John F.

“…N-Acetoxymethyl 4, N-pivaloyloxymethyl 5, and N-methyl 6 were evaluated as potential oral prodrugs of the parent tetrazole 3 in rats. Prodrug 5 was ineffective…”
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Respiratory syncytial virus fusion inhibitors. Part 7: Structure–activity relationships associated with a series of isatin oximes that demonstrate antiviral activity in vivo by Sin, Ny, Venables, Brian L., Combrink, Keith D., Gulgeze, H. Belgin, Yu, Kuo-Long, Civiello, Rita L., Thuring, Jan, Wang, X. Alan, Yang, Zheng, Zadjura, Lisa, Marino, Anthony, Kadow, Kathleen F., Cianci, Christopher W., Clarke, Junius, Genovesi, Eugene V., Medina, Ivette, Lamb, Lucinda, Krystal, Mark, Meanwell, Nicholas A.

“…A series of bezimidazole-isatin oximes were prepared and profiled as inhibitors of respiratory syncytial virus (RSV) replication in cell culture…”
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Respiratory syncytial virus fusion inhibitors. Part 4: Optimization for oral bioavailability by Yu, Kuo-Long, Sin, Ny, Civiello, Rita L., Wang, X. Alan, Combrink, Keith D., Gulgeze, H. Belgin, Venables, Brian L., Wright, J.J. Kim, Dalterio, Richard A., Zadjura, Lisa, Marino, Anthony, Dando, Sandra, D’Arienzo, Celia, Kadow, Kathleen F., Cianci, Christopher W., Li, Zhufang, Clarke, Junius, Genovesi, Eugene V., Medina, Ivette, Lamb, Lucinda, Colonno, Richard J., Yang, Zheng, Krystal, Mark, Meanwell, Nicholas A.

“…A series of benzimidazole-based inhibitors of respiratory syncytial virus (RSV) fusion were optimized for antiviral potency, membrane permeability and…”
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Respiratory syncytial virus fusion inhibitors. Part 6: An examination of the effect of structural variation of the benzimidazol-2-one heterocycle moiety by Combrink, Keith D., Gulgeze, H. Belgin, Thuring, Jan W., Yu, Kuo-Long, Civiello, Rita L., Zhang, Yi, Pearce, Bradley C., Yin, Zhiwei, Langley, David R., Kadow, Kathleen F., Cianci, Christopher W., Li, Zhufang, Clarke, Junius, Genovesi, Eugene V., Medina, Ivette, Lamb, Lucinda, Yang, Zheng, Zadjura, Lisa, Krystal, Mark, Meanwell, Nicholas A.

“…The effect of structural variation of the benzimidazol-2-one ring of RSV fusion inhibitors related to BMS-433771 ( 1) was examined in conjunction with side…”
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Corrigendum to “Inhibitors of HIV-1 attachment. Part 4: A study of the effect of piperazine substitution patterns on antiviral potency in the context of indole-based derivatives” [Bioorg. Med. Chem. Lett. 19 (2009) 5140] by Wang, Tao, Kadow, John F., Zhang, Zhongxing, Yin, Zhiwei, Gao, Qi, Wu, Dedong, Parker, Dawn DiGiugno, Yang, Zheng, Zadjura, Lisa, Robinson, Brett A., Gong, Yi-Fei, Spicer, Timothy P., Blair, Wade S., Shi, Pei-Yong, Yamanaka, Gregory, Lin, Pin-Fang, Meanwell, Nicholas A.

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Corrigendum to “Inhibitors of HIV-1 attachment. Part 2: An initial survey of indole substitution patterns” [Bioorg. Med. Chem. Lett. 19 (2009) 1977] by Meanwell, Nicholas A., Wallace, Owen B., Fang, Haiquan, Wang, Henry, Deshpande, Milind, Wang, Tao, Yin, Zhiwei, Zhang, Zhongxing, Pearce, Bradley C., James, Jennifer, Yeung, Kap-Sun, Qiu, Zhilei, Wright, J.J. Kim, Yang, Zheng, Zadjura, Lisa, Tweedie, Donald L., Yeola, Suresh, Zhao, Fang, Ranadive, Sunanda, Robinson, Brett A., Gong, Yi-Fei, Wang, Hwei-Gene Heidi, Spicer, Timothy P., Blair, Wade S., Shi, Pei-Yong, Colonno, Richard J., Lin, Pin-fang

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Preclinical pharmacokinetics of a novel HIV-1 attachment inhibitor BMS-378806 and prediction of its human pharmacokinetics by Yang, Zheng, Zadjura, Lisa, D'Arienzo, Celia, Marino, Anthony, Santone, Kenneth, Klunk, Lewis, Greene, Douglas, Lin, Pin-Fang, Colonno, Richard, Wang, Tao, Meanwell, Nicholas, Hansel, Steven

“…BMS‐378806 is a prototype of novel HIV attachment inhibitors that block the gp120 and CD4 interaction, the first step of HIV‐1 entry into cells. The present…”
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Corrigendum to “Respiratory syncytial virus fusion inhibitors. Part 4: Optimization for oral bioavailability” [Bioorg. Med. Chem. Lett. 17 (2007) 895–901] by Yu, Kuo-Long, Sin, Ny, Civiello, Rita L., Wang, X. Alan, Combrink, Keith D., Gulgeze, H. Belgin, Venables, Brian L., Kim Wright, J.J., Dalterio, Richard A., Zadjura, Lisa, Marino, Anthony, Dando, Sandra, D’Arienzo, Celia, Kadow, Kathleen F., Cianci, Christopher W., Li, Zhufang, Clarke, Junius, Genovesi, Eugene V., Medina, Ivette, Lamb, Lucinda, Colonno, Richard J., Yang, Zheng, Krystal, Mark, Meanwell, Nicholas A.

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Orally active fusion inhibitor of respiratory syncytial virus by CIANCI, Christopher, YU, Kuo-Long, GENOVESI, Eugene V, VENABLES, Brian, GULGEZE, Hatice, TREHAN, Ashok, JAMES, Jennifer, LAMB, Lucinda, MEDINA, Ivette, ROACH, Julia, ZHENG YANG, ZADJURA, Lisa, COMBRINK, Keith, COLONNO, Richard, CLARK, Junius, MEANWELL, Nicholas, KRYSTAL, Mark, NY SIN, PEARCE, Bradley, WANG, Alan, CIVIELLO, Rita, VOSS, Stacey, GUANGXIANG LUO, KADOW, Kathy

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Discovery of 4-benzoyl-1-[(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2-(R)-methylpi p erazine (BMS-378806): A novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions by TAO WANG, ZHONGXING ZHANG, RANADIVE, Sunanda, ROBINSON, Brett S, GONG, Yi-Fei, RICARRDI, Keith, SPICER, Timothy P, DEMINIE, Carol, ROSE, Ronald, WANG, Hwei-Gene Heidi, BLAIR, Wade S, SHI, Pei-Yong, WALLACE, Owen B, LIN, Pin-Fang, COLONNO, Richard J, MEANWELL, Nicholas A, DESHPANDE, Milind, HAIQUAN FANG, ZHENG YANG, ZADJURA, Lisa M, TWEEDIE, Donald L, HUANG, Stella, FANG ZHAO

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