Search Results - "Parker, Dawn D"

Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors by Naidu, B. Narasimhulu, Sorenson, Margaret E., Patel, Manoj, Ueda, Yasutsugu, Banville, Jacques, Beaulieu, Francis, Bollini, Sagarika, Dicker, Ira B., Higley, Helen, Lin, Zeyu, Pajor, Lori, Parker, Dawn D., Terry, Brian J., Zheng, Ming, Martel, Alain, Meanwell, Nicholas A., Krystal, Mark, Walker, Michael A.

“…[Display omitted] Integration of viral DNA into the host cell genome is an obligatory process for successful replication of HIV-1. Integrase catalyzes the…”
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Discovery of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain by Dzierba, Carolyn D., Dasgupta, Bireshwar, Karageorge, George, Kostich, Walter, Hamman, Brian, Allen, Jason, Esposito, Kim M., Padmanabha, Ramesh, Grace, James, Lentz, Kimberley, Morrison, John, Morgan, Daniel, Easton, Amy, Bourin, Clotilde, Browning, Marc R., Rajamani, Ramkumar, Good, Andrew, Parker, Dawn D., Muckelbauer, Jodi K., Khan, Javed, Camac, Daniel, Ghosh, Kaushik, Halan, Vivek, Lippy, Jonathan S., Santone, Kenneth S., Denton, R. Rex, Westphal, Ryan, Bristow, Linda J., Conway, Charles M., Bronson, Joanne J., Macor, John E.

“…Adaptor protein 2-associated kinase 1 (AAK1) is a member of the Ark1/Prk1 family of serine/threonine kinases and plays a role in modulating receptor…”
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Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir by Wang, Tao, Ueda, Yasu, Zhang, Zhongxing, Yin, Zhiwei, Matiskella, John, Pearce, Bradley C, Yang, Zheng, Zheng, Ming, Parker, Dawn D, Yamanaka, Gregory A, Gong, Yi-Fei, Ho, Hsu-Tso, Colonno, Richard J, Langley, David R, Lin, Pin-Fang, Meanwell, Nicholas A, Kadow, John F

“…The optimization of the 4-methoxy-6-azaindole series of HIV-1 attachment inhibitors (AIs) that originated with 1 to deliver temsavir (3, BMS-626529) is…”
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Potent Long-Acting Inhibitors Targeting the HIV‑1 Capsid Based on a Versatile Quinazolin-4-one Scaffold by Gillis, Eric P., Parcella, Kyle, Bowsher, Michael, Cook, James H., Iwuagwu, Christiana, Naidu, B. Narasimhulu, Patel, Manoj, Peese, Kevin, Huang, Haichang, Valera, Lourdes, Wang, Chunfu, Kieltyka, Kasia, Parker, Dawn D., Simmermacher, Jean, Arnoult, Eric, Nolte, Robert T., Wang, Liping, Bender, John A., Frennesson, David B., Saulnier, Mark, Wang, Alan Xiangdong, Meanwell, Nicholas A., Belema, Makonen, Hanumegowda, Umesh, Jenkins, Susan, Krystal, Mark, Kadow, John F., Cockett, Mark, Fridell, Robert

“…Long-acting (LA) human immunodeficiency virus-1 (HIV-1) antiretroviral therapy characterized by a ≥1 month dosing interval offers significant advantages over…”
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5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors by Peese, Kevin M, Allard, Christopher W, Connolly, Timothy, Johnson, Barry L, Li, Chen, Patel, Manoj, Sorensen, Margaret E, Walker, Michael A, Meanwell, Nicholas A, McAuliffe, Brian, Minassian, Beatrice, Krystal, Mark, Parker, Dawn D, Lewis, Hal A, Kish, Kevin, Zhang, Ping, Nolte, Robert T, Simmermacher, Jean, Jenkins, Susan, Cianci, Christopher, Naidu, B. Narasimhulu

“…A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on…”
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Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors by Patel, Manoj, Cianci, Christopher, Allard, Christopher W., Parker, Dawn D., Simmermacher, Jean, Jenkins, Susan, Mcauliffe, Brian, Minassian, Beatrice, Discotto, Linda, Krystal, Mark, Meanwell, Nicholas A., Naidu, B. Narasimhulu

“…The design, synthesis and structure–activity relationships associated with a series of C2-substituted pyrazolopyrimidines as potent allosteric inhibitors of…”
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Design, Synthesis, and Preclinical Profiling of GSK3739936 (BMS-986180), an Allosteric Inhibitor of HIV‑1 Integrase with Broad-Spectrum Activity toward 124/125 Polymorphs by Naidu, B. Narasimhulu, Patel, Manoj, McAuliffe, Brian, Ding, Bo, Cianci, Christopher, Simmermacher, Jean, Jenkins, Susan, Parker, Dawn D, Sivaprakasam, Prasanna, Khan, Javed A, Kish, Kevin, Lewis, Hal, Hanumegowda, Umesh, Krystal, Mark, Meanwell, Nicholas A, Kadow, John F

“…Allosteric HIV-1 integrase inhibitors (ALLINIs) have garnered special interest because of their novel mechanism of action: they inhibit HIV-1 replication by…”
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Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition by Swidorski, Jacob J., Jenkins, Susan, Hanumegowda, Umesh, Parker, Dawn D., Beno, Brett R., Protack, Tricia, Ng, Alicia, Gupta, Anuradha, Shanmugam, Yoganand, Dicker, Ira B., Krystal, Mark, Meanwell, Nicholas A., Regueiro-Ren, Alicia

“…[Display omitted] GSK3532795 (formerly BMS-955176) is a second-generation HIV-1 maturation inhibitor that has shown broad spectrum antiviral activity and…”
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Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of HIV-1 allosteric integrase inhibitors by Parcella, Kyle, Patel, Manoj, Tu, Yong, Eastman, Kyle, Peese, Kevin, Gillis, Eric, Belema, Makonen, Dicker, Ira B., McAuliffe, Brian, Ding, Bo, Falk, Paul, Simmermacher, Jean, Parker, Dawn D., Sivaprakasam, Prasanna, Khan, Javed A., Kish, Kevin, Lewis, Hal, Hanumegowda, Umesh, Jenkins, Susan, Kadow, John F., Krystal, Mark, Meanwell, Nicholas A., Naidu, B. Narasimhulu

“…[Display omitted] Allosteric integrase inhibitors (ALLINIs) of HIV-1 may hold promise as a novel mechanism for HIV therapeutics and cure. Scaffold…”
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Hepatitis C Virus NS5A Replication Complex Inhibitors: The Discovery of Daclatasvir by Belema, Makonen, Nguyen, Van N., Bachand, Carol, Deon, Dan H., Goodrich, Jason T., James, Clint A., Lavoie, Rico, Lopez, Omar D., Martel, Alain, Romine, Jeffrey L., Ruediger, Edward H., Snyder, Lawrence B., Laurent, Denis R. St, Yang, Fukang, Zhu, Juliang, Wong, Henry S., Langley, David R., Adams, Stephen P., Cantor, Glenn H., Chimalakonda, Anjaneya, Fura, Aberra, Johnson, Benjamin M., Knipe, Jay O., Parker, Dawn D., Santone, Kenneth S., Fridell, Robert A., Lemm, Julie A., O’Boyle, Donald R., Colonno, Richard J., Gao, Min, Meanwell, Nicholas A., Hamann, Lawrence G.

“…The biphenyl derivatives 2 and 3 are prototypes of a novel class of NS5A replication complex inhibitors that demonstrate high inhibitory potency toward a panel…”
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The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation by Chen, Yan, Sit, Sing-Yuen, Chen, Jie, Swidorski, Jacob J., Liu, Zheng, Sin, Ny, Venables, Brian L., Parker, Dawn D., Nowicka-Sans, Beata, Lin, Zeyu, Li, Zhufang, Terry, Brian J., Protack, Tricia, Rahematpura, Sandhya, Hanumegowda, Umesh, Jenkins, Susan, Krystal, Mark, Dicker, Ira D., Meanwell, Nicholas A., Regueiro-Ren, Alicia

“…[Display omitted] The design and synthesis of a series of C28 amine-based betulinic acid derivatives as HIV-1 maturation inhibitors is described. This series…”
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The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor by Naidu, B. Narasimhulu, Walker, Michael A., Sorenson, Margaret E., Ueda, Yasutsugu, Matiskella, John D., Connolly, Timothy P., Dicker, Ira B., Lin, Zeyu, Bollini, Sagarika, Terry, Brian J., Higley, Helen, Zheng, Ming, Parker, Dawn D., Wu, Dedong, Adams, Stephen, Krystal, Mark R., Meanwell, Nicholas A.

“…[Display omitted] •Synthesis and antiviral activities of series of pyrimidinone carboxamide described.•BMS-707035 is a potent HIV-1 integrase strand transfer…”
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Discovery and Preclinical Profiling of GSK3839919, a Potent HIV‑1 Allosteric Integrase Inhibitor by Parcella, Kyle, Wang, Tao, Eastman, Kyle, Zhang, Zhongxing, Yin, Zhiwei, Patel, Manoj, Tu, Yong, Zheng, Barbara Zhizhen, Walker, Michael A., Saulnier, Mark G., Frennesson, David, Bowsher, Michael, Gillis, Eric, Peese, Kevin, Belema, Makonen, Cianci, Christopher, Dicker, Ira B., McAuliffe, Brian, Ding, Bo, Falk, Paul, Simmermacher, Jean, Parker, Dawn D., Sivaprakasam, Prasanna, Kish, Kevin, Lewis, Hal, Hanumegowda, Umesh, Jenkins, Susan, Kadow, John F., Krystal, Mark, Meanwell, Nicholas A., Naidu, B. Narasimhulu

“…Allosteric HIV-1 integrase inhibitors (ALLINIs) have been of interest recently because of their novel mechanism of action. Strategic modifications to the C5…”
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Inhibitors of HIV-1 attachment: The discovery and structure–activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore by Swidorski, Jacob J., Liu, Zheng, Yin, Zhiwei, Wang, Tao, Carini, David J., Rahematpura, Sandhya, Zheng, Ming, Johnson, Kim, Zhang, Sharon, Lin, Pin-Fang, Parker, Dawn D., Li, Wenying, Meanwell, Nicholas A., Hamann, Lawrence G., Regueiro-Ren, Alicia

“…[Display omitted] 6,6-Fused ring systems including tetrahydroisoquinolines and tetrahydropyrido[3,4-d]pyrimidines have been explored as possible replacements…”
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Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 12. Structure–Activity Relationships Associated with 4‑Fluoro-6-azaindole Derivatives Leading to the Identification of 1‑(4-Benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl‑1H‑pyrrolo[2,3‑c]pyridin-3-yl)ethane-1,2-dione (BMS-585248) by Regueiro-Ren, Alicia, Xue, Qiufen M, Swidorski, Jacob J, Gong, Yi-Fei, Mathew, Marina, Parker, Dawn D, Yang, Zheng, Eggers, Betsy, D’Arienzo, Celia, Sun, Yongnian, Malinowski, Jacek, Gao, Qi, Wu, Dedong, Langley, David R, Colonno, Richard J, Chien, Caly, Grasela, Dennis M, Zheng, Ming, Lin, Pin-Fang, Meanwell, Nicholas A, Kadow, John F

“…A series of highly potent HIV-1 attachment inhibitors with 4-fluoro-6-azaindole core heterocycles that target the viral envelope protein gp120 has been…”
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Inhibitors of HIV-1 maturation: Development of structure–activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids by Swidorski, Jacob J., Liu, Zheng, Sit, Sing-Yuen, Chen, Jie, Chen, Yan, Sin, Ny, Venables, Brian L., Parker, Dawn D., Nowicka-Sans, Beata, Terry, Brian J., Protack, Tricia, Rahematpura, Sandhya, Hanumegowda, Umesh, Jenkins, Susan, Krystal, Mark, Dicker, Ira B., Meanwell, Nicholas A., Regueiro-Ren, Alicia

“…[Display omitted] We have recently reported on the discovery of a C-3 benzoic acid (1) as a suitable replacement for the dimethyl succinate side chain of…”
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C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitors by Liu, Zheng, Swidorski, Jacob J., Nowicka-Sans, Beata, Terry, Brian, Protack, Tricia, Lin, Zeyu, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Parker, Dawn D., Rahematpura, Sandhya, Jenkins, Susan, Beno, Brett R., Krystal, Mark, Meanwell, Nicholas A., Dicker, Ira B., Regueiro-Ren, Alicia

“…[Display omitted] A series of C-3 phenyl- and heterocycle-substituted derivatives of C-3 deoxybetulinic acid and C-3 deoxybetulin was designed and synthesized…”
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Discovery of BMS-955176, a Second Generation HIV‑1 Maturation Inhibitor with Broad Spectrum Antiviral Activity by Regueiro-Ren, Alicia, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Swidorski, Jacob J, Chen, Jie, Venables, Brian L, Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Beno, Brett R, Huang, Xiaohua S, Rahematpura, Sandhya, Parker, Dawn D, Haskell, Roy, Jenkins, Susan, Santone, Kenneth S, Cockett, Mark I, Krystal, Mark, Meanwell, Nicholas A, Hanumegowda, Umesh, Dicker, Ira B

“…HIV-1 maturation inhibition (MI) has been clinically validated as an approach to the control of HIV-1 infection. However, identifying an MI with both broad…”
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Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176) by Regueiro-Ren, Alicia, Swidorski, Jacob J, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Chen, Jie, Venables, Brian L, Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Easter, John, Beno, Brett R, Arora, Vinod, Huang, Xiaohua S, Rahematpura, Sandhya, Parker, Dawn D, Haskell, Roy, Santone, Kenneth S, Cockett, Mark I, Krystal, Mark, Meanwell, Nicholas A, Jenkins, Susan, Hanumegowda, Umesh, Dicker, Ira B

“…GSK3532795, formerly known as BMS-955176 (1), is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb…”
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Inhibitors of HIV-1 attachment. Part 10. The discovery and structure–activity relationships of 4-azaindole cores by Wang, Tao, Yang, Zhong, Zhang, Zhongxing, Gong, Yi-Fei, Riccardi, Keith A., Lin, Pin-Fang, Parker, Dawn D., Rahematpura, Sandhya, Mathew, Marina, Zheng, Ming, Meanwell, Nicholas A., Kadow, John F., Bender, John A.

“…A series of 4-azaindole oxoacetic acid piperazine benzamides was synthesized and evaluated in an effort to identify an oral HIV-1 attachment inhibitor with the…”
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