Zobrazeno 1 - 10 of 46 pro vyhledávání: '"Dawn D. Parker"'
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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
Autor: B. Narasimhulu Naidu, Manoj Patel, Brian McAuliffe, Bo Ding, Christopher Cianci, Jean Simmermacher, Susan Jenkins, Dawn D. Parker, Prasanna Sivaprakasam, Javed A. Khan, Kevin Kish, Hal Lewis, Umesh Hanumegowda, Mark Krystal, Nicholas A. Meanwell, John F. Kadow
Publikováno v: Journal of medicinal chemistry. 65(6)
Allosteric HIV-1 integrase inhibitors (ALLINIs) have garnered special interest because of their novel mechanism of action: they inhibit HIV-1 replication by promoting aberrant integrase multimerization, leading to the production of replication-defici
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3faa42431ce3f1fdb7932f28c2183dd4
https://pubmed.ncbi.nlm.nih.gov/35235334
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4
Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of HIV-1 allosteric integrase inhibitors
Autor: Kyle Parcella, Manoj Patel, Yong Tu, Kyle Eastman, Kevin Peese, Eric Gillis, Makonen Belema, Ira B. Dicker, Brian McAuliffe, Bo Ding, Paul Falk, Jean Simmermacher, Dawn D. Parker, Prasanna Sivaprakasam, Javed A. Khan, Kevin Kish, Hal Lewis, Umesh Hanumegowda, Susan Jenkins, John F. Kadow, Mark Krystal, Nicholas A. Meanwell, B. Narasimhulu Naidu
Publikováno v: Bioorganic & Medicinal Chemistry. 67:116833
Allosteric integrase inhibitors (ALLINIs) of HIV-1 may hold promise as a novel mechanism for HIV therapeutics and cure. Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of ALLINIs provided a series of potent compo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e022b9484eaf5af0acf5fbe2eef0aed
https://doi.org/10.1016/j.bmc.2022.116833
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5
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
Autor: Anuradha Gupta, Ira B. Dicker, Mark Krystal, Tricia Protack, Jacob Swidorski, Yoganand Shanmugam, Susan Jenkins, Alicia Ng, Umesh Hanumegowda, Nicholas A. Meanwell, Dawn D. Parker, Alicia Regueiro-Ren, Brett R. Beno
Publikováno v: Bioorganicmedicinal chemistry letters. 36
GSK3532795 (formerly BMS-955176) is a second-generation HIV-1 maturation inhibitor that has shown broad spectrum antiviral activity and preclinical PK predictive of once-daily dosing in humans. Although efficacy was confirmed in clinical trials, the
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b69b1afb3978f9ed0a66c4cca763dd5
https://pubmed.ncbi.nlm.nih.gov/33508465
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6
Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors
Autor: B. Narasimhulu Naidu, Brian McAuliffe, Jean Simmermacher, Mark Krystal, Dawn D. Parker, Nicholas A. Meanwell, Manoj Patel, Christopher W. Allard, Linda Discotto, Beatrice Minassian, Susan Jenkins, Christopher Cianci
Publikováno v: Bioorganicmedicinal chemistry letters. 30(21)
The design, synthesis and structure–activity relationships associated with a series of C2-substituted pyrazolopyrimidines as potent allosteric inhibitors of HIV-1 integrase (ALLINIs) are described. Structural modifications to these molecules were m
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f04d4fc9b0f588386489c6c450364e5c
https://pubmed.ncbi.nlm.nih.gov/32860982
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7
Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors
Autor: B. Narasimhulu Naidu, Dawn D. Parker, Helen Higley, Tricia Protack, Susan Jenkins, Manoj Patel, Zeyu Lin, Nicholas A. Meanwell, Brian Terry, Ira B. Dicker, Arvind Mathur, Chiradeep Panja, Michael A. Walker, Mark Krystal, Richard Rampulla
Publikováno v: Bioorganicmedicinal chemistry. 28(13)
The design, synthesis and structure-activity relationships associated with a series of bridged tricyclic pyrimidinone carboxamides as potent inhibitors of HIV-1 integrase strand transfer are described. Structural modifications to these molecules were
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16c6cd4134d454e316295d1cfacfe459
https://pubmed.ncbi.nlm.nih.gov/32389483
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