Zobrazeno 1 - 10 of 19 pro vyhledávání: '"Bruno D. Chapsal"'
1
Design of HIV-1 Protease Inhibitors with C3-Substituted Hexahydrocyclopentafuranyl Urethanes as P2-Ligands: Synthesis, Biological Evaluation, and Protein–Ligand X-ray Crystal Structure
Autor: Melinda Steffey, Johnson Agniswamy, Masayuki Amano, Garth L. Parham, Hiroaki Mitsuya, Arun K. Ghosh, Irene T. Weber, Yuan-Fang Wang, Bruno D. Chapsal
Publikováno v: Journal of Medicinal Chemistry. 54:5890-5901
We report the design, synthesis, biological evaluation, and the X-ray crystal structure of a novel inhibitor bound to the HIV-1 protease. Various C3-functionalized cyclopentanyltetrahydrofurans (Cp-THF) were designed to interact with the flap Gly48 c
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ffda8d89ace68bd0d4838ca47185d52
https://doi.org/10.1021/jm200649p
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2
Novel HIV-1 Protease Inhibitors (PIs) Containing a Bicyclic P2 Functional Moiety, Tetrahydropyrano-Tetrahydrofuran, That Are Potent against Multi-PI-Resistant HIV-1 Variants
Autor: Masayuki Amano, Hiroaki Mitsuya, Ravikiran S. Yedidi, Yasuhiro Koh, Kazuhiko Ide, Manabu Aoki, Sofiya Leschenko, Arun K. Ghosh, Debananda Das, Bruno D. Chapsal
Publikováno v: Antimicrobial Agents and Chemotherapy. 55:1717-1727
We identified GRL-1388 and -1398, potent nonpeptidic human immunodeficiency virus type 1 (HIV-1) protease inhibitors (PIs) containing a bicyclic P2 functional moiety, tetrahydropyrano-tetrahydrofuran (Tp-THF). GRL-1388 was as potent as darunavir (DRV
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::465b80b98986dd5c09c5abcfa20d8921
https://doi.org/10.1128/aac.01540-10
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3
Total Synthesis of Enantiopure (+)-γ-Lycorane Using Highly Efficient Pd-Catalyzed Asymmetric Allylic Alkylation
Autor: Iwao Ojima, Bruno D. Chapsal
Publikováno v: Organic Letters. 8:1395-1398
[reaction: see text] A highly efficient short total synthesis of (+)-gamma-lycorane (99% ee, 41% overall yield) was achieved by using the asymmetric allylic alkylation in the key step catalyzed by palladium complexes with novel chiral biphenol-based
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::abdee7b9762fb9f8644e51c67585b496
https://doi.org/10.1021/ol060181v
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4
Catalytic asymmetric transformations with fine-tunable biphenol-based monodentate ligands
Autor: Bruno D. Chapsal, Zihao Hua, Iwao Ojima
Publikováno v: Tetrahedron: Asymmetry. 17:642-657
A library of new fine-tunable monodentate phosphite and phosphoramidite ligands based on chiral biphenol have been designed and developed. These monodentate phosphorus ligands have exhibited excellent enantioselectivity in the Pd-catalyzed asymmetric
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7dd00e05534a7332385591562f5af583
https://doi.org/10.1016/j.tetasy.2005.12.035
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5
Design of the anti-HIV protease inhibitor darunavir
Autor: Bruno D. Chapsal, Arun K. Ghosh
The development of HIV protease inhibitors (PIs) and their inclusion in highly active antiretroviral therapies (HAARTs) marked the beginning of a treatment breakthrough in the management of human immunodeficiency virus (HIV)/acquired immunodeficiency
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f89dc9b7b9b1823bbf776f596b610a89
https://doi.org/10.1016/b978-0-12-397176-0.00013-3
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6
Substituent effects on P2-cyclopentyltetrahydrofuranyl urethanes: Design, synthesis, and X-ray studies of potent HIV-1 protease inhibitors
Autor: Masayuki Amano, Arun K. Ghosh, Melinda Steffey, Johnson Agniswamy, Bruno D. Chapsal, Hiroaki Mitsuya, Irene T. Weber, Yuan-Fang Wang
The design, synthesis, and biological evaluation of novel C3-substituted cyclopentyltetrahydrofuranyl (Cp-THF)-derived HIV-1 protease inhibitors are described. Various C3-functional groups on the Cp-THF ligand were investigated in order to maximize t
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f00985c88d5db889bb1694829469022
https://europepmc.org/articles/PMC3433276/
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8
Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation
Autor: Abigail Baldridge, Masayuki Amano, Arun K. Ghosh, D. Eric Walters, Bruno D. Chapsal, Hiroaki Mitsuya, Melinda Steffey, Yasuhiro Koh
Publikováno v: Journal of medicinal chemistry. 54(2)
The design, synthesis, and evaluation of a new series of hexahydrofuropyranol-derived HIV-1 protease inhibitors are described. We have designed a stereochemically defined hexahydrofuropyranol-derived urethane as the P2-ligand. The current ligand is d
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ac6e031d6615ab0de98ea582fec68da
https://pubmed.ncbi.nlm.nih.gov/21194227
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10
Design and synthesis of stereochemically defined novel spirocyclic P2-ligands for HIV-1 protease inhibitors
Autor: Yashiro Koh, Bruno D. Chapsal, Abigail Baldridge, Kazuhiko Ide, Hiroaki Mitsuya, Arun K. Ghosh
Publikováno v: Organic letters. 10(22)
The synthesis of a series of stereochemically defined spirocyclic compounds and their use as novel P2-ligands for HIV-1 protease inhibitors are described. The bicyclic core of the ligands was synthesized by an efficient nBu 3SnH-promoted radical cycl
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::36a3ab24159f6c72ea931c103c502bdb
https://pubmed.ncbi.nlm.nih.gov/18928291
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