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Your search keyword '"Zhu, Yongbao"' showing total 3 results
Start Over Author "Zhu, Yongbao" Journal bioorganic medicinal chemistry letters
3 results on '"Zhu, Yongbao"'

1. Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.

Author

Skerlj R, Bridger G, Zhou Y, Bourque E, McEachern E, Langille J, Harwig C, Veale D, Yang W, Li T, Zhu Y, Bey M, Baird I, Sartori M, Metz M, Mosi R, Nelson K, Bodart V, Wong R, Fricker S, Mac Farland R, Huskens D, and Schols D

Subjects
Amides chemistry, Amides pharmacology, Animals, Anti-HIV Agents chemistry, Anti-HIV Agents pharmacology, Dogs, Humans, Inhibitory Concentration 50, Molecular Structure, Piperidines chemical synthesis, Piperidines chemistry, Piperidines pharmacology, Pyridines chemical synthesis, Pyridines chemistry, Pyridines pharmacology, Rats, Virus Replication drug effects, Amides chemical synthesis, Anti-HIV Agents chemical synthesis, CCR5 Receptor Antagonists, Drug Design, HIV-1, Leukocytes, Mononuclear drug effects
Abstract

A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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2. Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.

Author

Skerlj R, Bridger G, McEachern E, Harwig C, Smith C, Kaller A, Veale D, Yee H, Skupinska K, Wauthy R, Wang L, Baird I, Zhu Y, Burrage K, Yang W, Sartori M, Huskens D, De Clercq E, and Schols D

Subjects
Aminoquinolines, Animals, Anti-HIV Agents chemistry, Anti-HIV Agents pharmacokinetics, Benzimidazoles, Butylamines, DNA Replication drug effects, Dogs, HIV-1 physiology, Heterocyclic Compounds, 1-Ring chemistry, Molecular Structure, Rats, Anti-HIV Agents chemical synthesis, Drug Design, HIV-1 drug effects, Receptors, CXCR4 antagonists & inhibitors, Virus Replication drug effects
Abstract

A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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3. Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.

Author

Skerlj R, Bridger G, McEachern E, Harwig C, Smith C, Wilson T, Veale D, Yee H, Crawford J, Skupinska K, Wauthy R, Yang W, Zhu Y, Bogucki D, Di Fluri M, Langille J, Huskens D, De Clercq E, and Schols D

Subjects
Administration, Oral, Aminoquinolines, Animals, Anti-HIV Agents chemistry, Anti-HIV Agents pharmacokinetics, Benzimidazoles, Butylamines, Calcium Signaling, Dogs, HIV-1 physiology, Heterocyclic Compounds, 1-Ring chemistry, Humans, Rats, Receptors, CXCR4 metabolism, Structure-Activity Relationship, Anti-HIV Agents chemical synthesis, HIV-1 drug effects, Receptors, CXCR4 antagonists & inhibitors, Virus Replication drug effects
Abstract

An early lead from the AMD070 program was optimized and a structure-activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca(2+) flux inhibition that displayed good pharmacokinetics in rat and dog., (Copyright © 2010 Elsevier Ltd. All rights reserved.)

Published
2011
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