التفاصيل البيبلوغرافية
العنوان:
1,3,4 trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains
المؤلفون:
Margaret A. Cascieri , Salvatore J. Siciliano , Karen Holmes , Sandra L. Gould , Kevin T. Chapman , William A. Schleif , J. J. Hale , Richard J. Budhu , Renee Danzeisen , Joseph Kessler , Anthony Carella , Julie A. DeMartino , Christopher A. Willoughby , Daria J. Hazuda , Sander G. Mills , Malcolm MacCoss , Michael W. Miller , Janet Lineberger , Emilio A. Emini , Lorraine Malkowitz , Keith G. Rosauer , Martin S. Springer , Gwen Carver
المصدر:
Bioorganic & Medicinal Chemistry Letters . 13:427-431
بيانات النشر:
Elsevier BV, 2003.
سنة النشر:
2003
مصطلحات موضوعية:
Pyrrolidines , Anti-HIV Agents , Stereochemistry , Clinical Biochemistry , Pharmaceutical Science , CHO Cells , CCR5 receptor antagonist , Biochemistry , Chemical synthesis , Pyrrolidine , chemistry.chemical_compound , Piperidines , In vivo , Cricetinae , Drug Discovery , Side chain , Animals , Humans , Chemokine CCL4 , Molecular Biology , Organic Chemistry , Antagonist , Hydrogen Bonding , Macrophage Inflammatory Proteins , In vitro , Rats , chemistry , CCR5 Receptor Antagonists , Molecular Medicine , Piperidine , Half-Life , HeLa Cells
الوصف:
A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding affinity (1.8 nM) and antiviral activity in PBMC's (IC95=50 nM). Compound 4a also has improved PK properties relative to 1.
تدمد:
0960-894X
DOI:
10.1016/s0960-894x(02)00988-5
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f017f22030882b47e409faa3a0cd7e8 https://doi.org/10.1016/s0960-894x (02)00988-5
Rights:
CLOSED
رقم الانضمام:
edsair.doi.dedup.....1f017f22030882b47e409faa3a0cd7e8
قاعدة البيانات:
OpenAIRE