ALLOPHENYLNORSTATINE-CONTAINING HIV-1 PROTEASE INHIBITORS: DESIGN, SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS FOR SELECTED P2 LIGANDS
Abdel-Rahman, H., El-Koussi, N., Alkaramany, G., Youssef, A., Kiso, Y. (2005). ALLOPHENYLNORSTATINE-CONTAINING HIV-1 PROTEASE INHIBITORS: DESIGN, SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS FOR SELECTED P2 LIGANDS. EKB Journal Management System, 28(1), 95-103. doi: 10.21608/bfsa.2005.65236
Hamdy M. Abdel-Rahman; Nawal A. El-Koussi; Gamal S. Alkaramany; Adel F. Youssef; Yoshiaki Kiso. "ALLOPHENYLNORSTATINE-CONTAINING HIV-1 PROTEASE INHIBITORS: DESIGN, SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS FOR SELECTED P2 LIGANDS". EKB Journal Management System, 28, 1, 2005, 95-103. doi: 10.21608/bfsa.2005.65236
Abdel-Rahman, H., El-Koussi, N., Alkaramany, G., Youssef, A., Kiso, Y. (2005). 'ALLOPHENYLNORSTATINE-CONTAINING HIV-1 PROTEASE INHIBITORS: DESIGN, SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS FOR SELECTED P2 LIGANDS', EKB Journal Management System, 28(1), pp. 95-103. doi: 10.21608/bfsa.2005.65236
Abdel-Rahman, H., El-Koussi, N., Alkaramany, G., Youssef, A., Kiso, Y. ALLOPHENYLNORSTATINE-CONTAINING HIV-1 PROTEASE INHIBITORS: DESIGN, SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS FOR SELECTED P2 LIGANDS. EKB Journal Management System, 2005; 28(1): 95-103. doi: 10.21608/bfsa.2005.65236

ALLOPHENYLNORSTATINE-CONTAINING HIV-1 PROTEASE INHIBITORS: DESIGN, SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS FOR SELECTED P2 LIGANDS

Bulletin of Pharmaceutical Sciences Assiut University
Article 11, Volume 28, Issue 1, June 2005, Page 95-103  XML PDF (250.46 K)
Document Type: Original Article
DOI: 10.21608/bfsa.2005.65236
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Authors
Hamdy M. Abdel-Rahman1; Nawal A. El-Koussi* 1; Gamal S. Alkaramany1; Adel F. Youssef1; Yoshiaki Kiso2
1Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
2Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Kyoto, 607-8412 Japan
Abstract
The design and development of potent HIV protease inhibitors remain an attractive target for antiviral therapy. A novel class of HIV protease inhibitors containing allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid] as a transition state mimic have been reported. In this work we fixed P2` (as tert-butylamino or 2-methylbenzylamino) and changed P2 moiety to provide two series of dipeptide analogs. Preliminary evaluation of the activity of the synthesized derivatives were determined as percentage of enzyme inhibition at 5  M level. The results showed that the introduction of 2-methylbenzylamino moiety as P2` ligand 6a-e considerably improved HIV inhibitory activity in comparison with the tert-butyl amino analogs 5a-e. It was found that compounds in both series retained activity still less than the lead compounds KNI-577 and KNI-727.
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