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65236

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

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Last updated: 25 Dec 2024

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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.

DOI

10.21608/bfsa.2005.65236

Authors

First Name

Hamdy

Last Name

Abdel-Rahman

MiddleName

M.

Affiliation

Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

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First Name

Nawal

Last Name

El-Koussi

MiddleName

A.

Affiliation

Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

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Orcid

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First Name

Gamal

Last Name

Alkaramany

MiddleName

S.

Affiliation

Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

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Orcid

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First Name

Adel

Last Name

Youssef

MiddleName

F.

Affiliation

Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

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City

-

Orcid

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First Name

Yoshiaki

Last Name

Kiso

MiddleName

-

Affiliation

Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Kyoto, 607-8412 Japan

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Volume

28

Article Issue

1

Related Issue

9815

Issue Date

2005-06-01

Receive Date

2004-11-22

Publish Date

2005-06-30

Page Start

95

Page End

103

Print ISSN

1110-0052

Online ISSN

3009-7703

Article File

BFSA_Volume 28_Issue 1_Pages 95-103.pdf

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https://bpsa.journals.ekb.eg/article_65236.html

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https://bpsa.journals.ekb.eg/service?article_code=65236

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Type

Original Article

Type Code

1,096

Publication Type

Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

Publication Link

https://bpsa.journals.ekb.eg/

MainTitle

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

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Article

Created At

22 Jan 2023