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doi:10.1016/j.bmc.2007.10.052 
Copyright © 2007 Elsevier Ltd All rights reserved.
Design, synthesis and structure–activity study of shorter hexa peptide analogues as HIV-1 protease inhibitors
Received 20 April 2007;
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Abstract
Inhibition of HIV-1 protease enzyme can render the Human Immunodeficiency Virus (HIV-1) non-infectious in vitro. Previous studies have shown that several shorter peptides were discovered as HIV-1 protease inhibitors. In this context, a series of shorter synthetic hexapeptides, Leu-Leu-Glu-Tyr-Val-Xaa (Xaa = Phe, Met, Tyr and Trp), were designed. The synthesized hexa peptides were screened for their HIV-1 protease inhibition. These peptides showed moderately good HIV-1 protease inhibition when compared to acetyl pepstatin.
Graphical abstract
The design, synthesis and HIV-1 protease inhibition of the shorter synthetic hexa peptides are discussed. Leu-Leu-Glu-Tyr-Val-Xaa. Where, Xaa = Phe, Met, Tyr or Trp.
Keywords: Human Immunodeficiency Virus; HIV-1 protease; Hexa peptides; Oyester peptides; Structural analogues; Design and synthesis
Article Outline
- 1. Introduction
- 2. Results and discussion
- 2.1. Design of peptides
- 2.2. HIV-1 protease inhibition studies
- 2.3. Structure–activity relationship studies
- 3. Conclusions
- 4. Materials and methods
- 4.1. General
- 4.2. Peptide synthesis
- 4.2.1. Boc-Tyr(2,6-diClBzl)-Val-OMe
- 4.2.2. Boc-Glu(OBzl)-Tyr(2,6-diClBzl)-Val-OMe
- 4.2.3. Boc-Leu-Glu(OBzl)-Tyr(2,6-diClBzl)-Val-OMe
- 4.2.4. Boc-Leu-Leu-Glu(OBzl)-Tyr(2,6-diClBzl)-Val-OMe
- 4.2.5. Boc-Leu-Leu-Glu(OBzl)-Tyr(2,6-diClBzl)-Val-(Xaa)-OMe (Xaa = Phe, Met, Tyr, or Trp)
- 4.2.6. Leu-Leu-Glu-Tyr-Val-(Xaa)-OH (Xaa = Phe, Met, Tyr, or Trp)
- 4.3. HIV-1 protease inhibition studies
- Acknowledgements
- References
