Synthesis and evaluation of urea and thiourea derivatives of lopinavir intermediate as potent antimicrobial, antioxidant agents and molecular docking studies against Staphopain

Synthesis and evaluation of urea and thiourea derivatives of lopinavir intermediate as potent... Keywords Lopinavir intermediate  Isocyanates  Isothiocyanates  Antimicrobial and antioxidant activity  Molecular docking studies Introduction HIV-1 protease inhibitors have emerged as some of the most powerful anti-HIV drugs reported to date, and they are the main components of highly active antiretroviral therapy (HAART) [1, 2]. Currently, there are nine HIV-1 protease inhibitors FDA approved for the effective treatment of AIDS, and some are marked darunavir (DRV) (1), ritonavir RTV) (2), lopinavir (LPV) (3), and amprenavir (APV) (4), as shown in Fig. 1. All these drugs are competitive inhibitors that bind in the active site of the enzyme [3]. Among the HIV aspartyl protease inhibitors, lopinavir is highly potent and plays a critical role in the conversion of viral Gag and O O NH H O N N N O O OH S N OH Ritonavir (RTV) NH O N N N NH O N OH O OH Amprenavir (APV) Lopinavir (LPV) Fig. 1 Important HIV-1 protease inhibitors Darunavir (DRV) Cysteine protease inhibition by lopinavir intermediate 105 Gag–Pol polyproteins into structural and functional proteins, which are essential for viral maturation in the virus life cycle [4]. The treatment of bacterial infections is a challenging therapeutic problem in the http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Synthesis and evaluation of urea and thiourea derivatives of lopinavir intermediate as potent antimicrobial, antioxidant agents and molecular docking studies against Staphopain

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Publisher
Springer Netherlands
Copyright
Copyright © 2016 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-016-2609-5
Publisher site
See Article on Publisher Site

Abstract

Keywords Lopinavir intermediate  Isocyanates  Isothiocyanates  Antimicrobial and antioxidant activity  Molecular docking studies Introduction HIV-1 protease inhibitors have emerged as some of the most powerful anti-HIV drugs reported to date, and they are the main components of highly active antiretroviral therapy (HAART) [1, 2]. Currently, there are nine HIV-1 protease inhibitors FDA approved for the effective treatment of AIDS, and some are marked darunavir (DRV) (1), ritonavir RTV) (2), lopinavir (LPV) (3), and amprenavir (APV) (4), as shown in Fig. 1. All these drugs are competitive inhibitors that bind in the active site of the enzyme [3]. Among the HIV aspartyl protease inhibitors, lopinavir is highly potent and plays a critical role in the conversion of viral Gag and O O NH H O N N N O O OH S N OH Ritonavir (RTV) NH O N N N NH O N OH O OH Amprenavir (APV) Lopinavir (LPV) Fig. 1 Important HIV-1 protease inhibitors Darunavir (DRV) Cysteine protease inhibition by lopinavir intermediate 105 Gag–Pol polyproteins into structural and functional proteins, which are essential for viral maturation in the virus life cycle [4]. The treatment of bacterial infections is a challenging therapeutic problem in the

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Jun 20, 2016

References

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