Unexpected Novel Binding Mode of Pyrrolidine-Based Aspartyl Protease Inhibitors: Design, Synthesis and Crystal Structure in Complex with HIV Protease

ChemMedChem ◽  
2006 ◽  
Vol 1 (1) ◽  
pp. 106-117 ◽  
Author(s):  
Edgar Specker ◽  
Jark Böttcher ◽  
Sascha Brass ◽  
Andreas Heine ◽  
Hauke Lilie ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Protease Inhibitors ◽  
Binding Mode ◽  
Hiv Protease ◽  
Aspartyl Protease ◽  
Design Synthesis ◽  
Synthesis And Crystal Structure ◽  
Aspartyl Protease Inhibitors

scholarly journals Inhibitory Activity of Human Immunodeficiency Virus Aspartyl Protease Inhibitors against Encephalitozoon intestinalis Evaluated by Cell Culture-Quantitative PCR Assay

2005 ◽  
Vol 49 (6) ◽  
pp. 2362-2366 ◽  
Author(s):  
Jean Menotti ◽  
Maud Santillana-Hayat ◽  
Bruno Cassinat ◽  
Claudine Sarfati ◽  
Francis Derouin ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Quantitative Pcr ◽  
Inhibitory Effect ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Aspartyl Protease ◽  
Pcr Assay ◽  
Real Time Quantitative Pcr ◽  
Quantitative Pcr Assay ◽  
Aspartyl Protease Inhibitors

ABSTRACT Immune reconstitution might not be the only factor contributing to the low prevalence of microsporidiosis in human immunodeficiency virus (HIV)-infected patients treated with protease inhibitors, as these drugs may exert a direct inhibitory effect against fungi and protozoa. In this study, we developed a cell culture-quantitative PCR assay to quantify Encephalitozoon intestinalis growth in U-373-MG human glioblastoma cells and used this assay to evaluate the activities of six HIV aspartyl protease inhibitors against E. intestinalis. A real-time quantitative PCR assay targeted the E. intestinalis small-subunit rRNA gene. HIV aspartyl protease inhibitors were tested over serial concentrations ranging from 0.2 to 10 mg/liter, with albendazole used as a control. Ritonavir, lopinavir, and saquinavir were able to inhibit E. intestinalis growth, with 50% inhibitory concentrations of 1.5, 2.2, and 4.6 mg/liter, respectively, whereas amprenavir, indinavir, and nelfinavir had no inhibitory effect. Pepstatin A, a reference aspartyl protease inhibitor, could also inhibit E. intestinalis growth, suggesting that HIV protease inhibitors may act through the inhibition of an E. intestinalis-encoded aspartyl protease. These results showed that some HIV protease inhibitors can inhibit E. intestinalis growth at concentrations that are achievable in vivo and that the real-time quantitative PCR assay that we used is a valuable tool for the in vitro assessment of the activities of drugs against E. intestinalis.

Synthesis of New Substituted 4,5-Dihydro-3H-spiro[1,5]-benzoxazepine-2,4′-piperidine and Biological Properties

2006 ◽  
Vol 59 (11) ◽  
pp. 812 ◽  
Author(s):  
Younes Laras ◽  
Nicolas Pietrancosta ◽  
Vincent Moret ◽  
Sylvain Marc ◽  
Cédrik Garino ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Functional Groups ◽  
Biological Properties ◽  
Hiv Protease ◽  
Aspartyl Protease ◽  
Electronic Effects ◽  
The Creation ◽  
Hiv 1 ◽  
Bace 1 ◽  
Aspartyl Protease Inhibitors

The reduction of substituted spiro-piperidinyl chromanone oximes with DIBAH reagents has been known to afford the corresponding substituted 4,5-dihydro-3H-spiro[1,5]-benzoxazepine-2,4′-piperidine. The position and electronic effects of the substituents on the aryl moiety control the observed rearrangement. Spiro-benzoxazepine analogue 5j represents a key intermediate for the creation of a library of diverse potential bioactive drugs. With three functional groups that could be selectively and orthogonally protected, many different substituents can be introduced. The obtained analogues were assayed as the possible aspartyl protease inhibitors HIV protease (HIV-1), and β-secretase (BACE-1).

Design, synthesis and crystal structure of six macrocyclic complexes as efficient and effective nitric oxide scavengers

Polyhedron ◽  
2018 ◽  
Vol 156 ◽  
pp. 249-256 ◽  
Author(s):  
Qingrong Cheng ◽  
Yuqi Wan ◽  
Liwen Wang ◽  
Guiying Liao ◽  
Zhiquan Pan
Keyword(s):  
Crystal Structure ◽  
Nitric Oxide ◽  
Macrocyclic Complexes ◽  
Design Synthesis ◽  
Synthesis And Crystal Structure

Pyrrolinone-Based HIV Protease Inhibitors. Design, Synthesis, and Antiviral Activity: Evidence for Improved Transport

1995 ◽  
Vol 117 (45) ◽  
pp. 11113-11123 ◽  
Author(s):  
Amos B Smith ◽  
Ralph Hirschmann ◽  
Alexander Pasternak ◽  
Mark C. Guzman ◽  
Akihisa Yokoyama ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Design Synthesis

Analogues of Key Precursors of Aspartyl Protease Inhibitors:  Synthesis of Trifluoromethyl Amino Epoxides

2005 ◽  
Vol 70 (2) ◽  
pp. 699-702 ◽  
Author(s):  
Nguyen Thi Ngoc Tam ◽  
Guillaume Magueur ◽  
Michèle Ourévitch ◽  
Benoit Crousse ◽  
Jean-Pierre Bégué ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Aspartyl Protease ◽  
Aspartyl Protease Inhibitors

HIV aspartyl protease inhibitors modify the percentage of activated leukocytes, as well as serum levels of IL-17A and NO during experimental leishmaniasis

2018 ◽  
Vol 60 ◽  
pp. 179-188 ◽  
Author(s):  
Daniele Luísa Ribeiro Alvarenga ◽  
Amanda Helen dos Santos Silva ◽  
Jacqueline Araújo Fiuza ◽  
Soraya Torres Gaze ◽  
Jaquelline Germano de Oliveira ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Serum Levels ◽  
Aspartyl Protease ◽  
Aspartyl Protease Inhibitors

Quinic Acid Derivatives as Sialyl Lewisx-Mimicking Selectin Inhibitors:  Design, Synthesis, and Crystal Structure in Complex with E-Selectin

2005 ◽  
Vol 48 (13) ◽  
pp. 4346-4357 ◽  
Author(s):  
Neelu Kaila ◽  
William S. Somers ◽  
Bert E. Thomas ◽  
Paresh Thakker ◽  
Kristin Janz ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Quinic Acid ◽  
Sialyl Lewisx ◽  
Design Synthesis ◽  
Synthesis And Crystal Structure

scholarly journals Novel aspartyl protease inhibitors, YF-0200R-A and B.

1994 ◽  
Vol 47 (5) ◽  
pp. 566-570 ◽  
Author(s):  
TSUTOMU SATO ◽  
KOJI NAGAI ◽  
MITSUYOSHI SHIBAZAKI ◽  
KENJI ABE ◽  
YUKIHIRO TAKEBAYASHI ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Aspartyl Protease ◽  
Aspartyl Protease Inhibitors
Sign in / Sign up

Export Citation Format

Share Document