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Your search keyword '"Lu, Zhijian"' showing total 4 results
Start Over Author "Lu, Zhijian" Topic hiv
4 results on '"Lu, Zhijian"'

1. Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.

Author

Lu Z, Bohn J, Rano T, Rutkowski CA, Simcoe AL, Olsen DB, Schleif WA, Carella A, Gabryelski L, Jin L, Lin JH, Emini E, Chapman K, and Tata JR

Subjects
Administration, Oral, Biological Availability, Drug Resistance, Viral, HIV enzymology, HIV Protease drug effects, HIV Protease Inhibitors administration & dosage, Molecular Structure, HIV drug effects, HIV Protease Inhibitors chemistry, HIV Protease Inhibitors pharmacology, Indinavir analogs & derivatives
Abstract

Efforts directed to identifying potent HIV protease inhibitors (PI) have yielded a class of compounds that are not only very active against wild-type (NL4-3) HIV virus but also very potent against a panel of PI-resistant viral isolates. Chemistry and biology are described.

Published
2005
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2. Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.

Author

Cheng Y, Zhang F, Rano TA, Lu Z, Schleif WA, Gabryelski L, Olsen DB, Stahlhut M, Rutkowski CA, Lin JH, Jin L, Emini EA, Chapman KT, and Tata JR

Subjects
Animals, Area Under Curve, Dogs, Drug Resistance, HIV Protease drug effects, HIV Protease Inhibitors metabolism, HIV Protease Inhibitors pharmacokinetics, Humans, Indinavir metabolism, Indinavir pharmacokinetics, Inhibitory Concentration 50, Metabolic Clearance Rate, Structure-Activity Relationship, Tumor Cells, Cultured, HIV drug effects, HIV Protease Inhibitors chemical synthesis, Indinavir analogs & derivatives
Abstract

Indinavir analogues with blocked metabolism sites show highly improved pharmacokinetic profiles in animals. The cis-aminochromanol substituted analogues exhibited excellent potency against both the wild-type (NL4-3) virus and protease inhibitor-resistant HIV strains.

Published
2002
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3. Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus

Author

Raghavan, Subharekha, Lu, Zhijian, Beeson, Teresa, Chapman, Kevin T., Schleif, William A., Olsen, David B., Stahlhut, Mark, Rutkowski, Carrie A., Gabryelski, Lori, Emini, Emilio, and Tata, James R.

Subjects
*HIV, *HTLV, *ENZYME inhibitors, *PROTEASE inhibitors
Abstract

Abstract: A series of HIV protease inhibitors with modifications on the P3 position have been designed and synthesized. These compounds exhibit excellent antiviral activity against both the wild type enzyme and PI-resistant clinical viral isolates. The synthesis and biological activity of the compounds are described. [Copyright &y& Elsevier]

Published
2007
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4. Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus

Author

Lu, Zhijian, Raghavan, Subharekha, Bohn, Joann, Charest, Mark, Stahlhut, Mark W., Rutkowski, Carrie A., Simcoe, Amy L., Olsen, David B., Schleif, William A., Carella, Anthony, Gabryelski, Lori, Jin, Lixia, Lin, Jiunn H., Emini, Emilio, Chapman, Kevin, and Tata, James R.

Subjects
*PROTEASE inhibitors, *HIV, *VIROLOGY
Abstract

A series of highly potent HIV protease inhibitors have been designed and synthesized. These compounds are active against various clinical viral isolates as well as wild-type virus. The synthesis and biological activity of these HIV protease inhibitors are discussed. [Copyright &y& Elsevier]

Published
2003
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