Results 251 to 260 of about 58,529 (279)

HIV-1 protease inhibitors in development

Expert Opinion on Investigational Drugs, 2002
Several pharmaceutical companies have developed an increasing number of second generation protease inhibitors (PI) during the last few years. Many of these compounds have been in preclinical trials and some are now in clinical use. All drugs in this category have been designed to be well absorbed and overcome the crucial problem of cross-resistance ...
S. Rusconi, S. La Seta Catamancio
openaire   +3 more sources

Development of HIV protease inhibitors: A survey

1998
In the treatment of infections caused by rapidly mutating viruses like human immunodeficiency virus (HIV), combination therapy with multiple drugs acting by different mechanisms offers several advantages over monotherapy. It may provide: synergistic effect, possible reduction of dosages and side-effects, and reduction of the chance of drug resistance ...
Eric J. Lien, Shijun Ren
openaire   +3 more sources

Oximinoarylsulfonamides as potent HIV protease inhibitors

Bioorganic & Medicinal Chemistry Letters, 2005
The need for a potent HIV protease inhibitor (PI) to combat emerging PI-resistant viruses is anticipated. Analogs formulated from the combination of structural fragments of Ritonavir, Lopinavir, and Amprenavir were synthesized. Analogs containing the oxime pharmacophore were found to have improved activities against both wild type and resistant (A17 ...
Chen Zhao, John T. Randolph, Minghua Sun, Charles A. Flentge, Dale J. Kempf, Larry L. Klein, Clinton M. Yeung, Vincent S. Stoll, Tatyana Dekhtyar   +8 more
openaire   +3 more sources

HIV Protease Inhibitor Resistance

2014
HIV protease is pivotal in the viral replication cycle and directs the formation of mature infectious virus particles. The development of highly specific HIV protease inhibitors (PIs), based on thorough understanding of the structure of HIV protease and its substrate, serves as a prime example of structure-based drug design.
M. Nijhuis, Annemarie M. J. Wensing, Axel Fun   +2 more
openaire   +2 more sources

The pharmacokinetics of HIV protease inhibitor combinations

Current Opinion in Infectious Diseases, 2005
The clinical use of double-boosted protease inhibitor regimens has evolved recently. This strategy offers a number of unique benefits, including pharmacokinetic enhancement of two different protease inhibitors with low dose ritonavir. We review the pharmacologic rationale for the double-boosted protease inhibitor combinations and the complex drug-drug ...
Desmond Maitland, Marta Boffito, Yohan Samarasinghe, Anton Pozniak   +3 more
openaire   +3 more sources

Perspectives in HIV Protease Inhibitors

1996
The therapy of HIV-1, the causative agent of AIDS, is limited today to a small number of different drugs, all of which are nucleoside analogues. Nucleoside analogues active against HIV are all inhibitors of reverse transcriptase (RT) and target primarily early events in the replication cycle of HIV.
openaire   +3 more sources

Enamino-oxindole HIV protease inhibitors

Bioorganic & Medicinal Chemistry Letters, 2012
We have designed and synthesized a series of HIV protease inhibitors (PIs) with enamino-oxindole substituents optimized to interact with the S2' subsite of the HIV protease binding pocket. Several of these inhibitors have sub-nanomolar K(i) and antiviral IC(50) in the low nM range against WT HIV and against a panel of multi-drug resistant (MDR) strains.
Sergei V. Gulnik, Tanya Guerassina, Douglas Ludtke, Abelardo Silva, Betty Yu, Elena Afonina, John W. Erickson, Michael Eissenstat, Hiroko Yokoe   +8 more
openaire   +3 more sources

HIV Protease Inhibitors: Present and Future

Future Virology, 2011
Antiretroviral therapy offers many options, largely based on the next-generation protease inhibitors (PIs). Early PI-based treatments involve high pill burdens and dosing schedules, and concerns of long-term toxicities are well established. In patients who have already achieved viral suppression, novel agents and strategies should be used to simplify ...
Pizzocolo Cecilia, Castagna A, Lazzarin Adriano   +2 more
openaire   +2 more sources

The synthesis of novel HIV-protease inhibitors

Bioorganic & Medicinal Chemistry, 1994
The syntheses, enzyme inhibition and antiviral activity of potent HIV-protease inhibitors containing novel beta-hydroxy ether and thioethers based on the transition state mimetic concept are discussed.
Viyyoor M. Girijavallabhan, Andrea Hart, Bimalendu Dasmahapatra, Ashit K. Ganguly, Naginbhai M. Patel, Nancy Butkiewicz, Frank Bennett   +6 more
openaire   +3 more sources

Dyslipidemia in the era of HIV protease inhibitors

Progress in Cardiovascular Diseases, 2003
Human immunodeficiency virus protease inhibitors are associated with metabolic abnormalities that may increase risk of atherosclerotic vascular disease, including dyslipidemia, insulin resistance, and central obesity. Dyslipidemia, characterized by hypercholesterolemia and hypertriglyceridemia, small low- and high-density lipoprotein particles, and in ...
openaire   +2 more sources