dpc-083 has been researched along with efavirenz* in 3 studies
1 review(s) available for dpc-083 and efavirenz
| Article | Year |
|---|---|
Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.
Acquired immunodeficiency syndrome (AIDS) is a disease caused by human immunodeficiency virus (HIV) that affects individuals on all continents. In 1987, the antiretroviral therapy began increasing survival rates and improving the quality of life for patients. Efavirenz (EFV) is a drug widely used in the treatment of HIV-AIDS since 1998. Belonging to a class of nonnucleoside reverse transcriptase inhibitors (NNRTI), it directly blocks the action of the enzyme and consequently the multiplication of the virus. Although EFV has provided excellent results in reducing viral load, cases of resistance associated with adverse effects have led to the search to find new analogs of this drug. Although many researchers are involved in this quest, curiously there is still no clinical substitute for EFV. To develop a second-generation version of EFV, it is essential understand the structure-activity relationships of the derivative compounds. Thus, the aims of the present review are to compare EFV and its derivatives using medicinal chemistry and to describe the main synthetic routes. Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Chemistry, Pharmaceutical; Cyclopropanes; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Conformation; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2016 |
2 other study(ies) available for dpc-083 and efavirenz
| Article | Year |
|---|---|
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
A series of 4,1-benzoxazepinone analogues of efavirenz (Sustiva) as potent NNRTIs has been discovered. The cis-3-alkylbenzoxazepinones are more potent then the trans isomers and can be synthesized preferentially by a novel stereoselective cyclization. The best compounds are potent orally bioavailable inhibitors of both wild-type HIV-1 and its clinically relevant K103N mutant virus, but are highly protein-bound in human plasma. Topics: Alkynes; Animals; Benzoxazines; Cyclopropanes; HIV Reverse Transcriptase; Humans; Macaca mulatta; Oxazines; Protein Binding; Quinazolines; Quinazolinones; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2001 |
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
A series of 4-alkenyl and 4-alkynyl-3, 4-dihydro-4-(trifluoromethyl)-2-(1H)-quinazolinones were found to be potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) of human immunodeficiency virus type-1 (HIV-1). The 4-alkenyl-3, 4-dihydro-4-(trifluoromethyl)-2-(1H)-quinazolinones DPC 082 and DPC 083 and the 4-alkynyl-3, 4-dihydro-4-(trifluoromethyl)-2-(1H)-quinazolinones DPC 961 and DPC 963 were found to exhibit low nanomolar potency toward wild-type RF virus (IC(90) = 2.0, 2.1, 2.0, and 1.3 nM, respectively) and various single and many multiple amino acid substituted HIV-1 mutant viruses. The increased potency is combined with favorable plasma serum protein binding as demonstrated by improvements in the percent free drug in human plasma when compared to efavirenz: 3.0%, 2.0%, 1.5%, 2. 8%, and 0.2-0.5% for DPC 082, DPC 083, DPC 961, DPC 963, and efavirenz, respectively. Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Blood Proteins; Cyclopropanes; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Structure; Mutation; Oxazines; Protein Binding; Quinazolines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Virus Replication | 2000 |