Big Chemical Encyclopedia

Chemical substances, components, reactions, process design ...

Articles Figures Tables About

Inhibitors reverse transcriptase

Eriksson M A L, J Pitera and P A Kollman 1999. Prediction of the Binding Free Energies of New TIBO-like HIV-1 Reverse Transcriptase Inhibitors Using a Combination of PROFEC, PB/SA, CMC/MD, and Free Energy Calculations. Journal of Medicinal Chemistry 42 868-881. [Pg.650]

Reverse transcriptase inhibitors are also used against certain viruses which although they are not retroviruses do require re verse transcriptase to repro duce The virus that causes heptatitis B is an example... [Pg.1180]

The most recent advance in treating HIV infections has been to simultaneously attack the virus on a second front using a protease inhibitor. Recall from Section 27.10 that proteases are enzymes that catalyze the hydrolysis of proteins at specific points. When HIV uses a cell s DNA to synthesize its own proteins, the initial product is a long polypeptide that contains several different proteins joined together. To be useful, the individual proteins must be separated from the aggregate by protease-catalyzed hydrolysis of peptide bonds. Protease inhibitors prevent this hydrolysis and, in combination with reverse transcriptase inhibitors, slow the reproduction of HIV. Dramatic reductions in the viral load in HIV-infected patients have been achieved with this approach. [Pg.1180]

In the realm of natural product synthesis, Kepler and Rehder utilized the K-R reaction to synthesize ( )-calanolide A (56), a potent non-nucleosidal human irmnunodeficiency virus (HIV-1) specific reverse transcriptase inhibitor. Propiophenone 57 was allowed to react with acetic anhydride in the presence of sodium acetate to afford benzopyranone 58 in 56% yield subsequent deacetylation of 58 gave 59. Flavone 59 was then transformed to ( ) calanolide A (56) over several steps. [Pg.529]

Heterocycles as nonnucleoside reverse transcriptase inhibitors for therapy of HIV-1 infection 99F26. [Pg.232]

Nucleosides, nucleotides, peptidomimetics, and reverse transcriptase inhibitors in HIV infection therapy 98CCC449. [Pg.235]

FIGURE 7.3 Diversity of structures that interact with the (a) HIV reverse transcriptase inhibitor binding site [8] and (b) the CCR5 receptor mediating HIV-1 fusion [9],... [Pg.129]

So far, five different protease inhibitors have been approved by the FDA for the treatment of HIV infection [3, 4]. Clinical trials in which protease inhibitors were evaluated in monotherapy demonstrated the potency of this class of inhibitors (decrease in HIV RNA levels, increase in CD4 cell counts). Treatment regimens were subsequently broadened to include reverse transcriptase inhibitors in combination with protease inhibitors. The result of these clinical trials has led to a list of guidelines with recommendations for the optimal treatment options. Prolonged control of the infection with combination therapy (highly active antiretroviral therapy, HAART ) could be shown. [Pg.1286]

Nelfinavir is a nonpeptidic, rationally designed HIV protease inhibitor. Nelfinavir has demonstrated efficacy in both monotherapy and in combination with the reverse transcriptase inhibitors stavudine (d4T) or zivudine + 3TC. The major side effect is mild to moderate diarrhea. [Pg.1287]

As with reverse transcriptase inhibitors, resistance to protease inhibitors may also occur. Mutations in the HIV protease gene were shown to confer resistance to each of the aforementioned molecules. In addition, passaging of viius in the presence of HIV protease inhibitors also gave rise to strains less susceptible to the original inhibitor or cross-reactive to other compounds in the same class. New Diug Targets... [Pg.1287]

The mass spectra of primary mono- and diaminoquinoxalines (with or without additional C-methyl groups) have been measured and analyzed. The role of N-pyridinyl-A -(quinoxalinylethyl)thiourea derivatives as HIV-1 (human immunodeficiency 1) reverse transcriptase inhibitors has been discussed in detail. [Pg.269]

The 2, 3 -dideoxynucleoside (ddN) analogues (Fig. 3) encompass a vast group of compounds that have been found active against HIV and HBV, although they have been primarily pursued for the treatment of HIV infections (AIDS). They are targeted at the HIV-associated reverse transcriptase (RT) and therefore also referred to as nucleoside reverse transcriptase inhibitors (NRTIs). They have to be distinguished from the nucleotide reverse transcriptase inhibitors (NtRTIs) such as adefovir (PMEA) and tenofovir (PMPA) (see above) which, like the NRTIs, act as chain... [Pg.72]

Gibson W (1996) Structure and assembly of the virion. Intervirology 39 389 00 Goldman ME, Nunberg JH, O Brien JA, Quintero JC, Schleif WA, Freund KF, Gaul SL, Saari WS, Wai IS, Hoffman JM et al. (1991) Pyridinone derivatives specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity. Proc Natl Acad Sci USA... [Pg.172]

Herandez J, Amador L, Amantea M, Chao H, Hawley P, Paradise L (2000) Short-course monotherapy with AG1549, a novel non-nucleoside reverse transcriptase inhibitor (NNRTI), in antiretroviral naive patients. In 7th conference on retroviruses and opportunistic infections. San Francisco, CA, Abstract 669... [Pg.173]

Lalezari JP, DeJesus E, Northfelt DW, Richmond G, Wolfe P, Haubrich R, Henry D, Powderly W, Becker S, Thompson M, Valentine E, Wright D, Carlson M, Riddler S, Haas FF, DeMasi R, Sista PR, Salgo M, Delehanty J (2003a) A controlled Phase II trial assessing three doses of enfuvirtide (T-20) in combination with abacavir, amprenavir, ritonavir and efavirenz in nonnucleoside reverse transcriptase inhibitor-naive HIV-infected adults. Antivir Ther 8 279-287... [Pg.197]

A general mechanism of resistance is reducing the affinity of the antiretroviral compound for its mutant target protein. Resistance mutations associated with reduced affinity are observed during treatment failure with a fusion inhibitor, nonnucleoside reverse transcriptase inhibitors (NNRTl), integrase inhibitor, and protease inhibitors as reviewed in Chaps. 3,4, 6, and 7 (Hazuda et al. 2007 Hsiou et al. 2001 King et al. 2002 Mink et al. 2005). [Pg.302]


See other pages where Inhibitors reverse transcriptase is mentioned: [Pg.1180]    [Pg.524]    [Pg.57]    [Pg.54]    [Pg.296]    [Pg.1284]    [Pg.1285]    [Pg.1286]    [Pg.212]    [Pg.348]    [Pg.584]    [Pg.1421]    [Pg.252]    [Pg.54]    [Pg.54]    [Pg.54]    [Pg.73]    [Pg.82]    [Pg.91]    [Pg.91]    [Pg.156]    [Pg.156]    [Pg.170]    [Pg.170]    [Pg.171]    [Pg.174]    [Pg.174]    [Pg.174]    [Pg.175]    [Pg.187]    [Pg.291]    [Pg.305]   
See also in sourсe #XX -- [ Pg.529 ]

See also in sourсe #XX -- [ Pg.414 , Pg.457 ]

See also in sourсe #XX -- [ Pg.121 , Pg.219 ]

See also in sourсe #XX -- [ Pg.33 ]

See also in sourсe #XX -- [ Pg.533 ]




SEARCH



Abacavir Nucleoside reverse transcriptase inhibitors (

Adefovir Nucleoside reverse transcriptase inhibitors (

Antiviral agents reverse transcriptase inhibitors

Antiviral drugs nucleoside reverse transcriptase inhibitors

Didanosine Nucleoside reverse transcriptase inhibitors (

Efavirenz reverse transcriptase inhibitors

Emtricitabine Nucleoside reverse transcriptase inhibitors

Ganciclovir Nucleoside reverse transcriptase inhibitors (

HIV-1 nucleoside reverse transcriptase inhibitors

HIV-1 reverse transcriptase inhibitors

Hormonal) Non-nucleoside reverse transcriptase inhibitors

Human immunodeficiency virus reverse transcriptase inhibitors

Indinavir Nucleoside reverse transcriptase inhibitors (

Lamivudine Nucleoside reverse transcriptase inhibitors (

Look up the names of both individual drugs and their drug groups to access full information Non-nucleoside reverse transcriptase inhibitors

Lopinavir Nucleoside reverse transcriptase inhibitors (

Methadone Nucleoside reverse transcriptase inhibitors (

NNRTI interactions Nucleoside reverse transcriptase inhibitors (

NSAIDs) Nucleoside reverse transcriptase inhibitors (

Nevirapine reverse transcriptase inhibitors

Non-nucleoside reverse transcriptase inhibitors

Non-nucleoside reverse transcriptase inhibitors NNRTIs)

Nonnucleoside inhibitor of HIV-1 reverse transcriptase

Nonnucleoside reverse transcriptase inhibitors

Nonnucleoside reverse transcriptase inhibitors NNRTIs)

Nonnucleoside reverse transcriptase with protease inhibitors

Nucleoside analog reverse transcriptase inhibitors

Nucleoside analogue reverse transcriptase inhibitors

Nucleoside and nucleotide reverse transcriptase inhibitors

Nucleoside reverse transcriptase inhibitor Numbering

Nucleoside reverse transcriptase inhibitors

Nucleoside reverse transcriptase inhibitors NRTIs)

Nucleoside reverse transcriptase inhibitors preparations

Nucleoside reverse-transcriptase inhibitors side effects

Nucleoside/nucleotide reverse transcriptase inhibitors

Nucleotide reverse transcriptase inhibitor

Nucleotide reverse transcriptase inhibitor NRTI)

Nucleotide reverse transcriptase inhibitors NTRTIs)

REVERSION INHIBITOR

Reverse inhibitor

Reverse transcriptase inhibitors RTIs)

Reverse transcriptase inhibitors abacavir

Reverse transcriptase inhibitors analogues

Reverse transcriptase inhibitors delavirdine

Reverse transcriptase inhibitors didanosine

Reverse transcriptase inhibitors emtricitabine

Reverse transcriptase inhibitors hepatitis

Reverse transcriptase inhibitors in HIV infection

Reverse transcriptase inhibitors lamivudine

Reverse transcriptase inhibitors side effects

Reverse transcriptase inhibitors stavudine

Reverse transcriptase inhibitors tenofovir

Reverse transcriptase inhibitors zalcitabine

Reverse transcriptase inhibitors zidovudine

Reverse transcriptase inhibitors, nevirapine, efavirenz, and delavirdine

Reverse transcriptase other inhibitors

Reversible inhibitors

Ribavirin Nucleoside reverse transcriptase inhibitors (

Stavudine Nucleoside reverse transcriptase inhibitors

Tipranavir Nucleoside reverse transcriptase inhibitors (

Transcriptase

Zalcitabine Nucleoside reverse transcriptase inhibitors (

© 2024 chempedia.info