Nucleotide Reverse Transcriptase Inhibitors

نویسنده

  • Martin S. Hirsch
چکیده

4 Optimal HIV-1 suppression often is difficult to achieve and maintain with currently available antiretroviral drugs, and viral resistance eventually emerges to many drugs. Chronic antiretroviral therapy is also associated with complications such as body fat redistribution, hypertriglyceridemia and hypercholesterolemia, abnormal glucose metabolism, lactic acidosis, pancreatitis, avascular necrosis of bone, and osteoporosis. New drugs are needed to enhance anti-HIV potency, overcome viral resistance, increase tolerability and convenience, and reduce toxicity. A number of antiretroviral drugs are in development, including new nucleotide reverse transcriptase inhibitors (ntRTIs), nucleoside reverse transcriptase inhibitors (nRTIs), nonnucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors, fusion and coreceptor inhibitors, and integrase inhibitors. This selective review will summarize some of the more promising compounds under study.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and molecular docking of novel N-((2-chloroquinolin-3-yl) methylene)-4-methylbenzenamine derivatives as anti-HIV-1 reverse transcriptase inhibitors

In this research work, a proficient method has been developed for the preparation of novel N-((2-chloroquinolin-3-yl) methylene)-4-methylbenzenamine derivatives from 2-chloroquinoline-3-carbaldehyde derivatives and p-toluidine in ethanol as solvent and using catalytic amount of acetic acid under reflux conditions to obtain desired products in good yields. The identification of all the synthesiz...

متن کامل

Human Immuno-Deficiency Virus Drug Resistance, Nuclesoide Reverse Transcriptase Inhibitors, Non-nuclesoide Reverse Transcriptase Inhibitors and associated drug resistance mutations in the Reverse Transcriptase Gene of Human Immuno Deficiency Virus-1

Resistance develops due to mutations in the reverse transcriptase gene of HIV-1 genome that does not respond towards the presence of effective drugs. Emergence of HIV-1 variants in the presence of effective drugs is a common occurrence. Drug resistance mutation means “the development of resistance mutations in the drug targeted HIV-1 genes” which causes the viruses to overcome the drug pressure...

متن کامل

Disease Management - Constructing Optimal NRTI-Based Combinations: Past, Present, and Future

Introduction More than a decade ago, it became apparent that treatment of HIV infection with only 1 antiretroviral agent was associated with the rapid development of resistance.[1] Clinical trials conducted at that time showed that combining 2 antiretroviral agents improved virologic and immunologic responses, compared with use of a single agent. Accordingly, 2-drug combination antiretroviral t...

متن کامل

Safety and Toxicity of Individual Antiretroviral Agents in Pregnancy NUCLEOSIDE AND NUCLEOTIDE ANALOGUE REVERSE TRANSCRIPTASE INHIBITORS

There are currently six approved nucleoside analogue reverse transcriptase inhibitors. Data are available from clinical trials in human pregnancy for zidovudine and lamivudine, while didanosine and stavudine are under study. Zalcitabine and abacavir have not been studied in pregnant women. Tenofovir disoproxil fumarate is the first acyclic nucleotide analogue reverse transcriptase inhibitor. Th...

متن کامل

Structural basis for the D-stereoselectivity of human DNA polymerase β

Nucleoside reverse transcriptase inhibitors (NRTIs) with L-stereochemistry have long been an effective treatment for viral infections because of the strong D-stereoselectivity exhibited by human DNA polymerases relative to viral reverse transcriptases. The D-stereoselectivity of DNA polymerases has only recently been explored structurally and all three DNA polymerases studied to date have demon...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:

دوره   شماره 

صفحات  -

تاریخ انتشار 2012