2006Fine Chemical IntermediatesRequires access

Recent Developments of Non-nucleoside Reverse Transcriptase Inhibitors

Yuxin Li

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Abstract

Upon the chemotherapy of HIV,the use of reverse transcriptase(RT)inhibitors is essential.RT inhibitors are divided into two main classes:nucleoside reverse transcriptase inhibitors(NRTIs),such as zidovudine(AZT),and non-nucleoside reverse transcriptase inhibitors(NNRTIs),such as nevirapine(Viramune).More than 30 different classes of NNRTIs have been developed,among them nevirapine,delavirdine and efavirenz are commercialized as anti-HIV drugs.Some compounds,which are currently in clinical trials,show potent anti-HIV activities.Such compounds include MKC-442,trovirdine,loviride.Thefirst generationNNRTIs are suffering from drug resistance,whereas thesecond generationNNRTIs shows an improved activity spectrum against the most common NNRTI-resistant HIV variants.Compounds belonging to thesecond generationNNRTIs include DPC083,capravirine,etravirine,rilpivirine etc.Rilpivirine is up to now the most effective compound against HIV.

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What this paper is about

Upon the chemotherapy of HIV,the use of reverse transcriptase(RT)inhibitors is essential.RT inhibitors are divided into two main classes:nucleoside reverse transcriptase inhibitors(NRTIs),such as zidovudine(AZT),and non-nucleoside reverse transcriptase inhibitors(NNRTIs),such as nevirapine(Viramune).More than 30 different classes of NNRTIs have been developed,among them nevirapine,delavirdine and efavirenz are commercialized as anti-HIV drugs.Some compounds,which are currently in clinical trials,show potent anti-HIV activities.Such compounds include MKC-442,trovirdine,loviride.Thefirst generationNNRTIs are suffering from drug resistance,whereas thesecond generationNNRTIs shows an improved activity spectrum against the most common NNRTI-resistant HIV variants.Compounds belonging to thesecond generationNNRTIs include DPC083,capravirine,etravirine,rilpivirine etc.Rilpivirine is up to now the most effective compound against HIV.

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Available abstract

Upon the chemotherapy of HIV,the use of reverse transcriptase(RT)inhibitors is essential.RT inhibitors are divided into two main classes:nucleoside reverse transcriptase inhibitors(NRTIs),such as zidovudine(AZT),and non-nucleoside reverse transcriptase inhibitors(NNRTIs),such as nevirapine(Viramune).More than 30 different classes of NNRTIs have been developed,among them nevirapine,delavirdine and efavirenz are commercialized as anti-HIV drugs.Some compounds,which are currently in clinical trials,show potent anti-HIV activities.Such compounds include MKC-442,trovirdine,loviride.Thefirst generationNNRTIs are suffering from drug resistance,whereas thesecond generationNNRTIs shows an improved activity spectrum against the most common NNRTI-resistant HIV variants.Compounds belonging to thesecond generationNNRTIs include DPC083,capravirine,etravirine,rilpivirine etc.Rilpivirine is up to now the most effective compound against HIV.

Key concepts: Nevirapine, Rilpivirine, Efavirenz, Etravirine, Reverse transcriptase, Chemistry, Zidovudine, Nucleoside Reverse Transcriptase Inhibitor

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