2009Zhongguo xin yao zazhiRequires access

Advances in the development of new generation of HIV-1 non-nucleoside reverse transcriptase inhibitors

Xinyong Liu

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Abstract

Currently,more than 50 different structures of non-nucleoside reverse transcriptase inhibitors(NNRTIs) have been found.Among them,nevirapine,delavirdine,efavirenz and etravirine are approved by FDA for the treatment of HIV-1 infection.For the mutations of HIV-1,rapid development of resistance to the drugs is the shortness of first and second generations of NNRTIs.Therefore,a new generation of NNRTIs must retain their potent activity against a wide range of drug resistant strains.In this review,we described the three-dimensional structural models of NNRTIs,and compared and analyzed the molecular structural features of the new generation of NNRTIs,including etravirine,rilpivirine,BILR 355 BS,GW695634,capravirine,triazole and tetrazole thioacetanilide analogues.

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What this paper is about

Currently,more than 50 different structures of non-nucleoside reverse transcriptase inhibitors(NNRTIs) have been found.Among them,nevirapine,delavirdine,efavirenz and etravirine are approved by FDA for the treatment of HIV-1 infection.For the mutations of HIV-1,rapid development of resistance to the drugs is the shortness of first and second generations of NNRTIs.Therefore,a new generation of NNRTIs must retain their potent activity against a wide range of drug resistant strains.In this review,we described the three-dimensional structural models of NNRTIs,and compared and analyzed the molecular structural features of the new generation of NNRTIs,including etravirine,rilpivirine,BILR 355 BS,GW695634,capravirine,triazole and tetrazole thioacetanilide analogues.

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Available abstract

Currently,more than 50 different structures of non-nucleoside reverse transcriptase inhibitors(NNRTIs) have been found.Among them,nevirapine,delavirdine,efavirenz and etravirine are approved by FDA for the treatment of HIV-1 infection.For the mutations of HIV-1,rapid development of resistance to the drugs is the shortness of first and second generations of NNRTIs.Therefore,a new generation of NNRTIs must retain their potent activity against a wide range of drug resistant strains.In this review,we described the three-dimensional structural models of NNRTIs,and compared and analyzed the molecular structural features of the new generation of NNRTIs,including etravirine,rilpivirine,BILR 355 BS,GW695634,capravirine,triazole and tetrazole thioacetanilide analogues.

Key concepts: Etravirine, Nevirapine, Rilpivirine, Efavirenz, Reverse transcriptase, Virology, Human immunodeficiency virus (HIV), Nucleoside Reverse Transcriptase Inhibitor

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