Design,Synthesis of Novel Substituted Heterothiadiazines and Heterothiatriazines as Potent HIV-1 NNR

来源 :2006中国天津世界艾滋病日科技会议 | 被引量 : 0次 | 上传用户:mechanical123
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  The HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are structurally diverse compounds that act by binding to an allosteric site,approximately 10A from the polymerase active site,causing a distortion of the catalytic aspartate triad.A number of NNRTIs including nevirapine,delavirdine,and efavirenz,are clinically used in combination of chemotherapy for AIDS.However,there are certain factors that restrict the clinical usefulness of these NNRTIs,including drug compatibilities,adverse effects,the emergence of drug-resistant viral strains,and cross resistance.Consequently,discovery and development of novel NNRTIs with new mechanism of action are of paramount importance.
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