| Progress of bis(heteroaryl)piperazines (BHAPs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) against human immunodeficiency virus type 1 (HIV-1). | |
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MedLine Citation:
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PMID: 20380641 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Since the first case of acquired immunodeficiency syndrome (AIDS) was reported in 1981, AIDS, as the global disease affecting 33.2 million people in 2007, has always been an unsolved problem worldwide. Reverse transcriptase (RT) is a crucial enzyme in the life cycle of human immunodeficiency virus type 1 (HIV-1), and thereby has been the prime drugs target for antiretroviral (ARV) therapy against AIDS. To date, two classes of RT inhibitors (RTIs), e.g., nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs), and a lot of compounds tested as RTIs have been described. To our knowledge, bis(heteroaryl)piperazines (BHAPs) have been considered as one class of promising NNRTIs, such as structurally and chemically related NNRTI delavirdine, which was approved by the U. S. Food and Drug Administration (FDA) for the treatment of HIV-1 infection in 1997. In this mini-review, we make attempts to report the progress of synthesis and structure-activity relationship (SAR) of BHAPs, in the meantime, the synergistic inhibition of HIV-1 replication by combining delavirdine with other HIV-1 inhibitors is also discussed. It will pave the way for the design and development of BHAPs as anti-HIV-1 agents in AIDS chemotherapy in the future. |
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Authors:
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Hui Xu |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't; Review |
Journal Detail:
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Title: Mini reviews in medicinal chemistry Volume: 10 ISSN: 1875-5607 ISO Abbreviation: Mini Rev Med Chem Publication Date: 2010 Jan |
Date Detail:
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Created Date: 2010-04-12 Completed Date: 2010-07-12 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101094212 Medline TA: Mini Rev Med Chem Country: Netherlands |
Other Details:
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Languages: eng Pagination: 62-72 Citation Subset: IM |
Affiliation:
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Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling, P. R. China. orgxuhui@nwsuaf.edu.cn |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Anti-HIV Agents
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chemical synthesis,
chemistry*,
pharmacology*,
therapeutic use Delavirdine / pharmacology, therapeutic use Drug Design Drug Synergism Drug Therapy, Combination HIV Infections / drug therapy HIV Reverse Transcriptase / antagonists & inhibitors HIV-1 / drug effects* Humans Piperazines / chemical synthesis, chemistry*, pharmacology*, therapeutic use Reverse Transcriptase Inhibitors / chemical synthesis, chemistry*, pharmacology*, therapeutic use Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Anti-HIV Agents; 0/Piperazines; 0/Reverse Transcriptase Inhibitors; 136817-59-9/Delavirdine; EC 2.7.7.49/HIV Reverse Transcriptase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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