Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors
A novel series of quinolones was discovered as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) using a structure-based approach. The lead quinolones exhibited single digit nanomolar potency in the HIV-1 replication assays. The preliminary SAR of these quinolones was also established v...
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| Published in | Bioorganic & medicinal chemistry letters Vol. 16; no. 16; pp. 4246 - 4251 |
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| Main Authors | , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
Oxford
Elsevier Ltd
15.08.2006
Elsevier |
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| Online Access | Get full text |
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| Abstract | A novel series of quinolones was discovered as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) using a structure-based approach. The lead quinolones exhibited single digit nanomolar potency in the HIV-1 replication assays. The preliminary SAR of these quinolones was also established via systematic structural modifications. These novel and potent quinolones could serve as advanced leads for further optimization. |
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| AbstractList | A novel series of quinolones was discovered as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) using a structure-based approach. The lead quinolones exhibited single digit nanomolar potency in the HIV-1 replication assays. The preliminary SAR of these quinolones was also established via systematic structural modifications. These novel and potent quinolones could serve as advanced leads for further optimization. |
| Author | Wu, Baogen Wolff, Karen Bursulaya, Badry He, Yun Ellis, David Anaclerio, Beth Yin, Hong Kuhen, Kelli L. Caldwell, Jeremy Karanewsky, Donald |
| Author_xml | – sequence: 1 givenname: David surname: Ellis fullname: Ellis, David – sequence: 2 givenname: Kelli L. surname: Kuhen fullname: Kuhen, Kelli L. – sequence: 3 givenname: Beth surname: Anaclerio fullname: Anaclerio, Beth – sequence: 4 givenname: Baogen surname: Wu fullname: Wu, Baogen – sequence: 5 givenname: Karen surname: Wolff fullname: Wolff, Karen – sequence: 6 givenname: Hong surname: Yin fullname: Yin, Hong – sequence: 7 givenname: Badry surname: Bursulaya fullname: Bursulaya, Badry – sequence: 8 givenname: Jeremy surname: Caldwell fullname: Caldwell, Jeremy – sequence: 9 givenname: Donald surname: Karanewsky fullname: Karanewsky, Donald – sequence: 10 givenname: Yun surname: He fullname: He, Yun email: yhe@gnf.org |
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| Keywords | HIV replication Molecule modeling HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) SAR Quinolones RNA-directed DNA polymerase HIV-1 virus Non nucleoside compound Modeling Optimization Structure activity relation Reverse transcriptase inhibitor Antiviral Chemical synthesis Quinolone derivatives Enzyme Transferases Retroviridae Enzyme inhibitor Quinoline derivatives Lentivirus Virus Nucleotidyltransferases Replication Human immunodeficiency virus |
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| SubjectTerms | Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Binding Sites Biological and medical sciences Drug Resistance, Viral HIV replication HIV Reverse Transcriptase - antagonists & inhibitors HIV-1 - metabolism HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) Medical sciences Models, Chemical Models, Molecular Molecule modeling Mutation Pharmacology. Drug treatments Quinolones Quinolones - chemistry Reverse Transcriptase Inhibitors - pharmacology SAR Structure-Activity Relationship Virus Replication |
| Title | Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors |
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