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Design, Synthesis, Antiviral Activity, and SARs of 14-Aminophenanthroindolizidines

Identifieur interne : 001F88 ( Main/Exploration ); précédent : 001F87; suivant : 001F89

Design, Synthesis, Antiviral Activity, and SARs of 14-Aminophenanthroindolizidines

Auteurs : ZIWEN WANG [République populaire de Chine] ; LEI WANG [République populaire de Chine] ; SHUANG MA [République populaire de Chine] ; YUXIU LIU [République populaire de Chine] ; LIZHONG WANG [République populaire de Chine] ; QINGMIN WANG [République populaire de Chine]

Source :

RBID : Pascal:12-0267991

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English descriptors

Abstract

Based on our previous structure-activity relationship and antiviral mechanism studies, a series of 14-aminophenanthroindolizidines (1a-i, 2, and 3) were designed, targeting tobacco mosaic virus (TMV) RNA, and synthesized and systematically evaluated for their antiviral activity against TMV. The bioassay results showed that most of these compounds exhibited good to excellent in vivo anti-TMV activity, ofwhich compounds 1d and 1h displayed significantly higher activity than commercial ningnanmycin, and thus emerged as potential inhibitors of plant virus. The introduction of amino groups at the 14-position of phenanthroindolizidines, which is proposed to interact with arginine residues around the TMV RNA, increased anti-TMV activity.


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Le document en format XML

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<div type="abstract" xml:lang="en">Based on our previous structure-activity relationship and antiviral mechanism studies, a series of 14-aminophenanthroindolizidines (1a-i, 2, and 3) were designed, targeting tobacco mosaic virus (TMV) RNA, and synthesized and systematically evaluated for their antiviral activity against TMV. The bioassay results showed that most of these compounds exhibited good to excellent in vivo anti-TMV activity, ofwhich compounds 1d and 1h displayed significantly higher activity than commercial ningnanmycin, and thus emerged as potential inhibitors of plant virus. The introduction of amino groups at the 14-position of phenanthroindolizidines, which is proposed to interact with arginine residues around the TMV RNA, increased anti-TMV activity.</div>
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