SrasV1, Main, Exploration, bibRecord, 001338

Design, Synthesis, and Biological Evaluation of Novel 4-Aminopiperidinyl-linked 3,5-Disubstituted-1,2,6-thiadiazine-1,1-dione Derivatives as HIV-1 NNRTIs.

Identifieur interne : 001338 ( Main/Exploration ); précédent : 001337; suivant : 001339

Design, Synthesis, and Biological Evaluation of Novel 4-Aminopiperidinyl-linked 3,5-Disubstituted-1,2,6-thiadiazine-1,1-dione Derivatives as HIV-1 NNRTIs.

Auteurs : Tao Liu [République populaire de Chine] ; Boshi Huang [République populaire de Chine] ; Ye Tian [République populaire de Chine] ; Xin Liang [République populaire de Chine] ; Hong Liu [République populaire de Chine] ; Huiqing Liu [République populaire de Chine] ; Peng Zhan [République populaire de Chine] ; Erik De Clercq [Belgique] ; Christophe Pannecouque [Belgique] ; Xinyong Liu [République populaire de Chine]

Source :

Chemical biology & drug design [ 1747-0285 ] ; 2015.

RBID : pubmed:25359703

Descripteurs français

KwdFr :
- Agents antiVIH (), Agents antiVIH (pharmacologie), Agents antiVIH (synthèse chimique), Conception de médicament, Humains, Infections à VIH (anatomopathologie), Infections à VIH (métabolisme), Infections à VIH (traitement médicamenteux), Lignée cellulaire, Relation structure-activité, VIH-1 (Virus de l'Immunodéficience Humaine de type 1) (métabolisme).
MESH :
- anatomopathologie : Infections à VIH.
- métabolisme : Infections à VIH, VIH-1 (Virus de l'Immunodéficience Humaine de type 1).
- pharmacologie : Agents antiVIH.
- synthèse chimique : Agents antiVIH.
- traitement médicamenteux : Infections à VIH.
- Agents antiVIH, Conception de médicament, Humains, Lignée cellulaire, Relation structure-activité.

English descriptors

KwdEn :
- Anti-HIV Agents (chemical synthesis), Anti-HIV Agents (chemistry), Anti-HIV Agents (pharmacology), Cell Line, Drug Design, HIV Infections (drug therapy), HIV Infections (metabolism), HIV Infections (pathology), HIV-1 (metabolism), Humans, Structure-Activity Relationship.
MESH :
- chemical , chemical synthesis : Anti-HIV Agents.
- chemical , chemistry : Anti-HIV Agents.
- chemical , pharmacology : Anti-HIV Agents.
- drug therapy : HIV Infections.
- metabolism : HIV Infections, HIV-1.
- pathology : HIV Infections.
- Cell Line, Drug Design, Humans, Structure-Activity Relationship.

Abstract

Based on the hybridization of the privileged fragments in DABO and DAPY-typed HIV-1 NNRTIs, a novel series of 4-aminopiperidinyl-linked 3,5-disubstituted-1,2,6-thiadiazine-1,1-dione derivatives were designed, synthesized, and evaluated for their in vitro anti-HIV activities in MT-4 cells. Most of the target compounds showed weak inhibitory activity against WT HIV-1. In order to confirm the mode of action of the target compounds, representative compounds Ba8 and Bb8 were selected to perform the HIV-1 RT inhibitory assay. In this assay, Ba8 and Bb8 displayed good activity with IC50 values of 3.15 and 1.52 μm, respectively. Additionally, preliminary structure-activity relationships (SARs) analysis and molecular docking studies of newly synthesized compounds are also discussed.

DOI: 10.1111/cbdd.12468
PubMed: 25359703

Affiliations:

Belgique, République populaire de Chine

Le document en format XML

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<term>HIV Infections (drug therapy)</term>
<term>HIV Infections (metabolism)</term>
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<front><div type="abstract" xml:lang="en">Based on the hybridization of the privileged fragments in DABO and DAPY-typed HIV-1 NNRTIs, a novel series of 4-aminopiperidinyl-linked 3,5-disubstituted-1,2,6-thiadiazine-1,1-dione derivatives were designed, synthesized, and evaluated for their in vitro anti-HIV activities in MT-4 cells. Most of the target compounds showed weak inhibitory activity against WT HIV-1. In order to confirm the mode of action of the target compounds, representative compounds Ba8 and Bb8 were selected to perform the HIV-1 RT inhibitory assay. In this assay, Ba8 and Bb8 displayed good activity with IC50 values of 3.15 and 1.52 μm, respectively. Additionally, preliminary structure-activity relationships (SARs) analysis and molecular docking studies of newly synthesized compounds are also discussed. </div>
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<name sortKey="Liu, Hong" sort="Liu, Hong" uniqKey="Liu H" first="Hong" last="Liu">Hong Liu</name>
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<name sortKey="Liu, Xinyong" sort="Liu, Xinyong" uniqKey="Liu X" first="Xinyong" last="Liu">Xinyong Liu</name>
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       | HfdSelect -Kh $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd   \
       | NlmPubMed2Wicri -a SrasV1

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Serveur d'exploration SRAS

Design, Synthesis, and Biological Evaluation of Novel 4-Aminopiperidinyl-linked 3,5-Disubstituted-1,2,6-thiadiazine-1,1-dione Derivatives as HIV-1 NNRTIs.

Design, Synthesis, and Biological Evaluation of Novel 4-Aminopiperidinyl-linked 3,5-Disubstituted-1,2,6-thiadiazine-1,1-dione Derivatives as HIV-1 NNRTIs.

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	Serveur d'exploration SRAS
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