Synthesis, Biological Activity, and ADME Properties of Novel S-DABOs/N-DABOs as HIV Reverse Transcriptase Inhibitors (Q60197481)

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26 January 2020

title

Synthesis, biological activity, and ADME properties of novel S-DABOs/N-DABOs as HIV reverse transcriptase inhibitors (English)

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1

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José A. Esté

13

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Bonaventura Clotet Sala

12

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Bonaventura Clotet

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Giovanni Maga

9

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ORCID Public Data File 2021

Maurizio Botta

14

object named as

Maurizio Botta

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8

Elena Dreassi

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author name string

Mafalda Pagano

2

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Luigi Franchi

3

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Daniele Castagnolo

4

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Silvia Schenone

5

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Gianni Casaluce

6

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Claudio Zamperini

7

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Alberta Samuele

10

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Encarna Gonzalo

11

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publication date

14 March 2012

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volume

7

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issue

5

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page(s)

883-896

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Nonnucleoside reverse transcriptase inhibitor resistance and the role of the second-generation agents

26 January 2020

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Slow binding-tight binding interaction between benzimidazol-2-one inhibitors and HIV-1 reverse transcriptase containing the lysine 103 to asparagine mutation

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Non-nucleoside HIV-1 reverse transcriptase inhibitors di-halo-indolyl aryl sulfones achieve tight binding to drug-resistant mutants by targeting the enzyme-substrate complex

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Novel broad-spectrum thiourea non-nucleoside inhibitors for the prevention of mucosal HIV transmission

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Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor

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In vitro microbicidal activity of the nonnucleoside reverse transcriptase inhibitor (NNRTI) UC781 against NNRTI-resistant human immunodeficiency virus type 1

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Recent advances in the DABOs family as potent HIV-1 non-nucleoside reverse transcriptase inhibitors

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Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants

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5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile

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Recent highlights in the synthesis of highly functionalized pyrimidines

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Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity

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7 January 2021

Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase

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Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.

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A multidisciplinary approach for the identification of novel HIV-1 non-nucleoside reverse transcriptase inhibitors: S-DABOCs and DAVPs

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A general, Brønsted acid-catalyzed hetero-Michael addition of nitrogen, oxygen, and sulfur nucleophiles

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An Improved One-pot Procedure for the Synthesis of Alkynes from Aldehydes

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Compensatory mutations rescue the virus replicative capacity of VIRIP-resistant HIV-1.

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Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes

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7 January 2021

Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study.

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7 January 2021

Identifiers

DOI

10.1002/CMDC.201200056

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26 January 2020

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