Recent advances on dual inhibitors targeting HIV reverse transcriptase associated polymerase and ribonuclease H

Synthesis of Polyoxygenated Tropolones and their Antiviral Activity against Hepatitis B Virus and Herpes Simplex Virus‐1

(2022) Daniel V. Schiavone et al.   CHEMISTRY-A EUROPEAN JOURNAL

Insights into HIV-1 Reverse Transcriptase (RT) Inhibition and Drug Resistance from Thirty Years of Structural Studies

(2022) Abhimanyu K. Singh et al.   Viruses-Basel

Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase

(2021) Antonella Messore et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploring New Scaffolds for the Dual Inhibition of HIV-1 RT Polymerase and Ribonuclease Associated Functions

(2021) Rita Meleddu et al.   MOLECULES

Identification of Novel HBV/HDV Entry Inhibitors by Pharmacophore- and QSAR-Guided Virtual Screening

(2021) Michael Kirstgen et al.   Viruses-Basel

Pyrroles as Privileged Scaffolds in the Search for New Potential HIV Inhibitors

(2021) Maria da Conceição Avelino Dias Bianco et al.   Pharmaceuticals

Long-acting cabotegravir and rilpivirine for HIV-1 suppression: switch to 2-monthly dosing after 5 years of daily oral therapy

(2021) Anthony Mills et al.   AIDS

Synthesis and Evaluation of Gallotannin Derivatives as Antioxidants and α-Glucosidase Inhibitors

(2021) Shota Machida et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Short‐course daily isoniazid and rifapentine for latent tuberculosis infection in people living with HIV who received coformulated bictegravir/emtricitabine/tenofovir alafenamide

(2021) Bo‐Huang Liou et al.   Journal of the International AIDS Society

Design of Biphenyl-Substituted Diarylpyrimidines with a Cyanomethyl Linker as HIV-1 NNRTIs via a Molecular Hybridization Strategy

(2020) Yuan Lei et al.   MOLECULES

1,2,4-Triazolo[1,5-a]pyrimidines as a Novel Class of Inhibitors of the HIV-1 Reverse Transcriptase-Associated Ribonuclease H Activity

(2020) Jenny Desantis et al.   MOLECULES

Pyrrolyl Pyrazoles as Non-Diketo Acid Inhibitors of the HIV-1 Ribonuclease H Function of Reverse Transcriptase.

(2020) Antonella Messore et al.   ACS Medicinal Chemistry Letters

Amide-containing α-hydroxytropolones as inhibitors of hepatitis B virus replication

(2020) Qilan Li et al.   ANTIVIRAL RESEARCH

Evolving understanding of HIV-1 reverse transcriptase structure, function, inhibition, and resistance

(2020) Francesc Xavier RUIZ et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

2-(Arylamino)-6-(trifluoromethyl)nicotinic Acid Derivatives: New HIV-1 RT Dual Inhibitors Active on Viral Replication

(2020) Angela Corona et al.   MOLECULES

Discovery of novel aminopiperidinyl amide CXCR4 modulators through virtual screening and rational drug design

(2020) Yoon Hyeun Oum et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and characterization of 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide-based compounds targeting the PA-PB1 interface of influenza A virus polymerase

(2020) Serena Massari et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Large Multidomain Protein NMR: HIV-1 Reverse Transcriptase Precursor in Solution

(2020) Tatiana V. Ilina et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker

(2019) Jing Tang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Pyrimidine 2,4-Diones in the Design of New HIV RT Inhibitors

(2019) Romeo et al.   MOLECULES

Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): Our past twenty years

(2019) Chunlin Zhuang et al.   Acta Pharmaceutica Sinica B

Dolutegravir/Lamivudine Single-Tablet Regimen: A Review in HIV-1 Infection

(2019) Lesley J. Scott   DRUGS

Dual inhibitor design for HIV-1 reverse transcriptase and integrase enzymes: a molecular docking study

(2019) Selami Ercan et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H

(2018) Lei Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity

(2018) Lei Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological assessment of 3,7-dihydroxytropolones

(2018) D. R. Hirsch et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Prediction of the binding mode and resistance profile for a dual-target pyrrolyl diketo acid scaffold against HIV-1 integrase and reverse-transcriptase-associated ribonuclease H

(2018) Fengyuan Yang et al.   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Design, Synthesis and Biological Evaluation of Novel Galloyl Derivatives as HIV-1 RNase H Inhibitors

(2018) Ping Gao et al.   Chemical Biology & Drug Design

From cycloheptathiophene-3-carboxamide to oxazinone-based derivatives as allosteric HIV-1 ribonuclease H inhibitors

(2018) Serena Massari et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Identification of a novel DGKα inhibitor for XLP-1 therapy by virtual screening

(2018) Suresh Velnati et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Natural product-inspired esters and amides of ferulic and caffeic acid as dual inhibitors of HIV-1 reverse transcriptase

(2017) Vijay P. Sonar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

6-Cyclohexylmethyl-3-hydroxypyrimidine-2,4-dione as an inhibitor scaffold of HIV reverase transcriptase: Impacts of the 3-OH on inhibiting RNase H and polymerase

(2017) Jing Tang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, biological evaluation and molecular modeling of 2-Hydroxyisoquinoline-1,3-dione analogues as inhibitors of HIV reverse transcriptase associated ribonuclease H and polymerase

(2017) Jing Tang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Double-Winged 3-Hydroxypyrimidine-2,4-diones: Potent and Selective Inhibition against HIV-1 RNase H with Significant Antiviral Activity

(2017) Sanjeev Kumar V. Vernekar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and antiviral evaluation of novel heteroarylcarbothioamide derivatives as dual inhibitors of HIV-1 reverse transcriptase-associated RNase H and RDDP functions

(2017) Angela Corona et al.   Pathogens and Disease

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H

(2016) Angela Corona et al.   ANTIVIRAL RESEARCH

Advances in rationally designed dual inhibitors of HIV-1 reverse transcriptase and integrase

(2016) Shuang-Xi Gu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Fragment-Based Discovery of 5-Arylisatin-Based Inhibitors of Matrix Metalloproteinases 2 and 13

(2016) Mariangela Agamennone et al.   ChemMedChem

Studies on Cycloheptathiophene-3-carboxamide Derivatives as Allosteric HIV-1 Ribonuclease H Inhibitors

(2016) Angela Corona et al.   ChemMedChem

A Recent Perspective on Discovery and Development of Diverse Therapeutic Agents Inspired from Isatin Alkaloids

(2016) Rajesh A. Rane et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

HIV-1 Reverse Transcriptase Polymerase and RNase H (Ribonuclease H) Active Sites Work Simultaneously and Independently

(2016) An Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase

(2016) Rita Meleddu et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Inhibitory effects of isatin Mannich bases on carbonic anhydrases, acetylcholinesterase, and butyrylcholinesterase

(2016) Dilan Ozmen Ozgun et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluations of Hydroxypyridonecarboxylic Acids as Inhibitors of HIV Reverse Transcriptase Associated RNase H

(2016) Jayakanth Kankanala et al.   JOURNAL OF MEDICINAL CHEMISTRY

3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H

(2016) Bulan Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical Evaluations

(2016) Jing Tang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Development of a Three-Component Oxidopyrylium [5 + 2] Cycloaddition

(2016) Michael P. D’Erasmo et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis, Neuro-protection and Anti-cancer Activities of Simple Isatin Mannich and Schiff Bases

(2016) Gang Chen et al.   Letters in Drug Design & Discovery

Design, synthesis, biological evaluation and docking studies of sulfonyl isatin derivatives as monoamine oxidase and caspase-3 inhibitors

(2016) Mohsen Tavari et al.   MedChemComm

Synthetic α-hydroxytropolones as inhibitors of HIV reverse transcriptase ribonuclease H activity

(2016) Ryan P. Murelli et al.   MedChemComm

Ribonuclease H/DNA Polymerase HIV-1 Reverse Transcriptase Dual Inhibitor: Mechanistic Studies on the Allosteric Mode of Action of Isatin-Based Compound RMNC6

(2016) Angela Corona et al.   PLoS One

Synthesis and biological evaluation of DAPY–DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase

(2015) Hai-Qiu Wu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase

(2015) Rita Meleddu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationship of Pyrrolyl Diketo Acid Derivatives as Dual Inhibitors of HIV-1 Integrase and Reverse Transcriptase Ribonuclease H Domain

(2015) Giuliana Cuzzucoli Crucitti et al.   JOURNAL OF MEDICINAL CHEMISTRY

N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase

(2015) Luca Pescatori et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Highly Conserved Residues Involved in Inhibition of HIV-1 RNase H Function by Diketo Acid Derivatives

(2014) Angela Corona et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Hydroxylated Tropolones Inhibit Hepatitis B Virus Replication by Blocking Viral Ribonuclease H Activity

(2014) Gaofeng Lu et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Hepatitis B virus replication is blocked by a 2-hydroxyisoquinoline-1,3(2H,4H)-dione (HID) inhibitor of the viral ribonuclease H activity

(2014) Catherine W. Cai et al.   ANTIVIRAL RESEARCH

Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays

(2014) Wenmin Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel Dual Small-Molecule HIV inhibitors: Scaffolds and Discovery Strategies

(2014) Anran Song et al.   CURRENT PHARMACEUTICAL DESIGN

Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase

(2014) Roberta Costi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Investigation of a Novel Series of 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as Human Immunodeficiency Virus Type 1 Integrase Inhibitors

(2014) Virginie Suchaud et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, Biochemical, and Antiviral Evaluations of C6 Benzyl and C6 Biarylmethyl Substituted 2-Hydroxylisoquinoline-1,3-diones: Dual Inhibition against HIV Reverse Transcriptase-Associated RNase H and Polymerase with Antiviral Activities

(2014) Sanjeev Kumar V. Vernekar et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-Hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs), Novel Inhibitors of HIV Integrase with a High Barrier to Resistance

(2013) Belete A. Desimmie et al.   ACS Chemical Biology

Rationally Designed Multitarget Anti-HIV Agents

(2013) P. Zhan et al.   CURRENT MEDICINAL CHEMISTRY

Active site and allosteric inhibitors of the ribonuclease H activity of HIV reverse transcriptase

(2013) Angela Corona et al.   Future Medicinal Chemistry

Detecting Allosteric Sites of HIV-1 Reverse Transcriptase by X-ray Crystallographic Fragment Screening

(2013) Joseph D. Bauman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Investigation of Cycloheptathiophene-3-carboxamide Derivatives Targeting Influenza Virus Polymerase Assembly

(2013) Serena Massari et al.   JOURNAL OF MEDICINAL CHEMISTRY

6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic Acids as Dual Inhibitors of Recombinant HIV-1 Integrase and Ribonuclease H, Synthesized by a Parallel Synthesis Approach

(2013) Roberta Costi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploiting Drug-Resistant Enzymes as Tools To Identify Thienopyrimidinone Inhibitors of Human Immunodeficiency Virus Reverse Transcriptase-Associated Ribonuclease H

(2013) Takashi Masaoka et al.   JOURNAL OF MEDICINAL CHEMISTRY

4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors

(2013) Muriel Billamboz et al.   ACS Medicinal Chemistry Letters

Catechins containing a galloyl moiety as potential anti-HIV-1 compounds

(2012) Yali Zhao et al.   DRUG DISCOVERY TODAY

Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach

(2012) Simona Distinto et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The design, synthesis and biological evaluations of C-6 or C-7 substituted 2-hydroxyisoquinoline-1,3-diones as inhibitors of hepatitis C virus

(2011) Yue-Lei Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

6-Benzoyl-3-hydroxypyrimidine-2,4-diones as dual inhibitors of HIV reverse transcriptase and integrase

(2011) Jing Tang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Alizarine derivatives as new dual inhibitors of the HIV-1 reverse transcriptase-associated DNA polymerase and RNase H activities effective also on the RNase H activity of non-nucleoside resistant reverse transcriptases

(2011) Francesca Esposito et al.   FEBS Journal

(−)-Epigallocatechin-3-gallate is a new inhibitor of hepatitis C virus entry

(2011) Noémie Calland et al.   HEPATOLOGY

3-Hydroxypyrimidine-2,4-diones as an Inhibitor Scaffold of HIV Integrase

(2011) Jing Tang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, Activity, and Structural Analysis of Novel α-Hydroxytropolone Inhibitors of Human Immunodeficiency Virus Reverse Transcriptase-Associated Ribonuclease H

(2011) Suhman Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Magnesium Chelating 2-Hydroxyisoquinoline-1,3(2H,4H)-diones, as Inhibitors of HIV-1 Integrase and/or the HIV-1 Reverse Transcriptase Ribonuclease H Domain: Discovery of a Novel Selective Inhibitor of the Ribonuclease H Function

(2011) Muriel Billamboz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of nicotinic acid benzylidene hydrazide derivatives

(2011) Rakesh Narang et al.   MEDICINAL CHEMISTRY RESEARCH

Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of isonicotinic acid-1-(substituted phenyl)-ethylidene/cycloheptylidene hydrazides

(2011) Vikramjeet Judge et al.   MEDICINAL CHEMISTRY RESEARCH

Lersivirine, a Nonnucleoside Reverse Transcriptase Inhibitor with Activity against Drug-Resistant Human Immunodeficiency Virus Type 1

(2010) R. Corbau et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Pharmacophore and structure–activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase

(2010) Zhengqiang Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold

(2010) Peter D. Williams et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

2-Hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: Influence of the alkylation of position 4

(2010) Muriel Billamboz et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

N-3 Hydroxylation of Pyrimidine-2,4-diones Yields Dual Inhibitors of HIV Reverse Transcriptase and Integrase

(2010) Jing Tang et al.   ACS Medicinal Chemistry Letters

Designed Multiple Ligands: An Emerging Anti-HIV Drug Discovery Paradigm

(2009) Peng Zhan et al.   CURRENT PHARMACEUTICAL DESIGN

Inhibition of HIV-1 Ribonuclease H Activity by Novel Frangula-Emodine Derivatives

(2009) Kharlamova Tatyana et al.   Medicinal Chemistry

Anti-Cancer, Anti-Diabetic and Other Pharmacologic and Biological Activities of Penta-Galloyl-Glucose

(2009) Jinhui Zhang et al.   PHARMACEUTICAL RESEARCH

Vinylogous Ureas as a Novel Class of Inhibitors of Reverse Transcriptase-Associated Ribonuclease H Activity

(2008) Michaela Wendeler et al.   ACS Chemical Biology

Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: Introducing a diketoacid functionality into delavirdine

(2008) Zhengqiang Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of pyrimidine and quinolone conjugates as a scaffold for dual inhibitors of HIV reverse transcriptase and integrase

(2008) Zhengqiang Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel Quinolinonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors: Design, Synthesis, and Biological Activities

(2008) Roberto Di Santo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of a Series of 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and the Reverse Transcriptase RNase H Domain

(2008) Muriel Billamboz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure and Function of HIV-1 Reverse Transcriptase: Molecular Mechanisms of Polymerization and Inhibition

(2008) Stefan G. Sarafianos et al.   JOURNAL OF MOLECULAR BIOLOGY