Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.

Journal of medicinal chemistry - 14 May 2020

Kang Dongwei, Feng Da, Sun Yanying, Fang Zengjun, Wei Fenju, De Clercq Erik, Pannecouque Christophe, Liu Xinyong, Zhan Peng

Abstract excerpt

The development of efficacious NNRTIs for AIDS therapy commonly encountered the rapid generation of drug-resistant mutations, which becomes a major impediment to effective anti-HIV treatment. Using a structure-based bioisosterism strategy, a series of piperidine-substituted thiophene[2,3-d]pyrimidine derivatives were designed and synthesized. Compound 9a yielded the greatest potency, exhibiting significantly...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Anti-HIV Agents
Share to Enzyme Assays

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to HIV Reverse Transcriptase

Share to Microsomes, Liver

Share to Molecular Docking Simulation

Share to Pyrimidines

Share to Reverse Transcriptase Inhibitors

Share to Thiophenes

Source

Identifiers

PMID: 32293182
DOI: 10.1021/acs.jmedchem.0c00117

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 3 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.PMID 32293182Read ↗

Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.Semantic proximity Read ↗

Development of enhanced HIV-1 non-nucleoside reverse transcriptase inhibitors with improved resistance and pharmacokinetic profiles.Semantic proximity Read ↗

Recent advances in the discovery and development of novel HIV-1 NNRTI platforms: 2006-2008 update.Semantic proximity Read ↗

Structure, Synthesis and Inhibition Mechanism of Nucleoside Analogues as HIV‐1 Reverse Transcriptase Inhibitors (NRTIs)Semantic proximity Read ↗

P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.Semantic proximity Read ↗

2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.Semantic proximity Read ↗

The Current Status of the NNRTI Family of Antiretrovirals Used Against HIV InfectionSemantic proximity Read ↗

Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses.Semantic proximity Read ↗

TSAO Compounds: The Comprehensive Story of a Unique Family of HIV- 1 Specific Inhibitors of Reverse TranscriptaseSemantic proximity Read ↗

Discovery of 2,4,5-Trisubstituted 6-Aminopyrimidines as Potent HIV-1 NNRTIs with Improved Resistance Profiles against the K103N/Y181C MutantSemantic proximity Read ↗

Challenges and approaches in the discovery of human immunodeficiency virus type‐1 non‐nucleoside reverse transcriptase inhibitorsSemantic proximity Read ↗

Diphenyl ether non-nucleoside reverse transcriptase inhibitors with excellent potency against resistant mutant viruses and promising pharmacokinetic properties.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.