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Christophe Pannecouque

Explore the profile of Christophe Pannecouque including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 403
Citations 3206
Followers 0
Related Specialties
Chemistry
Biochemistry
Pharmacology
Top 10 Co-Authors
Erik De Clercq
Xinyong Liu
Peng Zhan
Jan Balzarini
Dongwei Kang
Fen-Er Chen
Dirk Daelemans
Zhao Wang
Boshi Huang
Myriam Witvrouw
Published In
Eur J Med Chem
Bioorg Med Chem
J Med Chem
Bioorg Med Chem Lett
Chem Biol Drug Des
Affiliations
Soon will be listed here.
Recent Articles
1.
Structure-based design of novel 2,4,5-trisubstituted pyrimidine derivatives as potent HIV-1 NNRTIs by exploiting the tolerant regions in NNTRIs binding pocket
Zhou Z, Xie M, Zhuo Z, Wang Y, Zhao F, Tao S, et al.
Eur J Med Chem . 2025 Mar; 289:117464. PMID: 40048799
To promote the development of the new generation of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of novel 2,4,5-trisubstituted pyrimidine derivatives targeting the "tolerant region I″ and "tolerant region...
2.
Structure-based discovery of novel diarylpyrimidines as potent and selective Non-Nucleoside reverse transcriptase inhibitors: From CH(CN)-Biphenyl-Diarylpyrimidines to CNNH-Biphenyl-Diarylpyrimidines
Chen X, Pannecouque C, De Clercq E, Lian Y, Corona A, Dettori L, et al.
Eur J Med Chem . 2025 Jan; 285:117271. PMID: 39813776
In order to enhance the anti-HIV-1 potency and selectivity of the previously reported compound 3 (EC = 27 nM, SI = 1361), a series of novel biphenyl-diarylpyrimidine derivatives were developed...
3.
Synthesis, Characterization, and antiviral evaluation of New Chalcone-Based Imidazo[1,2-a]pyridine Derivatives: Insights from in vitro and in silico Anti-HIV studies
Azzouzi M, El Hadad S, Azougagh O, Ouchaoui A, Abou-Salama M, Oussaid A, et al.
Bioorg Chem . 2024 Dec; 154:108102. PMID: 39740310
Given the ease of synthetic accessibility and the promising biological profile demonstrated by both imidazo[1,2-a]pyridine and Chalcone derivatives, a series of Chalcone-based imidazo[1,2-a]pyridine derivatives were synthesized and characterized using H...
4.
Synthesis, crystal structure, and antiviral evaluation of new imidazopyridine-schiff base derivatives: and anti-HIV studies
Azzouzi M, Ouchaoui A, Azougagh O, El Hadad S, Abou-Salama M, Oussaid A, et al.
RSC Adv . 2024 Nov; 14(50):36902-36918. PMID: 39569129
A series of Imidazo[1,2-]pyridine-Schiff base derivatives were synthesized and characterized using H NMR, C NMR, Mass Spectrometry and FTIR techniques, and the structure of 4a was further confirmed through single-crystal...
5.
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile
Dai J, Jiang X, Gao H, Huang B, De Clercq E, Pannecouque C, et al.
Eur J Med Chem . 2024 Nov; 281:117033. PMID: 39536498
As an important part of anti-AIDS therapy, HIV-1 non-nucleoside reverse transcriptase inhibitors are plagued by resistance and toxicity issues. Taking our reported XJ-18b1 as lead compound, we designed a series...
6.
Expanding the Solvent/Protein Region Occupation of the Non-Nucleoside Reverse Transcriptase Inhibitor Binding Pocket for Improved Broad-Spectrum Anti-HIV-1 Efficacy: from Rigid Phenyl-Diarylpyrimidines to Flexible Hydrophilic...
Huang W, Pannecouque C, De Clercq E, Corona A, Maloccu S, Tramontano E, et al.
J Med Chem . 2024 Nov; 67(21):19889-19904. PMID: 39498544
Considering the nonideal antiresistance efficacy of our previously reported non-nucleoside reverse transcriptase inhibitor , a series of novel piperidine-diarylpyrimidine derivatives were designed through expanding solvent/protein region occupation. The representative compound...
7.
Rapid identification of novel indolylarylsulfone derivatives as potent HIV-1 NNRTIs miniaturized CuAAC click-chemistry-based combinatorial libraries
Gao P, Song S, Pannecouque C, De Clercq E, Zhan P, Liu X
RSC Med Chem . 2024 Oct; PMID: 39421538
This article presents the rapid identification of novel indolylarylsulfone (IAS) derivatives as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 through a miniaturized click-chemistry-based combinatorial library approach. Utilizing copper(i)-catalyzed azide-alkyne...
8.
"Pseudosubstrate Envelope"/Free Energy Perturbation-Guided Design and Mechanistic Investigations of Benzothiazole HIV Capsid Modulators with High Ligand Efficiency
Xu S, Wang S, Zhou Y, Foley N, Sun L, Walsham L, et al.
J Med Chem . 2024 Oct; 67(21):19057-19076. PMID: 39418501
Based on our proposed "pseudosubstrate envelope" concept, 25 benzothiazole-bearing HIV capsid protein (CA) modulators were designed and synthesized under the guidance of free energy perturbation technology. The most potent compound,...
9.
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses
Jiang X, Zalloum W, Gao Z, Dai J, Ji X, Xie M, et al.
Eur J Med Chem . 2024 Oct; 280:116941. PMID: 39369484
HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) play a crucial role in combination antiretroviral therapy (cART). To further enhance their antiviral activity and anti-resistance properties, we developed a series of novel...
10.
Fragment Addition-Based Design of Heteroaromatic-Biphenyl-DAPYs as Potent and Orally Available Non-nucleoside Reverse Transcriptase Inhibitors Featuring Significantly Enhanced Safety
Huang W, Pannecouque C, De Clercq E, Wang S, Chen F
J Med Chem . 2024 Oct; 67(19):17568-17584. PMID: 39352547
Our previously disclosed biphenyl-DAPY emerged as a potent inhibitor against WT HIV-1 and various mutant strains. Yet, its journey toward clinical application was thwarted by pronounced cytotoxicity and low selectivity...