ArticleEuropean journal of medicinal chemistry2015
Synthesis of dihydropyrimidine α,γ-diketobutanoic acid derivatives targeting HIV integrase.
Article in European journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 31 citations in OpenAlex.
- A Review on Medicinal Chemistry and Biological Activity of Dihydropyrimidinones Against HIV.Archiv der Pharmazie · 2026Review
- Design and synthesis of novel pyridopyrimidine moieties linked to coumarin ring of potentially active cytotoxic agents and their docking study.Scientific reports · 2025Article
- Phase transfer catalysts shift the pathway to transmetalation in biphasic Suzuki-Miyaura cross-couplings.Nature communications · 2024Article
- Novel Steroidal[17,16-Molecules (Basel, Switzerland) · 2023Article
- Article
- Highly Efficient Synthesis of Substituted 3,4-Dihydropyrimidin-2-(1Molecules (Basel, Switzerland) · 2019Article
- Recent developments in the synthesis and applications of dihydropyrimidin-2(1H)-ones and thiones.Molecular diversity · 2018Review
- Therapeutic potential of heterocyclic pyrimidine scaffolds.Chemistry Central journal · 2018Review
- FeCl₃∙6H₂O/TMSBr-Catalyzed Rapid Synthesis of Dihydropyrimidinones and Dihydropyrimidinethiones under Microwave Irradiation.Molecules (Basel, Switzerland) · 2017Article
- Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity.Iranian journal of pharmaceutical research : IJPR · 2016Review
Corrections and comments
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Authors and funding
9 authors at 5 institutions in 2 countries.
Funding
Abstract
The synthesis and antiviral evaluation of a series of dihydropyrimidinone and thiopyrimidine derivatives bearing aryl α,γ-diketobutanoic acid moiety are described using the Biginelli multicomponent reaction as key step. The most active among 20 synthesized novel compounds were 4c, 4d and 5b, which possess nanomolar HIV-1 integrase (IN) stand transfer (ST) inhibition activities. In order to understand their mode of interactions within the IN active site, we docked all the compounds into the previously reported X-ray crystal structure of IN. We observed that compounds 4c, 4d and 5b occupied an area close to the two catalytic Mg(2+) ions surrounded by their chelating triad (E221, D128 and D185), DC16, Y212 and the β-diketo acid moiety of 4c, 4d and 5b chelating Mg(2+). As those compounds lack anti-HIV activities in cell, their prodrugs were synthetized. The prodrug 4c' exhibited an anti-HIV activity of 0.19 μM in primary human lymphocytes with some cytotoxicity. All together, these results indicate that the new analogs potentially interact within the catalytic site with highly conserved residues important for IN catalytic activity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.