Design and synthesis of 1,2,4‐triazolo[1,5‐a]pyrimidine derivatives as PDE 4B inhibitors endowed with bronchodilator activity
Sign Up to like & getrecommendations! Published in 2019 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201900002
Abstract: A series of 1,2,4‐triazolo[1,5‐a]pyrimidine derivatives was designed, synthesized, and screened for their phosphodiesterase (PDE 4B) inhibitory activity and bronchodilation ability. Compound 7e showed 41.80% PDE 4B inhibition at 10 µM. Eight compounds were screened for their… read more here.
Keywords: bronchodilator activity; triazolo pyrimidine; activity; pyrimidine derivatives ... See more keywords
Discovery of novel pyrazole and pyrazolo[1,5‐a]pyrimidine derivatives as cyclooxygenase inhibitors (COX‐1 and COX‐2) using molecular modeling simulation
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200395
Abstract: Searching for effective and selective anti‐inflammatory agents, our study involved designing and synthesizing new pyrazole and pyrazolo[1,5‐a]pyrimidine derivatives 4–11. The structures of the synthesized derivatives were confirmed using different spectroscopic techniques. Virtual screening was achieved… read more here.
Keywords: pyrazole pyrazolo; cox; pyrazolo pyrimidine; cox cox ... See more keywords
Synthesis of functionalized triazolo[1,5-a]pyrimidine derivatives
Sign Up to like & getrecommendations! Published in 2018 at "Chemistry of Heterocyclic Compounds"
DOI: 10.1007/s10593-018-2230-1
Abstract: New triazolo[1,5-a]pyrimidines containing aroyl and acetyl or ester groups in the pyrimidine ring were synthesized in a process related to the Biginelli-like reaction, using hydrates of arylglyoxals, β-dicarbonyl compounds, and 1H-1,2,4-triazol-5-amine. Reaction was carried out… read more here.
Keywords: triazolo pyrimidine; synthesis functionalized; chemistry; pyrimidine derivatives ... See more keywords
A convenient route to the 1,2,5-oxadiazole-substituted 1,2,4-triazolo[1,5-a]pyrimidine derivatives
Sign Up to like & getrecommendations! Published in 2019 at "Chemistry of Heterocyclic Compounds"
DOI: 10.1007/s10593-019-02590-7
Abstract: A convenient synthesis of 1,2,4-triazole and 1,2,4-triazolo[1,5-a]pyrimidines with 3-amino-1,2,5-oxadiazole substituent starting from available 4-amino-1,2,5-oxadiazole-3-carbohydrazide and benzoyl cyanamide has been developed. read more here.
Keywords: route oxadiazole; triazolo pyrimidine; pyrimidine derivatives; substituted triazolo ... See more keywords
An efficient one-pot synthesis of highly functionalized benzylpyrazolyl pyrido[1,2-a]pyrimidine derivatives using CuFe2O4 nanoparticles under solvent-free conditions
Sign Up to like & getrecommendations! Published in 2017 at "Research on Chemical Intermediates"
DOI: 10.1007/s11164-017-3022-4
Abstract: An efficient and green protocol for the synthesis of novel benzylpyrazolyl pyrido[1,2-a]pyrimidine derivatives via three-component reaction of aryl aldehydes, 2-hydroxy-4H-pyrido[1,2-a]pyrimidine-4-ones, and 3-methyl-1-phenyl-1H-pyrazol-5-one has been reported using a magnetically separable and reusable heterogeneous copper ferrite (CuFe2O4)… read more here.
Keywords: free conditions; benzylpyrazolyl pyrido; pyrimidine derivatives; pyrimidine ... See more keywords
Metal free green protocol for the synthesis of bis-spiro piperidine and pyrimidine derivatives
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DOI: 10.1007/s11164-018-3310-7
Abstract: A highly efficient one-pot three-component synthesis of bis-spiro piperidine and pyrimidine derivatives has been reported by performing the reaction of formaldehyde, aromatic aniline and 1,3-dicarbonyl compounds. This reaction was carried out at room temperature in… read more here.
Keywords: pyrimidine derivatives; synthesis bis; piperidine pyrimidine; reaction ... See more keywords
Synthesis and biological evaluation of 7-(aminoalkyl)pyrazolo[1,5-a]pyrimidine derivatives as cathepsin K inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.11.029
Abstract: A series of novel 7-aminoalkyl substituted pyrazolo[1,5-a]pyrimidine derivatives were synthesized and tested for inhibition of cathepsin K. The synthetic methodology comprises cyclization of 5-aminopyrazoles with N-Boc-α-amino acid-derived ynones followed by transformation of the ester and… read more here.
Keywords: biological evaluation; pyrimidine derivatives; pyrimidine; pyrazolo pyrimidine ... See more keywords
Design, synthesis and antitumor evaluation of novel 5-methylpyrazolo[1,5-a]pyrimidine derivatives as potential c-Met inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104356
Abstract: A series of novel 5-methylpyrazolo[1,5-a]pyrimidine derivatives (10a-10x) were designed, synthesized, and evaluated for their in vitro inhibitory activities against c-Met kinase and antiproliferative activities against the SH-SY5Y, MDA-MB-231, A549, and HepG2 cell lines. Most of… read more here.
Keywords: methylpyrazolo pyrimidine; novel methylpyrazolo; met inhibitors; pyrimidine derivatives ... See more keywords
Design, synthesis, molecular docking and in silico ADMET profile of pyrano[2,3-d]pyrimidine derivatives as antimicrobial and anticancer agents.
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DOI: 10.1016/j.bioorg.2021.105186
Abstract: Pyrano[2,3-d]pyrimidine derivatives were synthesized by treating cyclic compounds containing active methylene group with aldehyde and malononitrile in butanol. The behavior of pyrano[2,3-d]pyrimidine towards some electrophlies namely triethylorthoformate followed by nitrogen nucleophiles as isobutylamine, urea, phenylthiourea,… read more here.
Keywords: pyrimidine derivatives; pyrano; ic50; pyrano pyrimidine ... See more keywords
Synthesis and biological evaluation of selected 7H-pyrrolo[2,3-d]pyrimidine derivatives as novel CDK9/CyclinT and Haspin inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Chemico-biological interactions"
DOI: 10.1016/j.cbi.2021.109643
Abstract: Protein kinases, including CDK9/CyclinT and Haspin, are regarded as potential drug targets in cancer therapy. Findings from a previous study suggested 7-azaindole as a privileged scaffold for producing inhibitors of CDK9/CyclinT and Haspin. Inspired by… read more here.
Keywords: pyrrolo pyrimidine; cyclint; pyrimidine derivatives; cyclint haspin ... See more keywords
Identification of thiazolo[5,4-d]pyrimidine derivatives as potent antiproliferative agents through the drug repurposing strategy.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.04.056
Abstract: A series of thiazolo[5,4-d]pyrimidine derivatives were synthesized and evaluated for their antiproliferative activities on three cancer cell lines. The structure-activity relationship studies were conducted through the variation in the three regions of the thiazolo-pyrimidine core.… read more here.
Keywords: thiazolo pyrimidine; potent antiproliferative; identification thiazolo; pyrimidine derivatives ... See more keywords