Synthesis of new series of pyrazolo[4,3-d]pyrimidin-7-ones and pyrido[2,3-d]pyrimidin-4-ones for their bacterial and cyclin-dependent kinases (CDKs) inhibitory activities

doi:10.1007/s00044-010-9328-z

Paper

DOI: 10.1007/s00044-010-9328-z

Synthesis of new series of pyrazolo[4,3-d]pyrimidin-7-ones and pyrido[2,3-d]pyrimidin-4-ones for their bacterial and cyclin-dependent kinases (CDKs) inhibitory activities

Published May 1, 2011 · D. Geffken, R. Soliman, F. S. Soliman

Medicinal Chemistry Research

Q2 SJR score

Citations

Influential Citations

Full textSemantic Scholar

Abstract

Two series of pyrazolo[4,3-d]pyrimidin-7-ones and pyrido[2,3-d]pyrimidin-4-ones were designed, synthesised, and evaluated for their antibacterial activities and CDKs inhibitory activities. The pyridazine derivative: 6-phenyl-5-phenylhydrazono-2,3,4,5-tetrahydropyridazine-3,4-dione (3a) revealed activity against Staphylococcus aureus as Gram-positive bacteria while compound 2-(2-Ethoxyphenyl-5-Phenylpiperazinosulfonamido)-3H-pyrido[2,3-d]pyrimidin-4-one (13c) was showing moderate antifungal activity against Candida albicans.

In Vitro Study

Study Snapshot

The pyrazolo[4,3-d]pyrimidin-7-ones show antibacterial activity against Staphylococcus aureus and moderate antifungal activity against Candida albicans, with potential applications in antimicrobial and antifungal pharmaceuticals.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Full text analysis coming soon...

References

DOI: 10.1016/J.BMC.2007.06.023

Utility of 6-amino-2-thiouracil as a precursor for the synthesis of bioactive pyrimidine derivatives.

6-amino-2-thiouracil is a useful precursor for the synthesis of bioactive pyrimidine derivatives with potential antibacterial, antifungal, and antitumor properties.

2007·73citations·N. Mohamed et al.·Bioorganic & medicinal chemistry

Bioorganic & medicinal chemistry

DOI: 10.1016/J.TET.2006.12.043

A novel and efficient synthesis of pyrimido[4,5-d]pyrimidine-2,4,7-trione and pyrido[2,3-d:6,5-d] dipyrimidine-2,4,6,8-tetrone derivatives

This study presents a novel, efficient method for synthesis of pyrimido[4,5-d]pyrimidine-2,4,7-trione and pyrido[2,3-d:6,5-d] dipyrimidine-2,4,6,8-tetrone derivatives under microwave-a

2007·105citations·M. Dabiri et al.·Tetrahedron

Tetrahedron

DOI: 10.1016/J.EJMECH.2006.03.028

Convenient synthesis of novel 4-substitutedamino-5-trifluoromethyl-2,7-disubstituted pyrido[2,3-d] pyrimidines and their antibacterial activity.

Compounds 4h and 4d show significant activity against Gram positive bacteria and moderate activity against Gram negative bacteria, while all compounds are inactive against Pseudomonas aeruginosa at the maximum concentration.

2006·67citations·S. R. Kanth et al.·European Journal of Medicinal Chemistry

European Journal of Medicinal Chemistry

DOI: 10.1016/J.TETASY.2004.09.007

Enantio- and regiospecific reduction of ethyl 4-phenyl-2,4-dioxobutyrate with baker’s yeast: preparation of (R)-HPB ester

Baker's yeast effectively reduces ethyl 2,4-dioxo-4-phenylbutyrate to (R)-HPB ester, an intermediate for synthesis of ACE inhibitors, in 80% isolated yield.

2004·32citations·N. Fadnavis et al.·Tetrahedron-asymmetry

Tetrahedron-asymmetry

DOI: 10.1016/J.BMC.2004.03.039

Slow-binding inhibition of 2-keto-3-deoxy-6-phosphogluconate (KDPG) aldolase.

Slow-binding inhibition of KDPG aldolase can occur with various pyruvate analogues, depending on the substituent R (methyl or aromatic ring), resulting in stabilized iminium ion or conjugated enamine.

2004·11citations·Rémi Braga et al.·Bioorganic & medicinal chemistry

Bioorganic & medicinal chemistry

DOI: 10.1016/J.BMCL.2004.02.040

Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5(')-sulfonamide moiety of phenyl ring.

New sildenafil analogues with phosphonate groups in the 5(')-sulfonamide moiety show a 10-fold increase in PDE5 inhibitory activity compared to sildenafil, offering potential for new erectile dysfunction treatments.

2004·11citations·Dae-Kee Kim et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

Citations

DOI: 10.1021/acs.jmedchem.3c01976

Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy

The R4-substituted analogue 31c (NPD-3519) shows improved antitrypanosomal efficacy and metabolic stability, making it a promising candidate for future human African trypanosomiasis drug development.

2024·1citation·Yang Zheng et al.·Journal of Medicinal Chemistry

Journal of Medicinal Chemistry

DOI: 10.3390/molecules27010247

Novel Substituted Purine Isosteres: Synthesis, Structure-Activity Relationships and Cytotoxic Activity Evaluation

Novel substituted purine isosteres show promising antiproliferative activity against prostate and colon cancer cells, with the most promising derivative 14b inducing apoptosis in PC-3 cells.

2021·2citations·Spyridon Dimitrakis et al.·Molecules

Molecules

DOI: 10.1016/j.bioorg.2020.104343

2,4-Diketo esters: Crucial intermediates for drug discovery.

2,4-diketo esters are crucial intermediates in drug discovery due to their versatile synthesis and potential clinical applications in various diseases.

2020·30citations·Nenad Joksimović et al.·Bioorganic chemistry

Bioorganic chemistry

DOI: 10.1134/S1070363219090019

Alkaline Hydrolysis of 3-(2-Arylhydrazinylidene)-2,4-dioxoalkanoates

Alkaline hydrolysis of 3-(2-arylhydrazinylidene)-2,4-dioxoalkanoic acids yields 3-(2-arylhydrazinylidene)-2,4-dioxoalkanoic acids with antimicrobial activity against gram

2019·0citations·T. V. Levenets et al.·Russian Journal of General Chemistry

Russian Journal of General Chemistry

DOI: 10.1134/S1070363218060075

Reactions of 3-Arylhydrazono-2,4-dioxobutanoates with Hydrazine Hydrate

Hydrazine hydrate catalyzes the cyclization of 4-substituted 3-arylhydrazono-2,4-dioxobutanoates acids esters to produce 4-arylazo-3-pyrazolecarboxylic acids derivatives.

2018·0citations·T. V. Levenets et al.·Russian Journal of General Chemistry

Russian Journal of General Chemistry

DOI: 10.1007/s00044-018-2180-2

Selective and novel cyclin-dependent kinases 4 inhibitor: synthesis and biological evaluation

The selective CDK4 inhibitor 9a shows promising antitumor activity and may serve as a promising lead compound for further development of new CDK4 inhibitors.

2018·1citation·Qingxiang Guo et al.·Medicinal Chemistry Research

Medicinal Chemistry Research

DOI: 10.1016/j.bmc.2017.10.012

An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.

Pyrazolo[4,3-d]pyrimidine scaffold has shown potential as an anti-cancer, anti-infectious, and phosphodiesterase inhibitor drug due to its diverse synthetic and pharmacological activities.

2018·33citations·S. Cherukupalli et al.·Bioorganic & medicinal chemistry

Bioorganic & medicinal chemistry

DOI: 10.1016/J.TETLET.2016.08.060

The first synthesis of isoxazolo[3,4-c]pyridine-7-ones

This study successfully synthesized new isoxazolo[3,4-c]pyridine scaffolds using ethyl 4-(cyanomethyl)-5-phenylisoxazole-3-carboxylate and Raney/Ni catalysts, yielding 3-phenylisoxa

2016·1citation·Ervin Csimbók et al.·Tetrahedron Letters

Tetrahedron Letters