Synthesis of new bis(pyrazolo[1,5- a ]pyrimidines) linked to different spacers with potential MurB inhibitory activity utilizing 1 H -pyrazole-3,5-diamines DOI
A.A. Ahmed, Ahmed E. M. Mekky, Sherif M. H. Sanad

et al.

Synthetic Communications, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 13

Published: Nov. 17, 2024

Recently, there has been an increased interest in developing new antibacterial agents that target the MurB inhibition, which is necessary for bacterial survival. We developed a two-step tandem protocol to synthesize 15 bis(pyrazolo[1,5-a]pyrimidines), are attached alkane cores by amide linkages. The involved reacting appropriate bis(2-cyanoacetamides) with dimethylformamide-dimethylacetal toluene at 80 °C 3-4 h. crude bis(2-cyano-3-(dimethylamino)acrylamides) was collected, then reacted 3,5-diamino-1H-pyrazoles. reaction gave desired products 82-92% yields after 5-6 h of heating reflux pyridine. Bis(2,7-diamino-3-(4-methoxybenzyl)pyrazolo[1,5-a]pyrimidine-6-carboxamides) demonstrated comparable efficacy ciprofloxacin. Their MIC and MBC ranged from 2.8-3.0 5.7-6.0 µM, respectively, against S. aureus E. coli. Moreover, these displayed promising inhibitory activity IC50 ranging 7.8 8.0 µM.

Language: Английский

Advances in pyrazolo[1,5-a]pyrimidines: synthesis and their role as protein kinase inhibitors in cancer treatment DOI Creative Commons

Terungwa H. Iorkula,

Osasere Jude-Kelly Osayawe,

Daniel A. Odogwu

et al.

RSC Advances, Journal Year: 2025, Volume and Issue: 15(5), P. 3756 - 3828

Published: Jan. 1, 2025

Pyrazolo[1,5- a ]pyrimidines are notable class of heterocyclic compounds with potent protein kinase inhibitor (PKI) activity, playing critical role in targeted cancer therapy.

Language: Английский

Citations

1
Synthesis of new bis(pyrazolo[1,5- a ]pyrimidines) linked to different spacers with potential MurB inhibitory activity utilizing 1 H -pyrazole-3,5-diamines DOI
A.A. Ahmed, Ahmed E. M. Mekky, Sherif M. H. Sanad

et al.

Synthetic Communications, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 13

Published: Nov. 17, 2024

Recently, there has been an increased interest in developing new antibacterial agents that target the MurB inhibition, which is necessary for bacterial survival. We developed a two-step tandem protocol to synthesize 15 bis(pyrazolo[1,5-a]pyrimidines), are attached alkane cores by amide linkages. The involved reacting appropriate bis(2-cyanoacetamides) with dimethylformamide-dimethylacetal toluene at 80 °C 3-4 h. crude bis(2-cyano-3-(dimethylamino)acrylamides) was collected, then reacted 3,5-diamino-1H-pyrazoles. reaction gave desired products 82-92% yields after 5-6 h of heating reflux pyridine. Bis(2,7-diamino-3-(4-methoxybenzyl)pyrazolo[1,5-a]pyrimidine-6-carboxamides) demonstrated comparable efficacy ciprofloxacin. Their MIC and MBC ranged from 2.8-3.0 5.7-6.0 µM, respectively, against S. aureus E. coli. Moreover, these displayed promising inhibitory activity IC50 ranging 7.8 8.0 µM.

Language: Английский

Citations

3