Related Experiment Videos
Synthesis, modeling and biological evaluation of hybrids from pyrazolo[1,5c]pyrimidine as antileishmanial agents
Kamal Fahmy Mohamed Atta1, Tamer Mohamed Ibrahim2, Omaima Osman Mahmoud Farahat1
1Department of Chemistry, Faculty of Science, Alexandria University, Alexandria 21321, Egypt.
Aim:
A new series of pyrazolo[1,5-c]pyrimidines were synthesized by different hybridization strategies.
Methodology:
All structures were confirmed by IR, 1H, 13C, 1H-13C heteronuclear multiple-quantum correlation (HMQC) spectra and microanalysis. They were evaluated for their in vitro antileishmanial activity against miltefosine and amphotericin B deoxycholate as reference drugs.
Results:
The most active compounds 2a and 9a demonstrated superior potencies to miltefosine by ten- and six-fold, respectively, for the promastigote form, and by 5.5-fold for the amastigote form. Their binding scenario to Leishmania major pteridine reductase was rationalized by docking experiments. In addition, all compounds were safe for the experimental animals orally up to 150 mg/kg and parenterally up to 75 mg/kg.
Conclusion:
This study provides novel chemotype class for antileishmanial activity. [Formula: see text].