Taking as lead structures previous reported pyrazoles, we designed and synthesized novel series of pyrazoles 2-5. All the isolated molecules were prepared by a stepwise protocol that allowed the preparation of N,S-thioketal intermediates which were then condensed with the proper hydrazine. Pyrazole hydrazones 3 displayed good antiproliferative and antioxidant activity, APs 4 exhibited significant antiangiogenetic properties and anilino-pyrazoles 5 showed antimalarial activity in the micromolar range. Overall, these results further support the pharmaceutical potential of amino pyrazoles in different therapeutic areas.
AMINO-PYRAZOLES: A PRIVILEGED SCAFFOLD FOR THE SYNTHESIS OF BIOLOGICALLY ACTIVE COMPOUNDS
Matteo Lusardi
2023-01-01
Abstract
Taking as lead structures previous reported pyrazoles, we designed and synthesized novel series of pyrazoles 2-5. All the isolated molecules were prepared by a stepwise protocol that allowed the preparation of N,S-thioketal intermediates which were then condensed with the proper hydrazine. Pyrazole hydrazones 3 displayed good antiproliferative and antioxidant activity, APs 4 exhibited significant antiangiogenetic properties and anilino-pyrazoles 5 showed antimalarial activity in the micromolar range. Overall, these results further support the pharmaceutical potential of amino pyrazoles in different therapeutic areas.
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