MATTEO LUSARDI

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...

A pyrazole nucleus is an easy-to-prepare scaffold with large therapeutic potential. Consequently, the search for new pyrazole-based compounds is of great interest to the academic community as well as industry. In the last ten years, a large number of papers and reviews on the design, synthesis, and biological evaluation of different classes of...

5-pyrazolyl urea derivatives represent attractive molecules endowed with interesting pharmaceutical properties. In particular, GeGe-3 showed promising antiangiogenetic activity interfering with MAPK and PI3K signalling pathways and inhibiting proliferation and migration in HUVEC cells. Furthermore, proteomic studies indicated Calreticulin as...

Compounds 1 showed promising antioxidant activity by inhibiting ROS formation in platelet. The substitution of the catechol moiety modulates the ability of the compounds to block ROS formation. To further extend the structure-activity relationships (SARs) and evaluate the insertion of an additional substituent on the pyrazole ring, derivatives...

The pyrazolyl urea GeGe-3 was identified as a potential angiogenesis inhibitor, interfering with MAPK and PI3K signaling pathways in HUVEC cells. The compound was able to inhibit cell migration and proliferation and to interfere with the intersegmental tube formation in zebrafish embryos. Furthermore, other investigation led to the...

5-Amino pyrazole carbohydrazides showed promising antioxidant activity, inhibiting reactive oxygen species (ROS) elevation in neutrophils. In previous structure-activity relationship (SAR) studies the free ammino group proved to be an important structural determinant for activity. In order to further extend the SARs of this class of compounds,...

The 3-phenyl pyrazoles 1 and the anilino pyrazoles 2 were identified as effective antimalarial agents. Through a molecular hybridization strategy, a library pyrazoles 3 was designed, synthesized and tested for antiplasmodial properties. 5-Anilino pyrazoles 3a-p were screened for their antimalarial properties using Chloroquine (CQ) as reference...

During the last years, we developed a large library of new selective phosphodiesterase 4D inhibitors, maintaining the catechol portion of the well-known PDE4 inhibitor Rolipram, featuring different substitutions in place of the lactam group of this reference compound. Based on the X-ray analysis of PDE4 inhibitors (PDE4Is) previously...