Development of anti-parasitic and antiviral agents

1] Development of novel antimalarials

This research activity led to the development of a series of antimalarial drugs characterized by diverse scaffolds and mechanism of action.

Developed antimalarial compounds can be divided as follows: i) quinolylhydrazone-based antimalarials; ii) antimalarials based on a pharmacophore structurally related to clotrimazole; iii) hybrids between pharmacophoric moieties of chloroquine and the novel class of clotrimazole-based antimalarials previously developed; iv) endoperoxide-containing antimalarials inspired by the natural compound dihydroplakortin; v) antimalarials with benzoxazine and quinazolyl structures; vi) quinolyl hydrazones as novel inhibitors of plasmodial serine-protease PfSUB1.


Researchers involved

  • Giuseppe Campiani
  • Brogi Simone - PostDoc
  • Giovani Simone - Ph.D. student
  • Relitti Nicola - Ph.D. student
  • Di Cerbo Luisa - Ph.D. student
2] Development of antiviral and anti-infective agents

This research activity led to the identification of a series of anti-HIV, anti-HCV and anti-tubercular compounds.

This research activity led to: i) development of anti-HIV agents active against reverse-transcriptase (RT), ii) development of anti-HCV agents active as NS3 helicase (hNS3) inhibitors, and iii) anti-tubercular compounds based on a quinolyl hydrazone structure. In the field of anti-HIV agents this research activity lead to the characterization of the first representative of the third generation non-nucleoside inhibitors (NNRTI), selectively binding the ternary HIV-1 RT complex. Regarding to the HCV hNS3 research line, the first nucleotide-mimicking inhibitor of hNS3 were discovered.


Researchers involved

  • Giuseppe Campiani