Novel Potent Metallocenes against Liver Stage Malaria

• Type: Article in International Scientific Journal
• Date: 2012

Authors

Joana Matos (Author) Other; Filipa P da Cruz (Author) Other; Elia Cabrita (Author) Other; Jiri Gut (Author) Other; Fatima Nogueira (Author) Other; Virgilio E do Rosario (Author) Other; Rui Moreira (Author) Other; Philip J Rosenthal (Author) Other; Miguel Prudencio (Author) Other; Paula Gomes (Author) FCUP

Journal

Title: Antimicrobial Agents and Chemotherapy

Vol. 56

Pages: 1564-1570

ISSN: 0066-4804

Publisher: American Society for Microbiology

Indexing

ISI Web of Knowledge - 34 Citations

Scopus - 35 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-002-CPH

DOI: 10.1128/aac.05345-11

Abstract (EN): Novel conjugates of the antimalarial drug primaquine (compound 1) with ferrocene, named primacenes, have been synthesized and screened for their activities against blood stage and liver stage malaria in vitro and host-vector transmission in vivo. Both transmission-blocking and blood-schizontocidal activities of the parent drug were conserved only in primacenes bearing a basic aliphatic amine group. Liver stage activity did not require this structural feature, and all metallocenes tested were comparable to or better than primaquine in this regard. Remarkably, the replacement of primaquine's aliphatic chain by hexylferrocene, as in compound 7, led to a similar to 45-fold-higher level activity against liver stage parasitemia than that of primaquine.

Language: English

Type (Professor's evaluation): Scientific