Ortho-nitrobenzyl derivatives as potential anti-schistosomal agents
Braz. J. Pharm. Sci. (Online)
;
54(2): e17376, 2018. tab, graf
Article
Dans Anglais
| LILACS
| ID: biblio-951932
ABSTRACT
ABSTRACT In the search for new anti-schistosomal agents, a series of fifteen ortho-nitrobenzyl derivatives was assayed in vitro against both the schistosomulum (somule) and adult forms of Schistosoma mansoni. Compounds 8 and 12 showed significant activity against somules at low micromolar concentrations, but none was active against adults. The SAR demonstrated that the compounds most active against the parasite were mutagenic to the human cell line RKO-AS45-1 only at concentrations 10- to 40-fold higher than the worm-killing dose. Given their electrophilicity, compounds were also screened as inhibitors of the S. mansoni cysteine protease (cathepsin B1) in vitro. Amides 5 and 15 exhibited a modest inhibition activity with values of 55.7 and 50.6 % at 100 µM, respectively. The nitrobenzyl compounds evaluated in this work can be regarded as hits in the search for more active and safe anti-schistosomal agents.
Texte intégral:
Disponible
Indice:
LILAS (Amériques)
Sujet Principal:
Schistosoma mansoni
langue:
Anglais
Texte intégral:
Braz. J. Pharm. Sci. (Online)
Thème du journal:
Farmacologia
/
Teraputica
/
Toxicologia
Année:
2018
Type:
Article
/
descriptif de projet
Pays d'affiliation:
Brésil
/
États-Unis d'Amérique
Institution/Pays d'affiliation:
Federal University of Minas Gerais/BR
/
Federal University of São João del Rei/BR
/
University of California San Diego/US
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