Anti-Trypanosomal and Antimalarial Properties of Tetralone Derivatives and Structurally Related Benzocycloalkanones.
Medicina (Kaunas)
; 55(5)2019 May 24.
Article
em En
| MEDLINE
| ID: mdl-31137665
ABSTRACT
Background and objectives:
Sleeping sickness and malaria alike are insect-borne protozoan diseases that share overlapping endemic areas in sub-Saharan Africa. The causative agent for malaria has developed resistance against all currently deployed anti-malarial agents. In the case of sleeping sickness, the currently deployed therapeutic options are limited in efficacy and activity spectra, and there are very few drug candidates in the development pipeline. Thus, there is a need to search for new drug molecules with a novel mode of actions. Materials andMethods:
In the current study, an in vitro screening of a library of tetralone derivatives and related benzocycloalkanones was effected against T. b. brucei and P. falciparum.Results:
Several hits with low micromolar activity (0.4-8 µM) against T. b. brucei were identified.Conclusions:
The identified hits have a low molecular weight (<280 Da), a low total polar surface area (<50 Ų), and a defined structure activity relationship, which all make them potential starting points for further hit optimization studies.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tripanossomíase Africana
/
Tetralonas
/
Malária
Limite:
Humans
Idioma:
En
Revista:
Medicina (Kaunas)
Assunto da revista:
MEDICINA
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
África do Sul
País de publicação:
CH
/
SUIZA
/
SUÍÇA
/
SWITZERLAND