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Carbamoyl-N-aryl-imine-urea: a new framework to obtain a putative leishmanicidal drug-candidate.


ABSTRACT: Leishmaniasis is a neglected parasitic disease, and current treatment includes limitations of toxicity, variable efficacy, high costs and inconvenient doses and treatment schedules. Therefore, new leishmanicidal drugs are still an unquestionable medical need. In this paper we described the design conception of a new framework, the carbamoyl-N-aryl-imine-urea, to obtain putative leishmanicidal drug-candidates. Compounds 9a-e and 10a-e were designed and synthesized and their leishmanicidal activity was studied in comparison to pentamidine, miltefosine and meglumine antimoniate. The conformational profile of the new carbamoyl-N-aryl-imine-urea framework was investigated by X-ray diffraction studies, using compound 9a as a model. The plasma stability of this putative peptide mime

SUBMITTER: Alves MA 

PROVIDER: S-EPMC9050848 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature