A Nature-Inspired Design Yields a New Class of Steroids Against Trypanosomatids.
Animals
Chagas Disease
/ drug therapy
Drug Development
Humans
Hydrazines
/ chemical synthesis
Ketones
/ chemical synthesis
Leishmania infantum
/ drug effects
Leishmania mexicana
/ drug effects
Leishmaniasis
/ drug therapy
Macrophages
/ drug effects
Mice
Parasitic Sensitivity Tests
Steroids
/ chemical synthesis
Structure-Activity Relationship
Thiosemicarbazones
/ chemical synthesis
Trypanocidal Agents
/ chemical synthesis
Trypanosoma cruzi
/ drug effects
anti-Leishmania spp. activity in vitro and in vivo
anti-T. cruzi activity in vitro and in vivo
cytotoxicity and genotoxicity
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
22 Oct 2019
22 Oct 2019
Historique:
received:
17
08
2019
revised:
08
10
2019
accepted:
12
10
2019
entrez:
27
10
2019
pubmed:
28
10
2019
medline:
9
4
2020
Statut:
epublish
Résumé
Chagas disease and Leishmaniasis are neglected endemic protozoan diseases recognized as public health problems by the World Health Organization. These diseases affect millions of people around the world however, efficient and low-cost treatments are not available. Different steroid molecules with antimicrobial and antiparasitic activity were isolated from diverse organisms (ticks, plants, fungi). These molecules have complex structures that make de novo synthesis extremely difficult. In this work, we designed new and simpler compounds with antiparasitic potential inspired in natural steroids and synthesized a series of nineteen steroidal arylideneketones and thiazolidenehydrazines. We explored their biological activity against
Identifiants
pubmed: 31652542
pii: molecules24203800
doi: 10.3390/molecules24203800
pmc: PMC6832524
pii:
doi:
Substances chimiques
Hydrazines
0
Ketones
0
Steroids
0
Thiosemicarbazones
0
Trypanocidal Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Consejo Nacional de Ciencia y Tecnología
ID : Nº 020/2015-14-INV-154, Paraguay
Organisme : Comisión Sectorial de Investigación Científica
ID : CSIC I+D 2016 program for the support grants ID435
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