In vitro leishmanicidal activity of lactone 1,4-dihydroquinoline derivatives against Leishmania (Leishmania) amazonensis

التفاصيل البيبلوغرافية
العنوان: In vitro leishmanicidal activity of lactone 1,4-dihydroquinoline derivatives against Leishmania (Leishmania) amazonensis
المؤلفون: Ana Carolina Bolela Bovo Candido, Rosangela da Silva de Laurentiz, Ana Paula da Rocha Pissurno, Lizandra Guidi Magalhães, Fernanda Amorim Santos
المساهمون: Universidade Estadual Paulista (Unesp), Univ Franca
المصدر: Web of Science
Repositório Institucional da UNESP
Universidade Estadual Paulista (UNESP)
instacron:UNESP
بيانات النشر: Springer Science and Business Media LLC, 2018.
سنة النشر: 2018
مصطلحات موضوعية: 0301 basic medicine, chemistry.chemical_classification, Cutaneous leishmaniasis, biology, 030231 tropical medicine, 030106 microbiology, Organic Chemistry, Dihydroquinoline derivatives, Lactone, medicine.disease, Leishmania, biology.organism_classification, In vitro, 03 medical and health sciences, 0302 clinical medicine, chemistry, Biochemistry, Toxicity, medicine, Macrophage, General Pharmacology, Toxicology and Pharmaceutics, Cytotoxicity, Amastigote
الوصف: Made available in DSpace on 2018-11-26T17:55:03Z (GMT). No. of bitstreams: 0 Previous issue date: 2018-09-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) A series of lactone 1,4-dihydroquinoline derivatives 4 (4 and 4aa-4cm) was screened for in vitro antileishmanial activity against the promastigote form of Leishmania (Leishmania) amazonensis. Screening results indicate that all of the synthesized compounds significantly reduced the growth of promastigote forms of promastigotes of L. (L.) amazonensis. The cytotoxicity of the most active compounds was also measured on peritoneal macrophage cells. Compounds 4ah and 4bn showed better activities than other derivatives with IC50 values of 6.22 and 9.05 mu M, respectively, with selectivity index 22 and 15 times less toxicity to macrophages cells than to parasites, respectively. The experimental data propose that the compounds may be further investigated against amastigote forms and may contribute to the search of new candidates drugs for treatment of cutaneous leishmaniasis. Univ Estadual Paulista, Fac Engn Ilha Solteira, Dept Fis & Quim, Sao Paulo, Brazil Univ Franca, Nucleo Pesquisas Ciencias Exatas & Tecnol, Franca, SP, Brazil Univ Estadual Paulista, Fac Engn Ilha Solteira, Dept Fis & Quim, Sao Paulo, Brazil FAPESP: 2014/07493-5 FAPESP: 2015/01394-8 FAPESP: 2016/24456-1
تدمد: 1554-8120
1054-2523
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c0eeba766550a732c2eb51b3b783fe9
https://doi.org/10.1007/s00044-018-2231-8
حقوق: OPEN
رقم الأكسشن: edsair.doi.dedup.....3c0eeba766550a732c2eb51b3b783fe9
قاعدة البيانات: OpenAIRE