Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species

Chronic pulmonary infection is a hallmark of lung disease in cystic fibrosis (CF). Infections dominated by non-fermentative Gram-negative bacilli are particularly difficult to treat and highlight an urgent need for the development of new class of agents to combat these infections. In this work, a s...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Saeed, Aamer, Bosch, María Alejandra, Bettiol, Marisa, Nossa González, Diana L., Erben, Mauricio Federico, Lamberti, Yanina Andrea
Formato:	Articulo
Lenguaje:	Inglés
Publicado:	2018
Materias:	Química antimicrobials thioureas guanidines drug-resistant cystic fibrosis
Acceso en línea:	http://sedici.unlp.edu.ar/handle/10915/81365
Aporte de:	SEDICI (UNLP) de Universidad Nacional de La Plata

id	I19-R120-10915-81365
record_format	dspace
institution	Universidad Nacional de La Plata
institution_str	I-19
repository_str	R-120
collection	SEDICI (UNLP)
language	Inglés
topic	Química antimicrobials thioureas guanidines drug-resistant cystic fibrosis
spellingShingle	Química antimicrobials thioureas guanidines drug-resistant cystic fibrosis Saeed, Aamer Bosch, María Alejandra Bettiol, Marisa Nossa González, Diana L. Erben, Mauricio Federico Lamberti, Yanina Andrea Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species
topic_facet	Química antimicrobials thioureas guanidines drug-resistant cystic fibrosis
description	Chronic pulmonary infection is a hallmark of lung disease in cystic fibrosis (CF). Infections dominated by non-fermentative Gram-negative bacilli are particularly difficult to treat and highlight an urgent need for the development of new class of agents to combat these infections. In this work, a small library comprising thiourea and guanidine derivatives with low molecular weight was designed; these derivatives were studied as antimicrobial agents against Gram-positive, Gram-negative, and a panel of drug-resistant clinical isolates recovered from patients with CF. One novel compound, a guanidine derivative bearing adamantane-1-carbonyl and 2-bromo-4,6-difluouro-phenyl substituents (H-BDF), showed potent bactericidal activity against the strains tested, at levels generally higher than those exhibited by tobramycin, ceftazimide and meropenem. The role that different substituents exert in the antimicrobial activity has been determined, highlighting the importance of the halo-phenyl group in the guanidine moiety. The new compound displays low levels of cytotoxicity against THP-1 and A549 cells with a selective index (SI) > 8 (patent application PCT/IB2017/054870, August 2017). Taken together, our results indicate that H-BDF can be considered as a promising antimicrobial agent.
format	Articulo Articulo
author	Saeed, Aamer Bosch, María Alejandra Bettiol, Marisa Nossa González, Diana L. Erben, Mauricio Federico Lamberti, Yanina Andrea
author_facet	Saeed, Aamer Bosch, María Alejandra Bettiol, Marisa Nossa González, Diana L. Erben, Mauricio Federico Lamberti, Yanina Andrea
author_sort	Saeed, Aamer
title	Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species
title_short	Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species
title_full	Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species
title_fullStr	Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species
title_full_unstemmed	Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species
title_sort	novel guanidine compound against multidrug-resistant cystic fibrosis-associated bacterial species
publishDate	2018
url	http://sedici.unlp.edu.ar/handle/10915/81365
work_keys_str_mv	AT saeedaamer novelguanidinecompoundagainstmultidrugresistantcysticfibrosisassociatedbacterialspecies AT boschmariaalejandra novelguanidinecompoundagainstmultidrugresistantcysticfibrosisassociatedbacterialspecies AT bettiolmarisa novelguanidinecompoundagainstmultidrugresistantcysticfibrosisassociatedbacterialspecies AT nossagonzalezdianal novelguanidinecompoundagainstmultidrugresistantcysticfibrosisassociatedbacterialspecies AT erbenmauriciofederico novelguanidinecompoundagainstmultidrugresistantcysticfibrosisassociatedbacterialspecies AT lambertiyaninaandrea novelguanidinecompoundagainstmultidrugresistantcysticfibrosisassociatedbacterialspecies
bdutipo_str	Repositorios
_version_	1764820488040742912

Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species

Ejemplares similares