Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolites

Autor:	Digby F. Warner, Kawaljit Singh, Mathew Njoroge, Kelly Chibale, Nicholas M. Njuguna, Elizabeth Kigondu
Rok vydání:	2014
Předmět:	Pharmacology Spectinomycin medicine.drug_class Chemistry Organic Chemistry Pharmaceutical Science Kanamycin Antimycobacterial Biochemistry Streptomycin Drug Discovery medicine Molecular Medicine Chlorpromazine Rifampicin Active metabolite medicine.drug
Zdroj:	Med. Chem. Commun.. 5:502-506
ISSN:	2040-2511 2040-2503
Popis:	The antimycobacterial activities of chlorpromazine and its metabolites were evaluated alone and in combination with antitubercular drugs. Although associated with limited antimycobacterial activity when tested individually, chlorpromazine and its metabolites exhibited clear synergy when tested in combination with a number of aminoglycosides as well as the active metabolite of rifampicin, 25-desaceteylrifampicin. The combination of chlorpromazine and spectinomycin was associated with the greatest synergy, yielding a fractional inhibitory concentration index (FICI) of 0.31. Synergistic interactions were also observed for combinations of 7-hydroxychlorpromazine or nor-chlorpromazine with kanamycin, streptomycin, spectinomycin and 25-desacetylrifampicin (FICI 0.19–0.5).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::3fefa9e2df5308e682d599373c0ef6fd https://doi.org/10.1039/c3md00387f Zobrazit plný text záznamu