Synthesis, antibacterial activity, and quantitative structure-activity relationships of new (Z)-2-(nitroimidazolylmethylene)-3(2H)-benzofuranone derivatives

Autor:	Narges, Hadj-esfandiari, Latifeh, Navidpour, Hooman, Shadnia, Mohsen, Amini, Nasrin, Samadi, Mohammad Ali, Faramarzi, Abbas, Shafiee
Rok vydání:	2007
Předmět:	Bacteria Molecular Structure Imidazoles Quantitative Structure-Activity Relationship Microbial Sensitivity Tests Anti-Bacterial Agents Benzofurans
Zdroj:	Bioorganicmedicinal chemistry letters. 17(22)
ISSN:	0960-894X
Popis:	A new series of (Z)-2-(1-methyl-5-nitroimidazole-2-ylmethylene)-3(2H)-benzofuranones (11a-p) and (Z)-2-(1-methyl-4-nitroimidazole-5-ylmethylene)-3(2H)-benzofuranones (12a-m) were synthesized and assayed for their antibacterial activity against Gram-positive and Gram-negative bacteria. Most of the 5-nitroimidazole analogues (11a-p) showed a remarkable inhibition of a wide spectrum of Gram-positive bacteria (Staphylococcus aureus, Streptococcus epidermidis, MRSA, and Bacillus subtilis) and Gram-negative Klebsiella pneumoniae, whereas 4-nitroimidazole analogues (12a-m) were not effective against selected bacteria. The quantitative structure-activity relationship investigations were applied to find out the correlation between the experimentally evaluated activities with various parameters of the compounds studied. The QSAR models built in this work had reasonable predictive power and could be explained by the observed trends in activities.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::78b759972386e7d7b3c2dd1a55ff1dcd https://pubmed.ncbi.nlm.nih.gov/17919903 Zobrazit plný text záznamu Full Text from ScienceDirect