Diastereomeric 7-ureidoacetyl cephalosporins. II. 7beta [[[(Aminocarbonyl) amino]-2-thienylacetyl] amino]-7-methoxy-3-[[(1-methyl-1H-tetrazol-5-yl) thio] methyl]-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid

Autor:	J. E. Dolfini, H. E. Applegate, M. G. Young, Treuner Uwe D, Christopher M. Cimarusti, William A. Slusarchyk, W. H. Koster, M. A. Ondetti, Hermann Breuer
Rok vydání:	1978
Předmět:	Pharmacology Bacteria Hydrochloride Stereochemistry medicine.drug_class Cephalosporin Diastereomer Thio Microbial Sensitivity Tests law.invention Cephalosporins Acylation chemistry.chemical_compound chemistry law Yield (chemistry) Drug Discovery medicine Urea Antibacterial activity Walden inversion
Zdroj:	The Journal of antibiotics. 31(6)
ISSN:	0021-8820
Popis:	The synthesis and antibacterial activity in vitro of 7-methoxylated cephalosporins having a thienylureidoacetyl or a thienylglycyl C-7 side-chain are described. Acylation of 7 beta-amino-7-methoxycephems with a novel 2-aminooxazolone hydrochloride under neutral conditions gave the thienylureidoacetyl derivatives in good yield with retention of configuration. 7 beta-[[D-[(Aminocarbonyl)amino]-2-thienylacetyl]amino]-7-methoxy-3-[[(1-methyl-1H-tetrazol-5-yl)thio] methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt (SQ 14,359) was found to have a broad-spectrum of antibacterial activity in vitro, particularly against beta-lactamase-producing organisms.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b79b98830d9bf0ab08f57d7e07cc5b83 https://pubmed.ncbi.nlm.nih.gov/681237 Zobrazit plný text záznamu