Synthesis and some biological properties of 6-aminopenicillanic derivatives.
The properties of 33 6-aminopenicillanic derivates were described, the majority of which and particularly all 3,4-disubstituted phenyl derivatives, are new compounds. These derivatives were synthesized by three different methods consisting in treating of 6-aminopenicillanic acid (6-APA) with appropriate phenylthio -- and phenoxyalkanecarboxylic acids. The method consisting in use of aryloxyketenes is new and claimed by the patent applications. All synthesized compounds were screened for their biological activity against 21 different strains of pathogenic microorganisms of species: Staphylococcus, Sarcina, Streptococcus, Escherichia, Proteus, Klebsiella, Neisseria, Pseudomonas, Bacillus subtilis and Candida albicans. In the present paper only the most interesting results of microbiological tests and some data concerning pharmacological investigations performed on rats, were presented. Among selected compounds both substances 30 and 32 showed animals weight growth stimulating activity.
D000818:Animals; D001419:Bacteria / Q000187:drug effects; D001835:Body Weight / Q000187:drug effects; D007928:Lethal Dose 50; D008722:Methods; D008826:Microbial Sensitivity Tests; D010397:Penicillanic Acid / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats
D010397:Penicillanic Acid