Zukowski E, Eckstein Z
Pol J Pharmacol Pharm. 1977 Jan-Feb;29(1):39-47.
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.
描述了33种6-氨基青霉烷衍生物的性质，其中大多数，特别是所有3,4-二取代苯基衍生物，都是新化合物。这些衍生物通过三种不同方法合成，包括用适当的苯硫基和苯氧基链烷羧酸处理6-氨基青霉烷酸（6-APA）。使用芳氧基烯酮的方法是新的，并已申请专利。对所有合成化合物针对21种不同致病微生物菌株进行了生物活性筛选，这些菌株包括葡萄球菌、八叠球菌、链球菌、大肠杆菌、变形杆菌、克雷伯菌、奈瑟菌、假单胞菌、枯草芽孢杆菌和白色念珠菌。在本文中，仅呈现了微生物测试中最有趣的结果以及对大鼠进行的药理学研究的一些数据。在所选化合物中，物质30和32均显示出促进动物体重增长的活性。
