Grier N, Dybas R A, Strelitz R A, Witzel B E, Dulaney E L
J Pharm Sci. 1982 Mar;71(3):365-7. doi: 10.1002/jps.2600710329.
A series of 14 antibacterial N-[omega,omega'-bis(cycloalkyl, bicyclo[2.2.1]heptyl, and substituted phenyl)-sec-alkyl]-1,3-diamino-2-propanol dihydrochloride salts were synthesized as potential topical antiseptics and disinfectants. Four derivatives which were particularly effective against Pseudomonas aeruginosa encompassed the three diverse ring-type substituents and an 8-n-pentadecyl moiety. The calculated Hansch hydrophobic parameter (pi) for the N-substituents of the more efficient compounds were in the range 7.0--9.0 and correlated with minimal inhibitory activity as a parabola for all of the products under the assay conditions. The potencies against Gram-positive and other Gram-negative bacteria were comparable to benzalkonium chloride and chlorhexidine.
合成了一系列14种抗菌的N - [ω,ω'-双(环烷基、双环[2.2.1]庚基和取代苯基)-仲烷基]-1,3 -二氨基-2 -丙醇二盐酸盐,作为潜在的局部防腐剂和消毒剂。对铜绿假单胞菌特别有效的四种衍生物包含三种不同的环型取代基和一个8 -正十五烷基部分。在测定条件下,更有效化合物的N -取代基的计算汉施疏水参数(π)在7.0 - 9.0范围内,并且与所有产品的最小抑菌活性呈抛物线相关。对革兰氏阳性菌和其他革兰氏阴性菌的效力与苯扎氯铵和氯己定相当。