Ray S, Singh M M, Agarwal A K, Kamboj V P
Contraception. 1987 Mar;35(3):283-7. doi: 10.1016/0010-7824(87)90029-1.
A comparative study of relative binding affinity (RBA) for estradiol-17 beta-receptors, estrogenicity and antifertility activity of compounds 2,2-dimethyl-3-phenyl-4-p-(3-n-butylamino-2-hydroxypropyloxy-pheny l)- 7-methoxycoumarin 4, 2,2-dimethyl-3-phenyl-4-p-(3-n-butylamino-2-hydroxy-propyloxyphenyl++ +)-7-methoxy chromene 5 and trans-2,2-dimethyl-3-phenyl-4-p-(3-n-butylamino-2-hydroxypropyloxyphe nyl)- 7-methoxychroman 6 with the corresponding 4-p-(beta-pyrrolidinoethoxyphenyl) compounds 1-3, is reported. It has been found that the introduction of the novel 3-n-butylamino-2-hydroxypropyloxy moiety in place of the classical tert-beta-aminoethoxy group leads to enhancement of antifertility activity.
报道了化合物2,2-二甲基-3-苯基-4-p-(3-正丁基氨基-2-羟基丙氧基苯基)-7-甲氧基香豆素4、2,2-二甲基-3-苯基-4-p-(3-正丁基氨基-2-羟基丙氧基苯基++)-7-甲氧基色烯5和反式-2,2-二甲基-3-苯基-4-p-(3-正丁基氨基-2-羟基丙氧基苯基)-7-甲氧基色满6与相应的4-p-(β-吡咯烷基乙氧基苯基)化合物1-3的相对结合亲和力(RBA)、雌激素活性和抗生育活性的比较研究。已发现,用新型的3-正丁基氨基-2-羟基丙氧基部分取代经典的叔-β-氨基乙氧基会导致抗生育活性增强。