CAS: 482-45-1; 4-((3-Methylbut-2-En-1-yl)Oxy)-7H-Furo[3,2-G]Chromen-7-One

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CAS号486-60-2 香柑醇； 5-羟基-6,7-呋喃并香豆素 | CAS号870-63-3 1-溴-3-甲基-2-丁烯 | CAS号484-20-8 佛手柑内酯 | CAS号486-60-2 香柑醇； 5-羟基-6,7-呋喃并香豆素 | CAS号737-52-0 氧化前胡素 | CAS号2643-85-8 水合氧化前胡素

佛手苷内酯置于三溴化硼,Potassium Carbonate体系中,用 二氯甲烷,丙酮 作为反应溶剂,化学反应 3.0H,反应生成 异欧前胡素
参考文献:呋喃香豆素单体作为cyp3A4抑制剂的设计,合成和评估.
标题:呋喃香豆素单体作为cyp3A4抑制剂的设计,合成和评估.
摘要:已发现从葡萄柚汁中分离出的许多呋喃香豆素在体外抑制cyp3A4的活性.在这项研究中,我们设计并合成了一系列基于佛手柑的类似物,以研究化学结构与cyp3A4活性抑制之间的关系.使用人肝微粒体和人肠道s9馏分进行了研究,其中睾丸激素为标记底物.除无活性的香豆素和酚醛呋喃香豆素衍生物外,发现烷氧基-呋喃香豆素类似物以剂量依赖性方式抑制cyp3A4活性,观测到的ic50值范围为0.13 +/-0.03至49.3 +/-1.9 Microm .发现不饱和呋喃衍生物表现出时间依赖性抑制,对6',7'的效力显示出2,4和14倍的增加 在预温育十分钟后,分别将-β-环氧香豆素,6',7'-二羟基香柠檬素和香柠檬素.呋喃部分的减少导致抑制力降低11倍,表明该官能团是这些化合物与cyp3A4之间相互作用的关键.
DOI:10.1039/b601096B

专利信息

专利号:US-2011236330-A1
优先权日:2008-12-09
标 题:Skin Whitening
发明人：MOUSSOU PHILIPPE; SABADOTTO MELANIE; RATHJENS ANDREAS
权利人:MOUSSOU PHILIPPE; SABADOTTO MELANIE; RATHJENS ANDREAS
摘要:Methods for reducing pigmentation or hyperpigmentation of skin comprising applying to the skin a substance of formula (I) in the D-form, L-form or racemic form (D,L) are disclosed: n n n n n n n n n n whereinn R 1 is selected from the group consisting of a hydrogen group (—H), a methyl group (—CH 3 ), an ethyl group (—CH 2 CH 3 ), a C3 alkyl group, a C4 alkyl group, an acetyl group (—C(O)CH 3 ), a propanoyl group (—C(O)CH 2 CH 3 ), an n-butanoyl group (—C(O)CH 2 CH 2 CH 3 ), and a 2-methyl-propanoyl group (—C(O)CH(CH 3 ) 2 ), R 2 is selected from the group consisting of a hydrogen group (—H), an ethyl group (CH 2 CH 3 ), a C3 alkyl group, a C4 alkyl group, an acetyl group (—C(O)CH 3 ), a propanoyl group (—C(O)CH 2 CH 3 ), an n-butanoyl group (—C(O)CH 2 CH 2 CH 3 ), and a 2-methyl-propanoyl group (—C(O)CH(CH 3 ) 2 ), R 3 is selected from the group consisting of a hydroxyl group (—OH), an amino group (NH 2 ), a methoxy group (OCH 3 ), an ethoxy group (—OCH 2 CH 3 ), a C3 alkoxy group, a C4 alkoxy group, and a benzyloxy group (—OCH 2 C 6 H 5 ), and X and Y are independently selected from the group consisting of a hydrogen group (—H), a methyl group (—CH 3 ), an ethyl group (—CH 2 CH 3 ), a C3 group alkyl, a C4 alkyl group, a halogen group, a methoxy group (—OCH 3 ), an ethoxy group (—OCH 2 CH 3 ), a C3 alkoxy group, a C4 alkoxy group, and a benzyloxy group (—OCH 2 C 6 H 5 ), provided that at least one of X and Y is not a hydrogen group (—H). nn Cosmetic compositions and/or topical compositions comprising the substance are useful for (i) lightening of the skin and/or (ii) whitening of the skin and/or (iii) reduction of pigmentation of the skin and/or (iv) reduction of hyperpigmentation of the skin and/or (v) inhibition of melanogenesis in the skin and/or (vi) prevention and/or retardation of signs of ageing and/or improving the skin appearance of an aged skin. Such composition are also useful for treatment of pigmentation or hyperpigmentation of the skin due to abnormal melanin synthesis and/or secretion.