Structure-activity relationship of minoxidil analogs as inhibitors of lysyl hydroxylase in cultured fibroblasts.
Structure-activity relationship of minoxidil analogs as inhibitors of lysyl hydroxylase in cultured fibroblasts.
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米诺地尔类似物作为培养成纤维细胞赖氨酰羟化酶抑制剂的构效关系。
DOI：
10.1016/0003-9861(92)90073-6
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发表时间：
1992
影响因子：
3.9
通讯作者：
Pinnell,SR
中科院分区：
文献类型：
--
作者：
Murad,S;Tennant,MC;Pinnell,SR
The structural features that confer upon minoxidil the ability to suppress lysyl hydroxylase activity in human skin fibroblasts were investigated. Substitution of the amino group in position 2 or 6 of the pyrimidine ring with a methyl group had no significant effect on the inhibitory activity of minoxidil, whereas substitution of both amino groups with methyl groups resulted in a complete loss of inhibitory activity. Together, these observations indicate that only one of the two amino groupsorthoto the nitroxide oxygen is essential for the enzyme-suppressing effect of minoxidil. Derivatives of minoxidil formed by hydroxylation at position 3 or 4 of the piperidine ring were as active as the parent compound in suppressing lysyl hydroxylase activity. However, replacement of the piperidinyl group in position 4 of the pyrimidine ring with a pyrrolidinyl, morpholinyl, orN-methylpiperazinyl group resulted in loss of inhibitory activity, demonstrating that the piperidinyl groupparato the nitroxide oxygen is essential for the enzyme-suppressing effect of minoxidil. Removing the nitroxide oxygen from position 1 of the pyrimidine ring resulted in a partial loss of the specificity of minoxidil for suppression of lysyl hydroxylase activity. The results indicate that distinct structural elements determine the enzyme-suppressing effect and the antihypertensive effect of minoxidil.
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米诺地尔抑制成纤维细胞增殖和赖氨酰羟化酶活性。
DOI：
--
发表时间：
1987
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Murad,S;Pinnell,SR
通讯作者：
Pinnell,SR
外用米诺地尔治疗早期男性型秃发。
DOI：
--
发表时间：
1985
期刊：
Journal of American Academy of Dermatology
影响因子：
--
作者：
Elise A. Olsen;Madeline S. Weiner;Elizabeth R. DeLong;S. R. Pinnell
通讯作者：
S. R. Pinnell
VI 型埃勒斯-当洛斯综合征成纤维细胞中各种类型胶原蛋白赖氨酰羟基化的比较。
DOI：
10.1016/s0174-173x(83)80030-2
发表时间：
1983
期刊：
Collagen and related research
影响因子：
--
作者：
Tajima,S;Murad,S;Pinnell,SR
通讯作者：
Pinnell,SR
米诺地尔被肝脏磺基转移酶硫酸化。
影响因子：
5.8
作者：
G. A. Johnson;K. Barsuhn;J. Mccall
通讯作者：
J. Mccall
米诺地尔的药理特性：一种新型降血压药。
影响因子：
3.5
作者：
D. Ducharme;W. Freyburger;B. E. Graham;R. Carlson
通讯作者：
R. Carlson