Synthesis and screening of conformationally restricted and conformationally free N-(tertiary aminoalkyl)dithiocarbamic acids and esters as inhibitors of neuronal nitric oxide synthase.

Synthesis and screening of conformationally restricted and conformationally free N-(tertiary aminoalkyl)dithiocarbamic acids and esters as inhibitors of neuronal nitric oxide synthase.
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作为神经元一氧化氮合酶抑制剂的构象限制型和构象游离型 N-(叔氨基烷基)二硫代氨基甲酸和酯的合成和筛选。

DOI:
10.1016/s0968-0896(98)00132-1
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发表时间:
1998
影响因子:
3.5
通讯作者:
Eckelman,WC
Eckelman,WC
中科院分区:
医学3区
文献类型:
--
作者:
Sassaman,MB;Giovanelli,J;Sood,VK;Eckelman,WC

文献摘要

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N-(叔氨基烷基)二硫代氨基甲酸和酯的合成和评价其抑制神经元型一氧化氮合酶的能力。初步结果表明,这些化合物能够作用于L-精氨酸的结合位点,并且构象限制性酯可能具有涉及辅因子(6 R)-5,6,7,8-四氢-1-生物蝶呤的第二活性位点。
N-(Tertiary aminoalkyl)dithiocarbamic acids and esters were synthesized and evaluated for their ability to inhibit neuronal nitric oxide synthase. Preliminary results show these compounds are able to act at the binding site for l-arginine and the conformationally restricted esters may have a second site of activity involving the cofactor (6R)-5,6,7,8-tetrahydro-l-biopterin.