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源自噻唑和咪唑的药物,或含有氮-碳-硫或叔氨基的药物。通过紫外/可见光谱法预测继发性抗甲状腺活性。

Drugs derived from thiazole and imidazole or with nitrogen-carbon-sulphur or tertiary amino groups. Prediction of secondary antithyroid activity by UV/visible spectroscopy.

作者信息

Jambut-Absil A C, Buxeraud J, Claude J, Raby C

机构信息

Laboratory of Chemical Pharmacy, Faculty of Pharmacy, Limoges, France.

出版信息

Arzneimittelforschung. 1987 Jul;37(7):772-7.

PMID:2445359
Abstract

The chemical structure of various drugs suggests their potential interference with thyroid metabolism by complexing molecular iodine in the thyroid gland. Spectroscopic analysis shows that such compounds form charge-transfer complexes with iodine in a 1:1 stoichiometry. The values of formation constant Kc indicate strong donor-acceptor interactions. Biochemical and histological studies carried out on the rat demonstrated that a correlation exists between the Kc values and the antithyroid activity. A mechanism of action of these molecules on thyroid function is proposed. The potential antithyroid activity of such compounds can therefore be predicted from the Kc values.

摘要

各种药物的化学结构表明,它们可能通过与甲状腺中的分子碘络合来干扰甲状腺代谢。光谱分析表明,此类化合物与碘以1:1的化学计量比形成电荷转移络合物。形成常数Kc的值表明存在强烈的供体-受体相互作用。对大鼠进行的生化和组织学研究表明,Kc值与抗甲状腺活性之间存在相关性。提出了这些分子对甲状腺功能的作用机制。因此,可以根据Kc值预测此类化合物的潜在抗甲状腺活性。

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