具有碳酸酐酶抑制和抗神经病理性疼痛活性的螺环磺酰胺类化合物。
Spirocyclic sulfonamides with carbonic anhydrase inhibitory and anti-neuropathic pain activity.
机构信息
Department of Chemistry, School of Technology, GITAM University, Hyderabad 502102, Telangana, India.
School of Chemical Sciences, SRTM University, Nanded 431606, Maharashtra, India.
出版信息
Bioorg Chem. 2019 Nov;92:103210. doi: 10.1016/j.bioorg.2019.103210. Epub 2019 Aug 17.
A novel series of 4-oxo-spirochromane bearing primary sulfonamide group were synthetized as Carbonic Anhydrase inhibitors (CAIs) and tested for their management of neuropathic pain. Indeed, CAs have been recently validated as novel therapeutic targets in neuropathic pain. All compounds, here reported, showed strong activity against hCA II and hCA VII with K values in the low or sub-nanomolar range. Two compounds (6d and 6l) showed good neuropathic pain attenuating effects and longer duration than drug reference acetazolamide in an animal model of oxaliplatin induced neuropathy.
一系列新型的 4-氧代螺色满酮类化合物被合成出来作为碳酸酐酶抑制剂（CAIs），并对其治疗神经性疼痛的效果进行了测试。事实上，碳酸酐酶最近被验证为神经性疼痛的新的治疗靶点。所有在此报道的化合物均对 hCA II 和 hCA VII 表现出很强的抑制活性，其 K 值处于低纳摩尔或亚纳摩尔范围。两种化合物（6d 和 6l）在奥沙利铂诱导的神经病变动物模型中显示出比药物对照乙酰唑胺更好的神经性疼痛缓解效果和更长的持续时间。
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