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异吲哚酮及其衍生物的生物活性。

Biological activities of isatin and its derivatives.

作者信息

Pandeya Surendra Nath, Smitha Sivakumar, Jyoti Mayank, Sridhar Seshaiah Krishnan

机构信息

Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221 005, India.

出版信息

Acta Pharm. 2005 Mar;55(1):27-46.

Abstract

Isatin is an endogenous compound identified in humans that possesses a wide range of biological activities. Isatin has anxiogenic, sedative, anticonvulsant activities and acts as a potent antagonist on atrial natriuretic peptide receptors in vitro. A series of p-substituted isatin semicarbazones have shown anticonvulsant activity in MES, scPTZ and scSTY tests. Various isatin-N-Mannich bases of isatin-3-thiosemicarbazones have shown antiviral and tuberculostatic activity. Methisazone is an effective compound against variola and vaccinia viruses. The N-dimethyl and morpholino derivative of 5-methyl isatin and trimethoprim exhibited an EC50 of more than 4.3 and 17.7 mg mL(-1), respectively. Isatin (3-o-nitrophenyl) hydrazone has shown activity against Walker carcinoma-256. Various substituted indolinones showed antitubercular activity against M. tuberculosis H37Rv with MIC ranging from 10-20 microg mL(-1). Isatin derivatives of Mannich bases had fibrinolytic, muscle relaxant, antiallergic, immunosuppressant, and antithrombotic activity. Isatin showed cardioinhibitory effect on frog heart, and hypotensive, respiratory depression and antidiuretic effects.

摘要

异吲哚酮是在人体中发现的一种内源性化合物,具有广泛的生物活性。异吲哚酮具有致焦虑、镇静、抗惊厥活性,并且在体外对心房利钠肽受体起强效拮抗剂的作用。一系列对-取代异吲哚酮缩氨基脲在最大电休克(MES)、皮下注射戊四氮(scPTZ)和皮下注射士的宁(scSTY)试验中显示出抗惊厥活性。异吲哚酮-3-硫代缩氨基脲的各种异吲哚酮-N-曼尼希碱已显示出抗病毒和抗结核活性。甲吲噻腙是一种抗天花病毒和牛痘病毒的有效化合物。5-甲基异吲哚酮的N-二甲基和吗啉代衍生物以及甲氧苄啶的半数有效浓度(EC50)分别大于4.3和17.7 mg/mL。异吲哚酮(3-邻硝基苯基)腙已显示出对沃克癌-256的活性。各种取代的吲哚啉酮对结核分枝杆菌H37Rv显示出抗结核活性,最低抑菌浓度(MIC)范围为10 - 20μg/mL。曼尼希碱的异吲哚酮衍生物具有纤溶、肌肉松弛、抗过敏、免疫抑制和抗血栓形成活性。异吲哚酮对蛙心显示出心脏抑制作用,以及降压、呼吸抑制和抗利尿作用。

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