Department of Pharmaceutical Chemistry, Hamdard University, New Delhi, India.
Arch Pharm (Weinheim). 2010 Nov;343(11-12):657-63. doi: 10.1002/ardp.201000098.
A series of (Z)-2-(substituted aryl)-N-(3-oxo-4-(substituted carbamothioyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl) hydrazine carboxamides (6a-r) was synthesized using 2-amino-5-nitrophenol as a starting material. All the synthesized compounds possessed two hydrogen-bonding domains and their effect on the activity was studied thereof. The anticonvulsant activity was assessed by the maximal electroshock test (MES), subcutaneous pentylenetetrazole test (scPTZ) and intraperitoneal thiosemicarbazide test (ipTSC). Compounds (6b, 6h, 6i, and 6p) were found to be the most potent of the series as they showed 83-100% protection in the MES test. They also displayed considerable activity in the chemically induced seizure tests. Most of the tested compounds were devoid of the neurotoxic and hepatotoxic effects.
使用 2-氨基-5-硝基苯酚作为起始原料，合成了一系列（Z）-2-（取代芳基）-N-（3-氧代-4-（取代氨甲酰硫基）-3,4-二氢-2H-苯并[b][1,4]恶嗪-7-基）肼甲酰胺（6a-r）。所有合成的化合物都具有两个氢键结合域，并研究了其对活性的影响。通过最大电休克试验（MES）、皮下戊四氮试验（scPTZ）和腹腔硫代卡巴肼试验（ipTSC）评估抗惊厥活性。发现化合物（6b、6h、6i 和 6p）是该系列中最有效的化合物，它们在 MES 试验中显示出 83-100%的保护作用。它们在化学诱导的惊厥试验中也表现出相当的活性。大多数测试化合物没有神经毒性和肝毒性作用。
