Synthesis, Antihypertensive Activity, and 3D-QSAR Studies of Some New p-Hydroxybenzohydrazide Derivatives
作者:Ritesh P. Bhole、Kishore P. Bhusari
DOI:10.1002/ardp.201000008
日期:2011.2
p‐Hydroxybenzohydrazide 2 on treatment with aromatic/aliphatic aldehyde followed by cyclization with carbon disulphide afforded compounds 4a–4n. Also, compound 2 by treatment of substituted isothiocyanate followed by the treatment of chloroacetic acid yields the corresponding compounds 6a–6i. All the test compounds were assayed for antihypertensive activity by non‐invasive blood pressure measurement
p-羟基苯甲酰肼 2 用芳香族/脂肪族醛处理,然后用二硫化碳环化得到化合物 4a-4n。同样,化合物2通过处理取代的异硫氰酸酯然后处理氯乙酸产生相应的化合物6a-6i。通过无创血压测量和有创血压测量方法测定所有测试化合物的抗高血压活性。测试化合物显示出显着的抗高血压活性。完整的化合物进行了 3D-QSAR 研究。通过PHASE程序进行3D-QSAR分析,获得了具有良好预测能力(r2 = 0.98,q2 = 0.74)的统计可靠模型。