4-(苯并咪(噻)唑2-)苯甲脒类化合物的合成及其一氧化氮合酶抑制活性

Synthesis and NOS Inhibitory Activity of 4-(Benzimidazole(or Benzoth iazole)-2-yl)-Benzamidine Compounds

目的 :寻找抑制一氧化氮合酶 (NOS)并对相关疾病具有较好治疗作用的化合物。方法 :以苯甲脒为基本母核 ,在苯环的对位引入 2 苯并咪 (噻 )唑基 ,然后在脒基N上引入环状或非环状的取代基 ,并测定目标化合物的诱生型NOS(iNOS)抑制活性。结果和结论 :合成了 4 (苯并咪 (噻 )唑 2 )苯甲脒类化合物 12个 ,其结构经IR、1 HNMR、MS和元素分析确证。初步的药理试验表明目标化合物具有不同程度的iNOS抑制活性 ,神经型NOS(nNOS)

AIM:To search for novel potent compounds with NOS inhibitory activity for the treatment of the related diseases METHOD:2-be nzimidazole or 2 -benzothiazole groups were introduced into the p-position of benzamidine,the n t he H on the amidines was substituted by alkyl,and the iNOS inhibitory activity of the target compounds were measured RESULT AND CONCLUSION:Seven 4-(benzimidazo le-2-yl)-benzamidine compounds(Ⅰ-1～7) and five 4-(benzothiazole-2 -yl)-benzami dine compounds(Ⅰ-8～12) were synthesized,and their structures were confir med b y 1HNMR,MS,IR spectra and elementary analysis The results of preli minary ph armacological test showed that the compounds had iNOS inhibitory activity,and t he test of nNOS inhibitory activity is under way