丹皮酚曼尼希碱衍生物的合成及抗血小板聚集活性

以丹皮酚和不同的有机胺为原料,利用曼尼希反应合成系列丹皮酚曼尼希碱衍生物,合成得到5个丹皮酚曼希尼碱衍生物.目标化合物的结构经过核磁共振氢谱(^(1)H NMR)和质谱(HR-MS)确证.采用Born比浊法,对5个目标化合物进行了以ADP为诱导剂的体外抗血小板聚集的活性试验;结果表明,目标化合物2a~2e(AIR:46.35%~85.39%)的活性均强于阳性对照药阿司匹林(AIR:35.08%),其中化合物2d(AIR:35.08%)的抗血小板聚集活性最强,具有进一步的研究价值.

Synthesis and Biological Activities of Some Mannich Bases of 5-(4-Hydroxyphenyl)-1,3,4-Oxadiazole-2-Thione

以对羟基苯甲酸乙酯为原料，经肼解、环化合成５（４羟基苯基）１，３，４二唑２硫酮，继而经Ｍａｎｎｉｃｈ反应合成了四种新曼尼希碱，其结构经红外光谱、核磁共振和元素分析证实。初步抑菌活性试验表明，显示弱的抑菌活性。

Synthesis and Biological Activity Study of New Schiff and Mannich Base Ligands Derived from Isatin and 3-Amino-1,2,4-triazole and Their Metal Complexes

Two new Mannich and Schiff base ligands namely： （1-（3＇-amino-methyl-1＇（H）-1＇,2＇,4＇-triazole）-3-（1＇（H）-l＇,2＇,4＇- triazole-3＇-yl） iminoisatin （Lt） and l-morpholinomethyl-3-（1＇（H）-1＇,2＇,4＇-triazolyl）iminoisatin （LII） were prepared from condensation reaction of the new Schiff base 3-（l＇（H）-l＇,2＇,4＇-triazole-3＇-yl）iminoisatin （SBH） （0.01 mol） with formaldehyde and 3-amino-l,2,4-triazole （3-At） or with formaldehyde and morpholine （0.01 mole each） respectively. Structures were characterized by tH NMR, CHN analyses, mass spectra and IR spectra. Metal complexes were synthesized by heating each ligand （0.02 mo with metal salts （0.01 moo in ethanol or ethanol： acetone mixture respectively. The formula of metal complexes were suggested depending on CHN and thermal analyses, metal and chloride contents, IR and UV-visible spectra, magnetic moments （laefr） and conductivity measurements. All complexes were of octahedral geometry except palladium （II） complexes which were square planar. The two ligands and some selected metal complexes showed various antibacterial and cytotoxic effects.