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Potentially Biodynamic Tetraaza Macrocycles and theirManganese Complexes: Antiandrogen Antimicrobialand PDI Studies

机译:潜在的生物动力四方体大环及其锰配合物:抗雄激素抗微生物和PDI研究

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摘要

Fourteen to eighteen membered tetraazamacrocyclic ligands N4TTD1–N4TTD4 have been synthesized by the condensation of aliphatic diamines. H2N–(CH2)y–NH2 (y = 2 or 3) and dicarboxylic acids, HOOC-(CH2)x–COOH (x = 1 or 2) in the presence of condensing reagents dicyclohexylcarbodiimide (DCHC) and 4-dimethylaminopyridine (DMAP). On reduction these macrocyclic ligands give N4TTD5-N4TTD8, which form complexes with manganese(II) acetate. The new products with octahedral geometry have been characterized by elemental analyses, molecular weight determinations, magnetic moment and spectral studies viz., infrared, electronic, mass and X-ray. On the basis of the spectral studies the binding sites are proposed as the nitrogen atom of the macrocycles. The formulation of the complexes as [Mn(CH3COO)2(N4TTDn)] (where n = 1 - 8) has been established on the basis of chemical composition. To assess the growth inhibiting potential of the ligands and their manganese (II) complexes biological screening have been undertaken. The testicular morphology, testicular sperm density, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trials and biochemical parameters of reproductive organs with ligands and their corresponding complexes, in vivo have also been described in the this communication.
机译:通过脂肪族二胺的缩合反应合成了十四至十八元四氮杂大环配体N4TTD 1 –N4TTD 4 。 H2N–(CH2)y–NH2(y = 2或3)和二羧酸,HOOC-(CH2)x–COOH(x = 1或2)在存在缩合试剂二环己基碳二亚胺(DCHC)和4-二甲基氨基吡啶(DMAP)的情况下)。在还原时,这些大环配体得到N4TTD 5 -N4TTD 8 ,其与乙酸锰(II)形成配合物。具有八面体几何形状的新产品的特征在于元素分析,分子量测定,磁矩和光谱研究,即红外,电子,质量和X射线。在光谱研究的基础上,结合位点被提议为大环的氮原子。根据化学组成确定了配合物的形式为[Mn(CH3COO)2(N4TTD n )](其中n = 1-8)。为评估配体及其锰(II)配合物的生长抑制潜力,已进行了生物学筛选。体内的睾丸形态,睾丸精子密度,精子运动力,附睾附睾精子密度和生育能力以及配体及其相应复合物的生殖器官的生化参数在体内也已有描述。

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