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11.
为了改善2,2-二甲基四氢噻唑盐酸盐(DMTD)的理化性质及提高辐射防护效价。方法合成了DMTD和胱胺的各种有机酸盐,对9.03Gy60Coγ射线一次全身照射的小鼠,照前给药,评价它们的辐射防护效果。结果大部分化合物具有不同程度的防护效果,其中DMTD酒石酸盐250mg/kg,照前一小时腹腔注射,存活率比单独照射对照组提高40%;胱胺琥珀酸盐250mg/kg,照前15分钟腹腔注射,存活率净增加77.5%。结论胱胺琥珀酸盐的辐射防护效果显著,值得进一步研究 相似文献
12.
噻唑烷二酮类药物是目前治疗糖尿病的主要药物之一,该类药物可增强机体胰岛素敏感性,降低胰岛素抵抗,在降糖效果上与磺脲类和二甲双胍类相当,但对胰岛B细胞的保护性远远要好于磺脲类和二甲双胍类,而且对心血管有着良好的保护作用。噻唑烷二酮类药物最主要的副作用是水肿和皮下脂肪增多。 相似文献
13.
本文报道一系列含硫亚硝基脲衍生物的合成、光谱学特征及对小鼠白血病L1210的作用。这些化合物都是CNC-半胱胺的衍生物,包括二硫化合物、2-氯乙基氨甲酸酯衍生物以及与羰基化合物环合而成的2,2-二取代的CNC-四氢噻唑。CNC-半胱胺及其二硫化合物、CNC-胱胺甲酰叠氮均有良好的抗L1210的作用;相应的氨甲酸酯衍生物和四氢噻唑衍生物的作用不明显。值得注意的是,2-甲基-2-乙氧羰甲基-3-CNC-四氢噻唑(15b)是一个例外,它对L1210有显著的抑制作用。 相似文献
14.
Four series of 1 H-pyrazole derivatives have been synthesized. The first series was synthesized starting with the reaction of 3-(5-bromo-2-thienyl)-1-phenyl-1 H-pyrazole-4-carboxaldehyde 1 with L-serine, L-cysteine, or L-penicillamine, followed by N-protection using (Boc)(2)O to provide compounds 2. The latter compounds could be N-deprotected by 4N HCl/dioxane to afford the second series 3 or reacted with NH(4)OH in the presence of DCC/HOBt to give the corresponding amides 4 followed by N-deprotection giving rise to compounds 5. The newly synthesized compounds were evaluated for their anti-inflammatory-antimicrobial activities. In addition, the ulcerogenic and acute toxicity profiles were determined. Compound 5b (2RS, 4R)-2-[3-(5-bromo-2-thienyl)-1-phenyl-1H-pyrazol-4-yl]-5-methylthiazolidine-4-carboxamide, proved to be the most active anti-inflammatory-antimicrobial agent in the present study with a good safety margin and no ulcerogenic effect. 相似文献
15.
Two novel series of imidazo[2', 1':5, 1]-1, 2, 4-triazolo[4, 3-c]quinazolines bearing 5-thioxo-1, 2, 4-triazoles, 6a-f, and 4-oxothiazolidines, 7a-f, were synthesized from corresponding thiosemicarbazide derivatives, 5a-f. The stepwise methodology applied to the preparation of compounds 5a-f was initiated with reaction of the parent 3-amino-1, 2, 4-triazolo[4, 3-c]quinazolines, 2, with ethyl 2-chloroacetoacetate resulting in annelation of the imidazole ring to give esters, 3a-c. However, hydrazinolysis of these ester derivatives gave the corresponding acid hydrazides, 4a-c, which on reaction with the appropriate alkyl isothiocyanate yielded compounds 5a-f. In turn, compounds 5, were cyclized with potassium hydroxide or with ethyl bromoacetate to give the corresponding thioxotriazoles 6 and oxothiazolidines 7, respectively. All synthesized compounds were screened for their in vitro antibacterial activity against various Gram-positive and Gram-negative bacteria. Some test compounds were found to possess potent antibacterial activities. Compound, 7f, exhibited much higher potency than the reference standard ciprofloxacin, against both types of bacteria, particularly, Gram-positive organisms. 相似文献