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简单节杆菌A1及耻垢杆菌MS1两种菌混合培养转化地塞米松中间体5α-△9(11)-16α-甲基-3μ,17μ,21-三羟基-孕甾烯-3μ,21-双醋酸酯-20酮(Ⅲ)可得到16α-甲基-△1.4.0(11)-孕甾烯-17α,21-双羟基-3,20双酮(Ⅳ)(65%收率)及少量的16α-甲基-△1.4孕甾烯-9α,11α-环氧-17α,21双羟基-3,20双酮(Ⅴ)。 相似文献
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用诺卡氏菌与节杆菌混合菌种转化从蕃麻皂素制得的中间体5α-△9(11)-16-16β-甲基-3β,17α,21三羟基孕甾烯-3β,21-双醋酸酯-20酮(Ⅰ)得50%的16β-甲基-△1,4,9(11)-孕甾三烯-20酮(Ⅱ)和少量的16β-甲基-9,11α环氧-△1,4孕甾二烯-20酮(Ⅲ)。另外,又用同样的混合菌种转化从剑麻皂素制得的中间体5α,17α甲基-17β羟基-雄甾-3酮(Ⅳ)得50%17α甲基-17β羟基-△1,4-雄甾二烯-3酮(Ⅴ)。如改变培养基则得3,17β-羟基-17α-甲基-9酮基-9,10开环-1,3,5(10)雄甾三烯化合物。 相似文献
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Synthesis of 35 new compounds of α-chloro-β-(5-nitro-2-furyl) acrylamides and 5-[α-chloro-β-(5-nitro-2-furyl ) vinyl]-oxadiazoles by known methods are reported. In preliminary test in mice 10 compounds were found to possess pronounced activity against Schistosomiasis japonica. Among these Ⅰ12, Ⅰ13, Ⅰ14, Ⅰ20, Ⅱ1 and Ⅱ8 were shown to be the most effective. 相似文献
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为了寻找心血管系统药物,以表雄酮为原料,合成了7个16,17位取代的目标化合物:2β-(4’-甲基-1’-哌嗪基)-3α-羟基-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α-羟基-16α-溴-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-氧-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-肟-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17β-氨基-5α-雄甾烷和2β—(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-16β-氨基-5α-雄甾烷。初步药理试验结果表明它们都有不同程度的抗心律失常活性。 相似文献
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Two forms of santonin exist in Artemisia cina Berg, i. e, α-and β-santonin. α-Santonin is therapeutically effective as an anthelmintic, while β-santonin is very weakly effective, so a method for the separation and determination of both forms is required. In the present paper, separation is made on silica gel-aluminum oxide G layer and determination is performed with a Shimadzu Chromatogram Scanner Model CS-900.Weigh accurately 0.20g of Artemisia powder (60 mesh) into a 50 ml Erlenmeyer flask, add 0.10g of Ca(OH)2 and 10.0 ml of water, then weigh the flask accurately. Boil the mixture for 10 minutes, cool, and weigh again, add more water to compensate the weight loss on boiling. Filter, apply the filtrate onto a silica gel-aluminum oxide G layer, develop with ethanol-conc, ammonia water (8:0.3), (Rf value: α-santonin 0.45,β-santonin 0.55). Scan the spot area of α-and β-santonin with a Shimadzu Chromatogram Scanner, Model CS-900, and calculate the weight with a calibration curve. Construct caliberation curves by plotting micrograms of standard α-and β-santonin vs. spot areas, two straight lines are obtained between 1~3μg, Instrument parameters are λ_s 270 nm, λ_R 400 nm, slit 10 mm, sensitivity x l, scan speed 40 mm/min, method of scanning: reflectance.The method is simple and rapid and is more sensitive than the elution method. The recovery of α-santonin is 95%. The method has been applied to the analysis of a number of different Artemisia samples. 相似文献
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慢性孵育β-淀粉样肽(25-35)对培养大鼠海马神经元外向钾电流的影响 总被引:4,自引:3,他引:1
目的 研究慢性孵育β-淀粉样肽(25-35) (β-AP25-35)对海马神经元上瞬时外向钾电流(IA)和延迟整流钾电流(IK)的影响。方法 在培养的大鼠海马神经元上用膜片钳全细胞记录钾通道电流。结果 β-AP25-35 3μmol·L-1 孵育细胞24h ,IK 电流幅度增加(44.3±5.4)% ,电流密度由(30.4±6.4)pA·PF-1 增加至(43.8±4.7)pA·PF-1 ;β-AP25-3510μmol·L-1 孵育12h ,IK 电流幅度增加(69.8±4.1) % ,电流密度增加至(51.6±7.9)pA·PF-1,呈浓度依赖性;β-AP25-35引起的IK 增加对TEA 5mmol·L-1 敏感;β-AP25-35上调IK 的作用主要发生在β-AP25-355用药后48h内。β-AP25-35对IA无显著性影响。结论 β-AP25-35选择性地增加海马神经元上IK,这一作用可能与β-AP的神经毒性有关 相似文献
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由5(及7)-[双-(β-羥乙基)-氨基]吲(口朶)-2-羧酸乙酯(Ⅶa,b)合成了5(及7)-[双-(β-氯乙基)-氨基]吲(口朶)-2-羧酸乙酯(Ⅱa和Ⅱb)、5(及7)-[双-(β-溴乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅱc和Ⅱd)以及5(及7)-[双-(β-碘乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅱe和Ⅱf)。再經水解制得其相应的羧酸(Ia-f)。此外又合成了5(及7)-乙氧羰氨基-吲(口朶)-2-羧酸乙酯(IXa,b)和5-乙氧基-7-[双-(β-氯乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅶ)。化合物Ia,Ib,Ic,Ⅱa,Ⅱb,Ⅱc,Ⅱe和Ⅱf对組織培养Hela細胞有明显的抑制作用。化合物Ⅰa,Ⅰb,Ⅱa和Ⅱb口服时对小鼠肉瘤180有明显的抑制作用。化合物Ⅰe,Ⅰf和Ⅻ对肉瘤180具有中度的抑制作用。 相似文献
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自16α,17α-环氧孕甾-4-烯-11α-醇-3,20-二酮(Ⅰ)經对甲苯磺酰化和消去反应得到16α,17α-坏氧孕甾-4,9(11)-二烯-3,20-二酮(Ⅱ),用氫溴酸打开环氧。氫解脫溴得到孕甾-4,9(11)-二烯-17α-醇-3,20-二酮(Ⅲ),引入C21-OAc得到孕甾-4,9(11)-二烯-17α,21-二醇-3,20-二酮21-醋酸脂(Ⅳ),然后按已知方法合成9α-氟-可的唑(Ⅵ).(Ⅵ)对(Ⅰ)的收率为17.4%理論。也进行了由(Ⅲ)先引入9β,11β-环氧,然后引入C21-OAc以合成9α-氟可的唑的試探。 相似文献
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Proteolysis of 14C-labeled globin, as well as the hydrolysis of the specific substrate benzoyl tyrosine ethyl ester, by purified bovine chymotrypsin was found to be inhibited by several steroid hormones. The inhibition of chymotrypsin by the steroids was of a competitive nature, with Ki values of 9.9 × 10?5 M for triamcinolone (9-fluoro-11β, 16α,17,21-tetrahydroxy-1,4-pregnadiene-3,20-dione), 1.6 × 10?4 M for cortisol (11β,17α,21-trihydroxypregn-4-ene-3,20-dione), 3.7 × 10?4 M for testosterone (17β-hydroxy-4-androsten-3-one), 5.0 × 10?4 M for dexamethasone (9-fluoro-11β,17,21-trihydroxy-16α-methyl-1,4-pregnadiene-3,20-dione), and 1.0 × 10?4 M for epicortisol (11α,17,21-trihydroxy-4-pregnene-3,20-dione). The activity of purified bovine trypsin on its specific substrate, TAME (tosyl arginine methyl ester), also showed a similar pattern of inhibition by steroids. Both chymotrypsin and trypsin were found to bind 3H-labeled dexamethasone and cortisol. This binding was markedly inhibited by the general protease inhibitor, PMSF (phenylmethanesulfonyl fluoride), whereas the chymotrypsin-specific inhibitor, TPCK (l-[1-tosyl-amido-2-phenyl]ethylchloromethyl ketone), inhibited only the steroid binding to chymotrypsin but not to trypsin. These observations indicate that serine proteases recognize steroid hormones in a fashion similar to the recognition of their specific substrates and that the steroids inhibit activity of these enzymes at their binding sites. 相似文献
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本文是说明用较短的新路线合成△1-16-次甲基-11-酮基-17α-羟基副腎皮酮(Ⅵ),即在化合物I中先引进C—11酮基(Ⅲ),再破断16α,17α-氧桥,加入21-乙酰氧基及在C-1脱氢,即得目的物Ⅵ。 相似文献
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7α-和7β-甲基-10β,17β-二乙酰氧基-△4-雌甾烯-3酮(简称7α-和7β-甲-乙氧雌酮)对小鼠抗早孕ED50分别为1.6和5.5 mg/kg。7α-甲-乙氧雌酮在大鼠也有抗早孕作用并使血浆孕酮浓度降低,应用10 μg/ml浓度能抑制离体妊娠大鼠卵巢孕酮合成。7α-和7β-甲-乙氧雌酮与兔子宫胞浆雌二醇受体的相对结合亲和力(RBA)分别为10.8和1.5,与孕酮受体的RBA均<1.7α-和7β-甲-乙氧雌酮都有较弱的雌激素和抗雌激素活性。 相似文献
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Yuan Tian Yang Hong Samuel J. Bonacorsi Aaron Balog Sharon Gong 《Journal of labelled compounds & radiopharmaceuticals》2014,57(1):1-11
For the first time, [3α‐3H] 17α‐hydroxy pregnenolone (1) was synthesized through a multiple step sequence. The presence of [3β‐3H] isomer in RP‐HPLC purified product was identified by tritium NMR. The [3β‐3H] isomer was then separated from [3α‐3H] 17α‐hydroxy pregnenolone with chiralPAK AD‐H column. [3α‐3H] pregnenolone (2) was synthesized from commercial available 5‐pregnen‐3,20‐dione in one step with an improved procedure. 相似文献