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小木蟲論壇-學術(shù)科研互動平臺 » 科研生活區(qū) » 專業(yè)外語 » 其他 » 中譯英翻譯
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laoshe5932銅蟲 (小有名氣)
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我們同時得到了4a 與4b異構(gòu)體，4a的異構(gòu)體SGLT-2的活性在200 nM以內(nèi)，而4b的異構(gòu)體SGLT-2的活性在300 nM以內(nèi)�？傮w而言這一系列的化合物活性均不理想，我們猜測可能是因為三元環(huán)張力較大，化合物結(jié)構(gòu)不穩(wěn)定，導(dǎo)致對酶的抑制效果降低，體外活性不夠理想�？紤]到環(huán)的張力對化合物結(jié)構(gòu)穩(wěn)定性的影響，我們嘗試合成環(huán)張力較小的四元環(huán)化合物，繼續(xù)考察其對體外SGLT-2酶抑制效果。 5a的羥基與5c羥甲基 易離去，使5a與5c形成碳正離子，在質(zhì)子溶劑中，可能發(fā)生碳正離子重排反應(yīng)，生成重排產(chǎn)物，這可能導(dǎo)致了其對SGLT-2酶沒有抑制效果。由構(gòu)效關(guān)系可以看出，羥基的存在對活性的影響，羥基化合物的活性明顯好于烷氧基化合物的活性，而單羥基的活性又好于多羥基的活性，且隨著碳原子的增加，單羥基化合物的對SGLT-2酶抑制效果也越來越弱。 |
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感謝參與，應(yīng)助指數(shù) +1
laoshe5932: 金幣+40, 謝謝！ 2015-12-21 08:49:42
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laoshe5932: 金幣+40, 謝謝！ 2015-12-21 08:49:42
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Both isomers of 4a and 4b were obtained and reactivity of that of 4a SGLT-2 was within 200 nM, while that of 4b was within 300 nM. In general, the reactivity of this series was not ideal and it was supposed to be the result of the highly strained three-membered ring which is responsible for the unstability of the compounds leading to deficiency in inhibiting enzyme and thus low reactivity in vitro. Taking the influence of ring strain on stability of the compounds into consideration, less strained four-membered rings were synthesized to observe its inhibition of SGLT-2 enzyme in vitro. It was easy for the elimination of the hydroxyl of 5a and the hydroxylmethyl of 5c to form carbocation. And carbocation is likely to undergo rearrangement in protic solvents, which may lead to the consequence of losing inhibition of enzyme SGLT-2. It could be concluded from the structure-activity relationship that how hydroxyl affects reactivity was that compounds with hydroxyl were significantly more reactive than those with alkyloxyl, compounds with monohydroxyl are better than those with multiple hydroxyls and inhibition of compounds with one hydroxyl on enzyme decreases along with the increase in the number of C atom. 你看下吧。有什么問題再說。 |
4樓2015-12-17 17:31:01
dyn_123
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laoshe5932: 金幣+20, ★有幫助, 謝謝您的翻譯 2015-12-21 08:50:31
感謝參與，應(yīng)助指數(shù) +1
laoshe5932: 金幣+20, ★有幫助, 謝謝您的翻譯 2015-12-21 08:50:31
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我試一下，不周之處望樓主多多包涵啦～ We got two different isomers namely 4a and 4b simultaneously. The activity of 4a in within 200nM, while 4b within 300nM. This kind of compounds, as a whole, didn't exhibit an ideal activity. And it probably resulted from the relatively strong strain tension of three-membered ring which leaded to the instability of the compounds and low inhibition effect on enzymes, thus demonstrating a bad activity in vitro. Taking the influence of the tension on the compound's stability into consideration, we tried to synthesize four-membered ring compounds which incorporated a relatively small tension in order to further check on the inhibition effect on SGLT-2 in vitro. The methyl group on 5a as well as the hydroxymethyl group on 5c are good leaving groups, giving rise to carbon cations. And in protonic solvent, the cations perhaps will rearrange to generate corresponding products, which may result in the failure to inhibit SGLT-2. It can be told that the existence of hydroxyl group exerted an impact no the activity in the light of SAR. Compounds with hydroxyl groups showed fat better activities than the ones without hydroxyl groups, while compounds with only one hydroxyl group showed better activities than the ones with more than one hydroxyl groups. In addition, as the number of carbon atoms increased, the inhibition effect of mono hydroxyl compounds on SGLT-2 got weaker and weaker. |
5樓2015-12-17 18:01:17
laoshe5932
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