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我们同时得到了4a 与4b异构体，4a的异构体SGLT-2的活性在200 nM以内，而4b的异构体SGLT-2的活性在300 nM以内。总体而言这一系列的化合物活性均不理想，我们猜测可能是因为三元环张力较大，化合物结构不稳定，导致对酶的抑制效果降低，体外活性不够理想。考虑到环的张力对化合物结构稳定性的影响，我们尝试合成环张力较小的四元环化合物，继续考察其对体外SGLT-2酶抑制效果。 5a的羟基与5c羟甲基 易离去，使5a与5c形成碳正离子，在质子溶剂中，可能发生碳正离子重排反应，生成重排产物，这可能导致了其对SGLT-2酶没有抑制效果。由构效关系可以看出，羟基的存在对活性的影响，羟基化合物的活性明显好于烷氧基化合物的活性，而单羟基的活性又好于多羟基的活性，且随着碳原子的增加，单羟基化合物的对SGLT-2酶抑制效果也越来越弱。 |
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vivian-lave
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【答案】应助回帖
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laoshe5932: 金币+40, 谢谢！ 2015-12-21 08:49:42
感谢参与，应助指数 +1
laoshe5932: 金币+40, 谢谢！ 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。有什么问题再说。 |
4楼2015-12-17 17:31:01
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laoshe5932: 金币+20, ★有帮助, 谢谢您的翻译 2015-12-21 08:50:31
感谢参与，应助指数 +1
laoshe5932: 金币+20, ★有帮助, 谢谢您的翻译 2015-12-21 08:50:31
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我试一下，不周之处望楼主多多包涵啦～ 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楼2015-12-17 18:01:17
6楼2015-12-21 08:47:56
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