Discovery and development of gliflozins/ja: Difference between revisions
Discovery and development of gliflozins/ja
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Created page with "Gliflozins " Tags: Mobile edit Mobile web edit |
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[[File:Mynd fyrir toflu1.png]] | [[File:Mynd fyrir toflu1.png]] | ||
{| class="wikitable" | {| class="wikitable" | ||
|- | |- | ||
! R !! IC<sub>50</sub> (nM) !! | ! R !! IC<sub>50</sub> (nM) !! 活性 | ||
|- | |- | ||
|align="center"| [[File:Bygging 1.png]] ||align="center"| 0.720 ||align="center"| '' | |align="center"| [[File:Bygging 1.png]] ||align="center"| 0.720 ||align="center"| ''試験管内''活性が向上* | ||
|- | |- | ||
|align="center"| [[File:Bygging 2.png]] ||align="center"| 1.14 ||align="center"| '' | |align="center"| [[File:Bygging 2.png]] ||align="center"| 1.14 ||align="center"| ''試験管内''活性が向上* | ||
|- | |- | ||
|align="center"| [[File:Bygging 3.png]] ||align="center"| 13.3 ||align="center"| | |align="center"| [[File:Bygging 3.png]] ||align="center"| 13.3 ||align="center"| 炭素数が増えるにつれて、IC-50値は変動 | ||
|- | |- | ||
|align="center"| [[File:1-Methoxy-n-butane.png]] ||align="center"| 19.6 ||align="center"| '' | |align="center"| [[File:1-Methoxy-n-butane.png]] ||align="center"| 19.6 ||align="center"| ''試験管内''での''活性が低下* | ||
|- | |- | ||
|align="center"| [[File:Bygging 5.png]] ||align="center"| 21.2 ||align="center"| '' | |align="center"| [[File:Bygging 5.png]] ||align="center"| 21.2 ||align="center"| ''試験管内''での''活性が低下* | ||
|} | |} | ||
''* | ''*エチル基との比較対象 (IC<sub>50</sub> = 16,7)'' | ||
表2において、''試験管内''活性は、近位フェニル環(X)のC-4領域の化合物によって変化する。C-4位に小さなメチル基や他のハロゲン原子があると、IC<sub>50</sub>は0.72-36.7の範囲になった(2-フリルを持つフェニルが環の位置にあることを考慮)。 | |||
'''表2:'''近位フェニル環のC-4領域にどの化合物があるかによる'''試験管内'''活性の違い。 | |||
''' | |||
[[File:Mynd fyrir toflu2.png]] | [[File:Mynd fyrir toflu2.png]] | ||
{| class="wikitable" | {| class="wikitable" | ||
|- | |- | ||
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|align="center"| CN ||align="center"| 36.7 | |align="center"| CN ||align="center"| 36.7 | ||
|} | |} | ||
'''表3:'''チアゾール環の関わり方によるIC<sub>50</sub>値の違い(他の構造は何も変えていない(X = Cl, R = フェニルと2-フリル)。 | |||
''' | |||
{| class="wikitable" | {| class="wikitable" | ||
|- | |- | ||
! | ! 化合物 !! IC<sub>50</sub> (nM) | ||
|- | |- | ||
|align="center"| [[File:Mynd fyrir toflu3-1.png]] ||align="center"| 0.720 | |align="center"| [[File:Mynd fyrir toflu3-1.png]] ||align="center"| 0.720 | ||
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|align="center"| [[File:Mynd fyrir toflu3-2.png]] ||align="center"| 1.11 | |align="center"| [[File:Mynd fyrir toflu3-2.png]] ||align="center"| 1.11 | ||
|} | |} | ||
== こちらも参照 == | |||
* [[Sodium-glucose transport proteins/ja]] | |||
* [[Sodium-glucose transport proteins]] | * [[SLC5A2/ja]] | ||
* [[SLC5A2]] | * [[SGLT1/ja]] | ||
* [[SGLT1]] | * [[SGLT2/ja]] | ||
* [[SGLT2]] | * [[Dapagliflozin/ja]] | ||
* [[Dapagliflozin]] | * [[Empagliflozin/ja]] | ||
* [[Empagliflozin]] | * [[Canagliflozin/ja]] | ||
* [[Canagliflozin]] | * [[Ipragliflozin/ja]] | ||
* [[Ipragliflozin]] | |||
{{Drug design/ja}} | |||
{{Drug design}} | |||
[[Category:Drug discovery|Gliflozins]] | [[Category:Drug discovery|Gliflozins]] | ||
[[Category:SGLT2 inhibitors| ]] | [[Category:SGLT2 inhibitors| ]] | ||