ChemInform Abstract: (E)-4-(2-((3-(Indol-5-yl)-1-oxo-2-butenyl)amino)phenoxy)butyric Acid Derivatives: A New Class of Steroid 5α-Reductase Inhibitors in the Rat Prostate. Part 1.

ChemInform ◽  
2010 ◽  
Vol 26 (47) ◽  
pp. no-no
Author(s):  
T. KUMAZAWA ◽  
H. TAKAMI ◽  
N. KISHIBAYASHI ◽  
A. ISHII ◽  
Y. NAGAHARA ◽  
...  
Keyword(s):  
Butyric Acid ◽  
New Class ◽  
Reductase Inhibitors ◽  
Rat Prostate

(E)-4-{2-[[3-(Indol-5-yl)-1-oxo-2-butenyl]amino]phenoxy}butyric Acid Derivatives: A New Class of Steroid 5.alpha.-Reductase Inhibitors in the Rat Prostate. 1

1995 ◽  
Vol 38 (15) ◽  
pp. 2887-2892 ◽  
Author(s):  
Toshiaki Kumazawa ◽  
Hitoshi Takami ◽  
Nobuyuki Kishibayashi ◽  
Akio Ishii ◽  
Yoshitomo Nagahara ◽  
...  
Keyword(s):  
Butyric Acid ◽  
New Class ◽  
Reductase Inhibitors ◽  
Rat Prostate ◽  
5 Alpha Reductase Inhibitors

Steroidal A ring aryl carboxylic acids: a new class of steroid 5.alpha.-reductase inhibitors

1990 ◽  
Vol 33 (3) ◽  
pp. 937-942 ◽  
Author(s):  
Dennis A. Holt ◽  
Mark A. Levy ◽  
David L. Ladd ◽  
Hye Ja Oh ◽  
Jill M. Erb ◽  
...  
Keyword(s):  
Carboxylic Acids ◽  
New Class ◽  
Reductase Inhibitors ◽  
5 Alpha Reductase Inhibitors

ChemInform Abstract: Steroidal A Ring Aryl Carboxylic Acids: A New Class of Steroid 5α-Reductase Inhibitors.

ChemInform ◽  
1990 ◽  
Vol 21 (33) ◽  
Author(s):  
D. A. HOLT ◽  
M. A. LEVY ◽  
D. L. LADD ◽  
H.-J. OH ◽  
J. M. ERB ◽  
...  
Keyword(s):  
Carboxylic Acids ◽  
New Class ◽  
Reductase Inhibitors

ChemInform Abstract: Indole Derivatives as a New Class of Steroid 5α-Reductase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 28 (16) ◽  
pp. no-no
Author(s):  
H. TAKAMI ◽  
H. KOSHIMURA ◽  
N. KISHIBAYASHI ◽  
A. ISHII ◽  
H. NONAKA ◽  
...  
Keyword(s):  
Indole Derivatives ◽  
New Class ◽  
Reductase Inhibitors

scholarly journals Isatin Derivatives as a New Class of Aldose Reductase Inhibitors With Antioxidant Activity

2021 ◽  
Author(s):  
Wenchao Liu ◽  
Huan Chen ◽  
Xiaonan Zhang ◽  
Xin Zhang ◽  
Long Xu ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Acetic Acid ◽  
Aldose Reductase ◽  
Acid Group ◽  
Docking Studies ◽  
Side Chain ◽  
New Class ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Isatin Derivatives

Abstract In this work, isatin was employed as the scaffold to design aldose reductase inhibitors with antioxidant activity. Most of the isatin derivatives were proved to be excellent in the inhibition of aldose reductase (ALR2) with IC 50 values at submicromolar level, and (E)-2-(5-(4-methoxystyryl)-2,3-dioxoindolin-1-yl) acetic acid (9g) was identified as the most effective with an IC 50 value of 0.015 μM. Moreover, compounds 9a-h with styryl side chains at the C5 position of isatin showed potent antioxidant activity. Particularly, the phenolic compound 9h demonstrated similar antioxidant activity with the well-known antioxidant Trolox. Structure-activity relationship and molecular docking studies showed that the acetic acid group at N1 and C5 p-hydroxystyryl side chain were the key structures to increase the aldose reductase inhibitory activity and antioxidant activity.

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