1161933-93-2

Upstream product

• 62-53-3 aniline 
• 89587-10-0 2,3,4,9-Tetrahydro-2-phenyl-1H-pyrido<3,4-b>indol-1-one 
• 6250-88-0 4,9-Dihydropyrano<3,4-b>indol-1(3H)-on 

Downstream Products

• 1161934-04-8 (2-phenyl-1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acid t-butyl ester 
• 1161933-11-4 (2-phenyl-1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acid 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of novel (1-thioxo-1,2,3,4- tetrahydro-β-carbolin-9-yl)acetic acids as selective inhibitors for AKR1B1

New substituted (1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acids were designed as the inhibitor of AKR1B1 based upon the structure of rhetsinine, a minor alkaloidal component of Evodia rutaecarpa, and twenty derivatives were synthesized and evaluated. The most active compound of the series was (2-benzyl-6-methoxy-1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl) acetic acid (7m), which showed comparable inhibitory activity for AKR1B1 (IC50 = 0.15 μM) with clinically used epalrestat (IC50 = 0.1 μM). In the view of activity and selectivity, the most potent compound was (2-benzyl-6-carboxy-1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acid (7t), which showed strong inhibitory effect (IC50 = 0.17 μM) and very high selectivity for AKR1B1 against AKR1A1 (311:1) and AKR1B10 (253:1) compared with epalrestat.

FUSED TRICYCLIC COMPOUND HAVING ALDOSE REDUCTASE INHIBITORY ACTIVITY

A fused tricyclic compound having aldose reductase inhibitory activity and shown by the following formula, wherein R1 independently represents 1 to 3 atoms or substituents selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, cycloalkyl, alkylene, or alkoxy group, and a protected or unprotected hydroxyl or carboxyl group, R2 represents a protected or unprotected carboxyl group, R3 independently represents 1 or 2 atoms or substituents selected from a hydrogen atom, a halogen atom, an oxo group, a substituted or unsubstituted alkyl or alkoxy group, and a protected or unprotected carboxyl group, A represents an alkylene group, and B represents an oxygen atom, a sulfur atom, or a group shown by the following formula, wherein R4 represents an alkyl or aryl group substituted with an aryl, cycloalkyl, or heterocyclic group, and X represents an oxygen atom or a sulfur atom.