130181-76-9Relevant academic research and scientific papers
Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases
De Luca, Laura,Mancuso, Francesca,Ferro, Stefania,Buemi, Maria Rosa,Angeli, Andrea,Del Prete, Sonia,Capasso, Clemente,Supuran, Claudiu T.,Gitto, Rosaria
, p. 276 - 282 (2018)
Coumarin derivatives are a peculiar class of inhibitors of the family of metalloenzymes carbonic anhydrases (CA, EC 4.2.1.1). Several coumarins display higher affinity and selectivity toward most relevant and druggable CA isoforms. By decorating the natur
KV1.3 INHIBITORS AND THEIR MEDICAL APPLICATION
-
Page/Page column 34; 48, (2016/10/04)
The present invention relates to a compound of the general formula (III) or a salt, solvate or prodrug thereof, as well as medical uses involving them, wherein (III) A1 is selected from the group consisting of N and C-R8; A2 is selected from the group consisting of N and C-R3; A3 is selected from the group consisting of N and C-R9; A4 and A5 and A6 are independently selected from the group consisting of N and C-R1; R1 is selected from the group consisting of hydrogen, (C1-C3)alkyl, halogen, (C1-C3)alkoxy and (C1-C3)haloalkyl; R2 is selected from the group consisting of hydrogen, halogen and (C1-C3)alkyl; R3 is selected from the group consisting of hydrogen, (C1-C3)alkyl, NR4R5, (C1-C3)alkyl- NR4R5 and cyano; wherein R4 and R5 are independently selected from the group consisting of hydrogen, (C3- C5)cycloalkyl, (C3-C5)heterocycloalkyl, (C1-C3)alkyl, or R4 and R5 together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring optionally comprising in addition to the aforementioned nitrogen atom a further heteroatom group selected from the group consisting of O and NR6, wherein R6 is selected from the group consisting of hydrogen, methyl, acetyl and formyl; Y is selected from the group consisting of O and S; R7 is selected from the group consisting of hydrogen, and (C1-C3)alkyl; R8 is selected from the group consisting of (C1-C4)alkyl, (C3-C5)cycloalkyl, and (C3- C5)heterocycloalkyl; R9 is selected from the group consisting of hydrogen, (C1-C3)alkyl, (C1-C3)alkoxy, and methods for producing such compounds.
