Literature DB >> 10371028

Pyrrolo[3,2-c]quinoline derivatives: a new class of kynurenine-3-hydroxylase inhibitors.

F Heidempergher1, P Pevarello, A Pillan, V Pinciroli, A Della Torre, C Speciale, M Marconi, M Cini, S Toma, F Greco, M Varasi.   

Abstract

A series of pyrrolo[3,2-c]quinoline derivatives were synthesised and evaluated as inhibitors of selected enzymes of the kynurenine pathway. 7-Chloro-3-methyl-1H-pyrrolo[3,2-c]quinoline-4-carboxylic acid (7a) was found to be a relatively potent and selective inhibitor of kynurenine-3-hydroxylase (KYN-3-OHase). A molecular modelling study showed a good superimposition of 7a with PNU-156561 and kynurenine the natural substrate of KYN-3-OHase.

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Year:  1999        PMID: 10371028     DOI: 10.1016/s0014-827x(99)00009-9

Source DB:  PubMed          Journal:  Farmaco        ISSN: 0014-827X


  2 in total

Review 1.  Major Developments in the Design of Inhibitors along the Kynurenine Pathway.

Authors:  Kelly R Jacobs; Gloria Castellano-Gonzalez; Gilles J Guillemin; David B Lovejoy
Journal:  Curr Med Chem       Date:  2017       Impact factor: 4.530

2.  Copper(II)-Catalyzed (3+2) Cycloaddition of 2H-Azirines to Six-Membered Cyclic Enols as a Route to Pyrrolo[3,2-c]quinolone, Chromeno[3,4-b]pyrrole, and Naphtho[1,8-ef]indole Scaffolds.

Authors:  Pavel A Sakharov; Nikolai V Rostovskii; Alexander F Khlebnikov; Mikhail S Novikov
Journal:  Molecules       Date:  2022-09-02       Impact factor: 4.927

  2 in total

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