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Discovery and Development of Laquinimod : An Immunomodulator for Treatment of Multiple Sclerosis

Wennerberg, Johan LU (2025) In ACS Symposium Series 1505. p.311-332
Abstract

Starting with the lead compound roquinimex, a selection of 3-quinolinecarboxamide derivatives were synthesized and evaluated for the treatment of the autoimmune disease multiple sclerosis. Structure-activity relationships were established in animal studies and from these, laquinimod was chosen as the drug candidate due to its superior potency and toxicological profile as compared to roquinimex. However, the medicinal chemistry route used the hazardous reagents phosgene and sodium hydride and the route suffered from a tedious work up as well as unreliable quality. A safe and practical process initiating from readily available 2-amino-6-chlorobenzoic acid is described.

Please use this url to cite or link to this publication:
author
organization
publishing date
type
Chapter in Book/Report/Conference proceeding
publication status
published
subject
host publication
Complete Accounts of Integrated Drug Discovery and Development : Recent Examples from the Pharmaceutical Industry - Recent Examples from the Pharmaceutical Industry
series title
ACS Symposium Series
editor
Pesti, Jaan A. ; Abdel-Magid, Ahmed F. and Vaidyanathan, Rajappa
volume
1505
pages
22 pages
publisher
The American Chemical Society (ACS)
external identifiers
  • scopus:105023367240
ISSN
0097-6156
1947-5918
ISBN
9780841296947
DOI
10.1021/bk-2025-1505.ch008
language
English
LU publication?
yes
id
e205742a-de1e-46e9-86e8-217fbc8f08ad
date added to LUP
2026-02-03 14:49:49
date last changed
2026-02-03 14:50:49
@inbook{e205742a-de1e-46e9-86e8-217fbc8f08ad,
  abstract     = {{<p>Starting with the lead compound roquinimex, a selection of 3-quinolinecarboxamide derivatives were synthesized and evaluated for the treatment of the autoimmune disease multiple sclerosis. Structure-activity relationships were established in animal studies and from these, laquinimod was chosen as the drug candidate due to its superior potency and toxicological profile as compared to roquinimex. However, the medicinal chemistry route used the hazardous reagents phosgene and sodium hydride and the route suffered from a tedious work up as well as unreliable quality. A safe and practical process initiating from readily available 2-amino-6-chlorobenzoic acid is described.</p>}},
  author       = {{Wennerberg, Johan}},
  booktitle    = {{Complete Accounts of Integrated Drug Discovery and Development : Recent Examples from the Pharmaceutical Industry}},
  editor       = {{Pesti, Jaan A. and Abdel-Magid, Ahmed F. and Vaidyanathan, Rajappa}},
  isbn         = {{9780841296947}},
  issn         = {{0097-6156}},
  language     = {{eng}},
  pages        = {{311--332}},
  publisher    = {{The American Chemical Society (ACS)}},
  series       = {{ACS Symposium Series}},
  title        = {{Discovery and Development of Laquinimod : An Immunomodulator for Treatment of Multiple Sclerosis}},
  url          = {{http://dx.doi.org/10.1021/bk-2025-1505.ch008}},
  doi          = {{10.1021/bk-2025-1505.ch008}},
  volume       = {{1505}},
  year         = {{2025}},
}