Document Detail

Synthesis and oral antiallergic activity of carboxylic acids derived from imidazo[2,1-c][1,4]benzoxazines, imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles.
MedLine Citation:
PMID:  2897466     Owner:  NLM     Status:  MEDLINE    
4H-Imidazo[2,1-c][1,4]benzoxazine-2-carboxylic acid (3) was found to possess potent activity in the IgE-induced rat passive cutaneous anaphylaxis model which may be predictive of clinical antiallergic activity. Compared to disodium cromoglycate (DSCG, 1), 3 was less active following iv administration but unlike DSCG showed very significant oral activity. To explore the structural requirements for this activity, a range of tricyclic compounds was prepared and their activities were measured. Individual 2-carboxylic acids derived from imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles showed iv activities up to 10(3) times as potent as DSCG and many of them showed significant oral activity. From these, imidazo[1,2-a]quinoxaline-2-carboxylic acid 114 has been chosen for further development.
I R Ager; A C Barnes; G W Danswan; P W Hairsine; D P Kay; P D Kennewell; S S Matharu; P Miller; P Robson; D A Rowlands
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  31     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  1988 Jun 
Date Detail:
Created Date:  1988-06-30     Completed Date:  1988-06-30     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1098-115     Citation Subset:  IM    
Roussel Laboratories Ltd., Swindon, Wilts, United Kingdom.
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MeSH Terms
Carboxylic Acids / chemical synthesis
Cromolyn Sodium / pharmacology
Histamine H1 Antagonists / chemical synthesis*,  pharmacology
Hypersensitivity / drug therapy*
Imidazoles / chemical synthesis*
Oxazines / chemical synthesis
Passive Cutaneous Anaphylaxis / drug effects
Pyrroles / chemical synthesis*
Quinoxalines / chemical synthesis
Structure-Activity Relationship
Thiazoles / chemical synthesis
Reg. No./Substance:
0/Carboxylic Acids; 0/Histamine H1 Antagonists; 0/Imidazoles; 0/Oxazines; 0/Pyrroles; 0/Quinoxalines; 0/Thiazoles; 15826-37-6/Cromolyn Sodium; 76002-75-0/imidazo(1,2-a)quinoxaline-2-carboxylic acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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