Immunomodulating action and structure-activity relationships of substituted phenylamides of 5-amino-3-methylisoxazole-4-carboxylic acid.

Abstract:

:A series of 5-amino-3-methylisoxazole-4-carboxylic acid amides has been prepared by condensation of 5-amino-3-methylisoxazole-4-carboxylic acid with ethyl chloroformate. The resulting mixed anhydride undergoes condensation with appropriate phenylamides to form the corresponding amides 6-16. The compounds obtained were evaluated for their immunological activities in cultures of human peripheral blood mononuclear cells (PMBC). We found that the activities of the compounds in the proliferation test and in the lipopolysaccharide (LPS)-induced cytokine production in PBMC cultures were differential. The stimulatory or inhibitory effects depended strongly on the origin and location of substituents in the phenyl ring which is described in the discussion and was supported by QSAR studies.

journal_name

Arch Pharm (Weinheim)

journal_title

Archiv der Pharmazie

authors

Ryng S,Zimecki M,Sonnenberg Z,Mokrosz MJ

doi

10.1002/(sici)1521-4184(19995)332:5<158::aid-ardp1

keywords:

subject

Has Abstract

pub_date

1999-05-01 00:00:00

pages

158-62

issue

5

eissn

0365-6233

issn

1521-4184

pii

10.1002/(SICI)1521-4184(19995)332:5<158::AID-ARDP1

journal_volume

332

pub_type

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