Document Detail

Studies on topical antiinflammatory agents. II. Synthesis and vasoconstrictive activity of 21-substituted corticosteroids with sulfur-containing moieties.
MedLine Citation:
PMID:  2805160     Owner:  NLM     Status:  MEDLINE    
As part of the search for new topical antiinflammatory agents, various 21-substituted corticosteroids having sulfur-containing moieties were prepared and tested for vasoconstrictive activity in humans. A structure-activity relationship study revealed that substitution of the 21-hydroxy group with a lower alkyl-thio group enhanced the activity. The activities of the 21-methylthio (3Ad) and the 21-ethylthio (3Ae) compounds were more potent than that of 9 alpha-fluoro-11 beta,21-dihydroxy-16 beta-methyl-17 alpha-valeroyloxy-1,4- pregnadiene-3,20-dione (betamethasone 17-valerate, BV).
M Mitsukuchi; T Ikemoto; M Taguchi; S Higuchi; S Abe; H Yasui; K Hatayama; K Sota
Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Chemical & pharmaceutical bulletin     Volume:  37     ISSN:  0009-2363     ISO Abbreviation:  Chem. Pharm. Bull.     Publication Date:  1989 Jul 
Date Detail:
Created Date:  1989-12-12     Completed Date:  1989-12-12     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  0377775     Medline TA:  Chem Pharm Bull (Tokyo)     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  1795-801     Citation Subset:  IM    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Administration, Topical
Adrenal Cortex Hormones / chemical synthesis*,  pharmacology,  toxicity
Anti-Inflammatory Agents / chemical synthesis*,  pharmacology,  toxicity
Chemical Phenomena
Vasoconstriction / drug effects*
Reg. No./Substance:
0/Adrenal Cortex Hormones; 0/Anti-Inflammatory Agents; 0/Mutagens
Erratum In:
Chem Pharm Bull (Tokyo) 1989 Dec;37(12):3435

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

Previous Document:  Application of chemical P450 model systems to studies on drug metabolism. I. Phencyclidine: a multi-...
Next Document:  Antianoxic action and active constituents of evodiae fructus.