Design, synthesis and evaluation of novel diaryl pyrrolopyrimidine and pyrrolothiazine derivatives as inhibitors of tumor necrosis factor stimulated gene-14 (TSG-14) production

A novel series of pyrrolothiazines 2-4 and pyrrolopyrimidines 5-7 have been synthesized. The structures of these compounds were established by spectroscopic and element microanalytical data. The newly synthesized compounds were evaluated as inhibitors of TSG-14. The most effective results were obtai...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2014-05, Vol.78, p.419-424
Main Authors: Hilmy, Khalid M H, Soliman, Dalia H, Shahin, Esmat B A, El-Deeb, Hala S, El-Kousy, Salah M
Format: Article
Language:English
Subjects:
Animals
C-Reactive Protein - antagonists & inhibitors
C-Reactive Protein - biosynthesis
Dose-Response Relationship, Drug
Drug Design
Lipopolysaccharides - antagonists & inhibitors
Lipopolysaccharides - pharmacology
Male
Molecular Structure
Pyrimidines - administration & dosage
Pyrimidines - chemical synthesis
Pyrimidines - pharmacology
Pyrroles - administration & dosage
Pyrroles - chemical synthesis
Pyrroles - chemistry
Pyrroles - pharmacology
Rats
Serum Amyloid P-Component - antagonists & inhibitors
Serum Amyloid P-Component - biosynthesis
Structure-Activity Relationship
Thiazines - chemical synthesis
Thiazines - chemistry
Thiazines - pharmacology
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Summary:A novel series of pyrrolothiazines 2-4 and pyrrolopyrimidines 5-7 have been synthesized. The structures of these compounds were established by spectroscopic and element microanalytical data. The newly synthesized compounds were evaluated as inhibitors of TSG-14. The most effective results were obtained by the S-sec-butyl derivatives 6e (80%) and the N-ethyl derivatives 4e (70%).
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2014.03.068