Document Detail


Safety and efficacy of new 3,6-diaryl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine analogues as potential phosphodiesterase-4 inhibitors in NIH-3T3 mouse fibroblastic cells.
MedLine Citation:
PMID:  21722319     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
A novel series of potential phosphodiesterase-4 (PDE-4) inhibitors, 6-(3-(cyclopentyloxy)-4-methoxyphenyl)-3-aryl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, were developed. Different concentrations of the synthesized compounds were tested on cultured NIH-3T3 cells in order to determine their safety and efficacy in NIH-3T3 mouse fibroblastic cells in comparison to rolipram, a selective PDE-4 inhibitor. The viability of cells was determined by (3-(4,5-dimethylthiazol-2-yl)-2,5-di-phenyltetrazoliumbromide (MTT) assay. The PDE inhibition rate was measured indirectly by determination of concentrations of extracellular cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) using enzyme-linked immunoassay technique. The results showed that, all tested compounds caused a marked increase in the concentration of cAMP, whereas the concentration of cGMP stayed approximately unchanged. The cytotoxic IC(50) of all synthesized compounds were approximately two folds greater than their required concentration for inhibition of PDE-4 (in term of elevation of cAMP) and thus these structures could be used to develop potent and safe inhibitors of PDE-4 enzyme.
Authors:
Maryam Baeeri; Alireza Foroumadi; Maryam Motamedi; Azadeh Yahya-Meymandi; Loghman Firoozpour; Seyed Nasser Ostad; Abbas Shafiee; Saeid Souzangarzadeh; Mohammad Abdollahi
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-7-1
Journal Detail:
Title:  Chemical biology & drug design     Volume:  -     ISSN:  1747-0285     ISO Abbreviation:  -     Publication Date:  2011 Jul 
Date Detail:
Created Date:  2011-7-4     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101262549     Medline TA:  Chem Biol Drug Des     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 John Wiley & Sons A/S.
Affiliation:
Faculty of Pharmacy, and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 1417614411, Iran Chemistry Department, Shahr-e-Rey Branch, Islamic Azad University, Tehran 18735-334, Iran Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.
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