Scopus
🔓 Açık Erişim
Marginally designed new profen analogues have the potential to inhibit cyclooxygenase enzymes
Archiv der Pharmazie · Ocak 2015
Makale Bilgileri
DergiArchiv der Pharmazie
Yayın TarihiOcak 2015
Cilt / Sayfa348 · 55-61
Scopus ID2-s2.0-84920517024
Erişim🔓 Açık Erişim
Özet
The current structure-activity relationship of profens (i.e., 2-arylpropionic acid derivatives, a class of non-steroidal anti-inflammatory drugs) discusses the importance of α-monomethyl substitution on these compounds, since the activities obtained through their corresponding arylacetic acid derivatives (i.e., a-demethylated derivatives) or α,α-dimethyl-substituted compounds are less than what is observed for the parent profens. Unfortunately, this implies a generalization in structure-activity relationships of profens in such a way that a mono-(non-methyl)alkyl group or dialkyl substituent replaced at the a-position of a profen analogue results in abolished activity. Therefore, within this study, we aimed to question this generalization employing ibuprofen, flurbiprofen, and naproxen as model compounds. A series of α-(non-methyl)alkyl-substituted ibuprofen and flurbiprofen analogues as well as α,α-dialkylsubstituted ibuprofen, flurbiprofen, and naproxen derivatives were synthesized and screened for their potential to inhibit cyclooxygenase enzymes. In addition, since profens have negligible potential to inhibit lipoxygenase enzymes, the effect of such derivatization was also questioned in lipoxygenase inhibition assays. The findings only partially agreed with the current structure-activity approach of profens and the activity results of some compounds were found as beyond ordinary.
Yazarlar (8)
1
Hayrettin Ozan Gulcan
2
Serdar Ünlü
3
Anatoli Dimoglo
4
Yasemin Şahin
5
Ilker Esiringu
6
Tuba Erҫetin
7
Demet Öz
8
Mustafa Şahin
Anahtar Kelimeler
COX
LOX
Profens
α-Monosubstitution
α,α-Disubstitution
Kurumlar
Eastern Mediterranean University
Famagusta Turkey
Gebze Teknik Üniversitesi
Gebze Turkey
Nobel Drug Pharmaceutical R&D Center (Nobel-Ilac Ar-Ge Merkezi)
Duzce Turkey
Metrikler
4
Atıf
8
Yazar
5
Anahtar Kelime