Rheumatology: Current Research
Open Access

Synthesis and biological evaluation of (Z)-2-amino-4-benzylidene-1,3-oxathiolan-5-one derivatives as novel COX-1/2 and 5-LOX inhibitors

International Conference and Exhibition on Orthopedics & Rheumatology

August 13-15, 2012 Hilton Chicago/Northbrook, USA

Dongmei Zhao

Scientific Tracks Abstracts: Rheumatology & Orthopedics

Abstract :

Volume 2, Issue 3 - 67 Rheumatology ISSN: 2161-1149 Rheumatology, an open access journal Orthopedics & Rheumatology-2012 August 13-15, 2012 International Conference and Exhibition on Orthopedics & Rheumatology August 13-15, 2012 Hilton Chicago/Northbrook, USA R heumatoid arthritis (RA) is an inflammatory autoimmune disease characterized by chronic joint inflammation and articular manifestations, eventually leading to permanent disability without early therapeutic interventions. A number of biological treatments are available for rheumatoid arthritis. Nonsteroidal anti-inflammatory drugs (NSAIDs), one kind of most widely used medication in the world because of their high efficacy in pain remission and anti-inflammatory, are the most important drugs for treating RA. Darbufelone as a novel anti-infammatory drug which blocks the activity of both COX-2 and 5-LOX is currently being evaluated in Phase III clinical trials for the treatment of rheumatoid arthritis. Based on scaffold hopping strategy, a series of (Z)-2-amino-4-benzylidene-1,3-oxathiolan-5-one derivatives were designed using Darbufelone as the leading compound. Forty (Z)-2-amino-4-benzylidene-1,3-oxathiolan-5-one derivatives were sequentially obtained through a nine-step process from substituted-benzaldehyde. Twenty-two compounds displayed potent inhibitory activities against COX-2 and 5-LOX with IC50 in the range of 0.82~10.45 �?¼M

Biography :

Dongmei Zhao got her doctor degree in 2007 and was promoted to be professor and tutor of doctors at the same year in Shenyang Pharmaceutical University. She has undertaken several various scientific research projects at different levels. One of her research direction focuses on design, synthesis and activity evaluation of new Nonsteroidal antiinflammatory drugs( NSAIDs) Darbufelone and its derivatives. She has collaborated with pharmaceutical company over 5 years on the study of NSAIDs