10H-Phenothiazines: a new class of enzyme inhibitors for inflammatory diseases.
The phenothiazine nucleus is known for their inhibitory activity towards the regulatory enzymes that are contributing to diseases such as asthma, autoimmune diseases including allergic rheumatoid and encephalomyelitis. In this study a number of substituted phenothiazines were synthesized and screened for their biological activity against the regulatory enzymes involved in inflammatory diseases. Our results show that the newly synthesized compounds 4a-c and 5a-c exhibited promising target specific enzyme inhibition against phosphodiesterase, prostaglandin dehydrogenase and superoxide dismutase activity depending on steric factors of the molecules.
Sadanandam
Y S
YS
Organic Chemistry Division, Indian Institute of Chemical Technology, Taranaka, Hyderabad 500 007, Andhra Pradesh, India.
Shetty
Meera M
MM
Rao
A Bhaskar
AB
Rambabu
Y
Y
D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001249:Asthma / Q000188:drug therapy; D001327:Autoimmune Diseases / Q000188:drug therapy; D004791:Enzyme Inhibitors; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000201:enzymology; D010640:Phenothiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D010726:Phosphodiesterase Inhibitors; D013329:Structure-Activity Relationship; D013482:Superoxide Dismutase / Q000037:antagonists & inhibitors
D000893:Anti-Inflammatory Agents; D004791:Enzyme Inhibitors; D010640:Phenothiazines; D010726:Phosphodiesterase Inhibitors; D013482:Superoxide Dismutase