We have developed novel orally active quinazoline analogues as inhibitors of AP-1 and NF- κB mediated transcriptional activation. Among the derivatives prepared, 1-[2-(2-thienyl) quinazolin-4-ylamino]-3-methyl-3-pyrroline-2, 5-dione (10) showed significant activity in an adjuvant-induced arthritis rat model by reducing the swelling by 65% in the non-injected foot. The synthesis, structure–activity relationship, and in vivo activity are described.
[Chandrika, P Mani; Yakaiah; Narsaiah; Sridhar; Venugopal; Rao, J Venkateshwara; Kumar, K Pranay; Murthy; Rao, A Raghu Ram Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2009 , vol. 48, # 6 p. 840 - 847]
[Storz, Thomas; Heid, Richard; Zeldis, Joseph; Hoagland, Steven M.; Rapisardi, Vito; Hollywood, Susan; Morton, George Organic Process Research and Development, 2011 , vol. 15, # 4 p. 918 - 924]