197236-49-0Relevant academic research and scientific papers
Synthesis and SAR studies of potent H+/K+-ATPase inhibitors of quinazolinone-Schiff's base analogues
Rakesh,Shantharam,Manukumar
, p. 1 - 8 (2016)
A series of quinazolinone derived Schiff base derivatives 7–36 were synthesized and characterized by analytical and spectroscopic techniques. The synthesized analogues were screened for their in vitro H+/K+-ATPase inhibition. Most of the compounds showed excellent activity, compared to that of omeprazole, a reference drug. In particular, hydroxy and methoxy derivatives 13–24 were the most active compounds possessing a significant increase for different substituents on the benzene ring thus, contributing positively to gastric H+/K+-ATPase inhibition. Preliminary structure-activity relationship revealed that the compounds 13–24 with electron donating moiety (OH, OCH3) were found to be excellent activity and compounds 9–12 and 25–36 with electron withdrawing moiety (Cl, F, NO2 and Br) were found to be least antiulcer agents.
Facile zeolite induced Fischer-indole synthesis: A new approach to bioactive natural product rutaecarpine
Mhaske, Santosh B.,Argade, Narshinha P.
, p. 3417 - 3420 (2007/10/03)
Starting from glutaric anhydride (5) we have demonstrated an elegant six-step practical synthesis of bioactive natural product rutaecarpine (1a) via o-amidoglutaranilic acid formation, esterification, chemoselective ester reduction, intramolecular dehydrative cyclizations, hydrazone formation and zeolite induced Fischer-indole synthesis with 53% overall yield. The conditions employed in the present synthesis are mild, efficient and general.
