74173-87-8Relevant articles and documents
Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors
Ichikawa, Masanori,Yokomizo, Aki,Itoh, Masao,Sugita, Kazuyuki,Usui, Hiroyuki,Shimizu, Hironari,Suzuki, Makoto,Terayama, Koji,Kanda, Akira
scheme or table, p. 1930 - 1949 (2011/05/03)
To obtain small and efficient squalene synthase inhibitors, a flexible 2-aminobenzhydrol open form structure was designed and showed potent inhibitory activity comparable to 4,1-benzoxazepin compounds. Further chemical modification led to the discovery of a novel template with a strong squalene synthase inhibitory activity, and its basic structure-activity relationship was revealed. The X-ray crystallographic data of compound 12 bound to the active site of squalene synthase provided an important insight into the binding mode of this alternative template that formed 11-membered ring conformations with an intramolecular hydrogen bond.
Synthesis of the antitumoural agent batracylin and related isoindolo[1,2-b]quinazolin-12(10H)-ones
Martínez-Viturro, Carlos M.,Domínguez, Domingo
, p. 1023 - 1026 (2008/02/04)
The synthesis of batracylin and related isoindolo[1,2-b]quinazolin-12-ones from easily accessible o-acylanilines is reported. The preparation of these tetracyclic compounds through a Mitsunobu reaction followed by spontaneous cyclodehydration shows the ability of this methodology to afford good yields of a wide variety of diversely 7, 8, 9, 10-substituted isoindoloquinazolinones in two steps.
2-[[2-Methyl-1-[2-benzoyl(or benzyl)phenyl]-1H-imidazol-5-yl]methyl]-1H-isoindole-1,3(2H)-diones
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, (2008/06/13)
A multistep process is presented for the preparation of imidazobenzodiazepines of the formula STR1 wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl. Also presented are novel intermediates utilized in the process. The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants. The end products are especially useful in intravenous compositions for use in preoperative anesthesia.