A new entry to pyrazolo[4,3-e][1,4]diazepines. Facile synthesis of pyrazolo [4,3-e][1,4]diazepin-5,8-diones, 5,6,8-triones and pyrazolo[4,3-e]pyrrolo-[1,2-a][1,4]diazepin-5,10-diones

Abstract

A facile approach to pyrazolo [4,3-e][1,4]diazepin-5,8-diones and pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepin-5,10-diones is reported. Strategy involved the utility of α-amino acid as a three-atom segment in the construction of diazepine skeleton on the preformed pyrazole ring.

Combinatorial Library Synthesis and Biological Evaluation of Pyrazolo[4,3‐e][1,4]diazepine as a Potential Privileged Structure

“…[10] When diazepines fused to thiophenes, imidazoles, pyrazines, pyrroles and isoxazoles were tested, the general structure-activity relationship (SAR) patterns of benzodiazepinones were most similar to those of the pyrazolodiazepine series. [11] Although some pyrazolodiazepine derivatives have been synthesized, [12][13][14][15] the evaluation of diverse structural analogues against different target proteins is lacking. Herein, we report the combinatorial synthesis, biological evaluation and analysis of the pyrazolodiazepine skeleton to determine whether this core structure possesses the properties of a privileged structure, [16] applying the b-turn mimicking concept of tetrahydro-1,4-pyrazolodiazepin-8-one (3) [17,18] .…”