Synthesis and Pharmacological Evaluation of (Nitrooxy)alkyl Apovincaminates

Article abstract of DOI:10.1021/jm00059a004

A series of (nitrooxy)alkyl apovincaminates has been synthesized and evaluated for their effects on vertebral and femoral blood flow.These derivatives were prepared from apovincaminic acid (4).In cerebral circulation, compound 5 (0.03-1.0 mg/kg iv) caused a dose-dependent increase in cerebral blood flow (CerBF) without affecting the blood pressure.It was more potent than vinpocetine (2).The structures of 2 and 5, determined by X-ray crystallography, showed differences in the electrostatic potential image and in the conformation of the ethyl group at the 16-position.