Enalapril characterization

Conformational restriction has also been used to determine the bioactive conformation of enzyme-inhibitor systems for which no X-ray crystal structure is available. Thorsett et al. (49) synthesized conformationally restricted bicyclic lactam derivatives of the angiotensin converting enzyme (ACE)inhibitors enalapril (20) and enalaprilat (21) (Fig. 15.9) to characterize torsion angles in the bioactive conformation. Analog (22) was used to constrain the torsion angle psi (T ). Flynn et al. 

Ribbing s disease, which is characterized by multiple epiphyseal dystrophy. In a randomized, double-blind comparison of amlodipine (10 mg/day) and enalapril (20 mg/day) in 50 patients for 6 months, both drugs significantly reduced blood pressure, but amlodipine increased heart rate and plasma concentrations of noradrenaline and angiotensin II (7). These undesired effects make ACE inhibitors a better choice for prevention of cardiac dysfunction. 

For example, characterization of enalapril and pCD complex was performed by combining C CP/MAS with several sofid-state techniques [15]. These experiments leaded to the conclusion that the complex was a new solid amorphous form that was difierent from its precursors. Enalapril is used in hypertension treatment and sufiers d radation in the sohd state as a consequence of its interaction with the difierent excipients commonly used in tablet formulation, such as microcrystaUine cellulose, magnesium stearate and eudragit E. 

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