Nilvadipine

The methyl groups adjacent to the pyridine nitrogens can also be modified without changing calcium channel blocking activity. The most significant change involves replacement of methyl by a nitrile group. Hantsch type condensation of the nitrobenzaldehyde 43 with methyl acetoacetate and the vinyl amine 44 from isopropyl 3-cyano-3-ketopropionate leads directly to nilvadipine (45) [13]. 

C7H5NO3 99-61-6) see Bamidipine Benidipine Efonidipine hydrochloride ethanol lopanoic acid Lercanidipine hydrochloride Manidipine Nicardipine Nilvadipine Nimodipine Nitrendipine Rosoxacin nitrobenzene... 

Napoli et al. [286] found that the nifedipine treatment of stroke-prone spontaneously hypertensive rats (SPSHR) suppressed the plasma and LDL oxidation and the formation of oxidation-specific epitopes and increased the survival of rats independently of blood pressure modification. Their results suggest that the protective effects of calcium blockers of dihydro-pyridine-type on cerebral ischemia and stroke may, at least in part, depend on their antioxidant activity. In vivo antioxidant effect of nilvadipine on LDL oxidation has been studied in hypertensive patients with high risk of atherosclerosis [287], It was found that there was a significant decrease in the level of LDL cholesterol oxidation in patients after nilvadipine treatment. 

Nabazenil, 209 Naboctate, 209 Nafimidone, 90 Naflocort, 75 Nafoxidine, 65 Naftifme, 55 Nalmefene, 62 Naltrexone, 62 Napamezole, 87 Narcotic antagonist, 62 Nedocromil, 8 Nefazodone, 98 Neflumozide, 133 Netobimin, 36 Neuromuscular blocker, 69 Nifedipine, 106 Nilvadipine, 107 Nisoxetine, 30 Nitromifene, 65 Nizatidine, 95 Nomifensine, 146... 

The frontal analysis technique has been used for the determination of enantioselective binding constants of chiral drugs such as warfarin, verapamil, nilvadipine, and semotidil with proteins such as bovine serum albumin (BSA), human serum albumin (HSA), and plasma lipoproteins (45-51). 

NAL Mohamed, Y Kuroda, A Shibukawa, T Nakagawa, ST Elo Gizawy, HF Askal, ME El Kommos. Binding analysis of nilvadipine to plama lipoproteins by capillary electrophoresis-frontal analysis. J Pharm Biomed Anal 21 1037-1043, 1999. 

The product (15-2) from aldol condensation of meto-nitrobenzaldehyde with the dimethyl acetal from ethyl 4-formylacetoacetate (15-1) provides the starting material for a dihydropyridine in which one of the methyl groups is replaced by a nitrile. Reaction of (15-2) with the eneamine from isopropyl acetoacetate gives the corresponding dihydropyridine hydrolysis of the acetal function with aqueous acid affords the aldehyde (15-3). That function is then converted to its oxime (15-4) by reaction with hydroxylamine. Treatment of that intermediate with hot acetic acid leads the oxime to dehydrate to a nitrile. There is this obtained nilvadipine (15-5) [16]. 

HPLC In situ thermal (+)-Nilvadipine 4-VP/EDMA rac-Nilvadipine [176]... 

---