Friedrich Bossert

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Michael-addition of 3-aminocrotonic acid ester 7 to aralkylidene acetoacetic acid esters 6 is followed by ring closure to give novel 4-aryl-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylates 8 with non-identical ester functions. In the series of 3-nitrophenyl derivatives (8, Ar=3-nitrophenyl) the pharmacological activities (coronary vasodilation,(More)
In the series of 1,4-dihydro-2,6-dimethyl-4-nitrophenyl-pyridine-3,5-dicarboxylates the vasodilating action (increase of O2-saturation in the coronary sinus of the dog) is found to be dependent on the position of the nitro function (ortho and meta superior to para) and on the nature of the ester group. One representative, niludipin (BAY a 7168, No. 17;(More)
1. The effects on contractile activity of 2 series of nifedipine-derivatives were investigated in isolated, isotonically contracting cat papillary muscles. 2. For structure-activity studies the lipophilicity of all compounds was determined by means of reversed phase thin-layer chromatography. 3. Neither the ortho-NO2 group in a series of arylderivatives nor(More)
Replacement of the 2-alkyl group by amino in the structure of cardiovascular 4-aryl-2,6-dialkyl-1,4-dihydropyridine-3,5-dicarboxylates 1 is tolerated without loss of antihypertensive activity. The rules found for the substitution of the aromatic ring and the ester functions in 1 still hold for the novel 2-amino-1,4-dihydropyridines 6, 7 and 9 obtained by(More)
677 ( t 9 6 0 ) . [3] Benda, P., etal.: J. Neurosurg. 34, 310 ( 1 9 7 1 ) . [4] Schmidek, H. H., etal.: J. Neurosurg. 34, 335 ( t 9 7 t ) . [5] Ivankovic, S., Druckrey, H.: Z. Krebsforsch. 71, 320 ( 1 9 6 8 ) . [6j Kleihues, P., etal.: Verh. Dtseh. Ges. Path. 52. Tag., 372 ( t 9 6 8 ) . [7] Wechsler, W., et al.: Ann. N. Y. Acad. Sci. 159, 360 (t969). [8](More)
Key step of the synthesis of the calcium antagonistic cerebral vasodilator (+/-) isopropyl-2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate (Bay e 9736, nimodipine) (5) is the cyclizing Michael addition of 3 onto 4. A pharmacokinetic study with 14C-nimodipine in the rat revealed as major metabolites the dihydropyridines 6(More)
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