75229-66-2Relevant academic research and scientific papers
Synthesis and comparative pharmacological studies of 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylates with non-identical ester functions
Meyer,Bossert,Wehinger,Stoepel,Vater
, p. 407 - 409 (2007/10/02)
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, anti-hypertensive activity) of the asymmetrically substituted derivatives are shown to be superior to those of the corresponding symmetrically substituted derivatives in many cases. One representative of this class 3-ethyl-5-methyl-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedica rboxylate (nitrendipine, Bay e 5009, No. 3) was selected for further development as an antihypertensive drug.
Sila-Drugs, 16th Communication. Sila-Analogues of Nifedipine-Like Dialkyl 4-Aryl-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylates, I
Tacke, R.,Bentlage, A.,Towart, R.,Meyer, H.,Bossert, F.,et al.
, p. 494 - 501 (2007/10/02)
The nifedipine-like 1,4-dihydropyridines 10a and 11a as well as their sila-analogues 10b, 10c, and 11b were synthesized for the first time. 10a, 10b, 10c, 11a, 11b, and their precursors 8a, 8b, 9a, and 9b were characterized by their physical and chemical properties, and their structures confirmed by analyses, 1H NMR and mass spectroscopy.The antispasmodic, vasodilating, and antihypertensive properties of 10a, 10b, 10c, 11a, and 11b were compared. - Keywords: Sila-analogues of Nifedipine Derivatives, Syntheses, Pharmacological Activity
