Synthesis and smooth muscle calcium channel antagonist effect of alkyl. aminoalkyl 1,4 - dihydro - 2,6 - dimethyl - 4 - nitro imidazole - 3,5 pyridine dicarboxylates.
DARU-Journal of Faculty of Pharmacy Tehran University of Medical Sciences. 2001; 9 (3-4): 40-5
in English
| IMEMR
| ID: emr-56607
ABSTRACT
The discovery that 1,4-dihydropyridine [DHP] class of calcium channel antagonist inhibits the Ca+° influx represented a major therapeutic advance in the treatment of cardiovascular diseases such as hypertension, angina pectoris and other spastic smooth muscle disorders. A novel class of calcium channel antagonist of flunarizine containing arylpiperazinyl moiety has recently been reported. It was therefore of interest to determine the effect that selected C-3 substituents contained amino alkyl and arylpiperazine, in conjunction with a C-4 1-methyl-5-nitro-2-imidazolyl substituents on calcium channel antagonist activity. The unsymmetrical analogues were prepared by a procedure reported by Meyer in which 1-methyl-5-nitro-imidazol-2-carboxaldehyde was reacted with acetoacetic esters and alkyl 3-aminocrotonate. In vitro calcium channel antagonist activities were determined by the use of high K+ contraction of guinea pig ileal longitudinal smooth muscle. All compounds exhibited comparable calcium channel antagonist activity [IC50=10[-9] to 10[-11] M] against reference drug nifedipine [IC50=2.75 +/- 0.36 x 10[-10] M]
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Index:
IMEMR (Eastern Mediterranean)
Main subject:
Piperazines
/
Dihydropyridines
/
Calcium Channel Blockers
/
Nifedipine
/
Nitroimidazoles
Language:
English
Journal:
J. Fac. Pharm. Tehran Univ. Med. Sci.
Year:
2001
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