114772-19-9Relevant articles and documents
Synthesis and calcium channel blocker activity of alkyl 1,4-dihydro-2,6-dimethyl-4-nitrobenzyl thioimidazolyl-3,5-pyridinedicarboxylates
Zarghi,Faizi,Abdolahnejad,Fassihi
, p. 175 - 179 (2007/10/03)
New alkyl ester analogues of nifedipine, in which the orthonitrophenyl group of position 4 is replaced by 1-methyl 2-(p-nitrobenzyl)thio-5-imidazolyl substituent, were synthesized and evaluated as calcium-channel antagonists using the high K+ contraction of guinea-pig ileal longitudinal smooth muscle. The results for the symmetrical esters showed that increasing the length of methylen chain in C3 and C5 ester substituents decreased activity. When the presence of bulky lipophilic esters increased activity. In ztnsymmetrical diester series, the results showed when R1 is a small substituent (R1=Me), increasing of the lipophilic property in R2 substituent increased the activity if this high lipophilicity don't accompany with steric hinderance. Our results demonstrate that the most active compound was diphenyl ester derivative and it was almost seven times more active than the reference drug nifedipine.
Synthesis and calcium antagonist activity of new 1,4-dihydropyridines containing nitrobenzylimidazolyl substituent in ginea-pig ileal smooth muscle
Zarghi,Derakhshandeh,Roshanzamir,Jorjani,Rastegar,Varmazyari,Shafiee
, p. 15 - 20 (2007/10/03)
New alkyl ester analogues of nifedipine, in which the ortho-nitrophenyl group of position 4 is replaced by 1-(4-nitrobenzyl)-5-imidazolyl or 2-methylthio-1-(4-nitrobenzyl)-5-imidazolyl substituent, were synthesized and evaluated as calcium-channel antagonists using the electrically induced contraction of guinea-pig ileal longitudinal smooth muscle. Our results demonstrate that all compounds inhibited the contractile response of guinea-pig ileum to electrical stimulation and the IC50 value of the most potent compounds 6a and 6f were significantly lower than that of nifedipine. Therefore, they are more potent than nifedipine.
ANGIOTENSIN II RECEPTOR BLOCKING IMIDAZOLES
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, (2008/06/13)
Substituted imidazoles such as STR1 are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.