Amini, Mohsen’s team published research in Arzneimittel-Forschung in 2002 | 6136-93-2

Arzneimittel-Forschung published new progress about Calcium channel blockers. 6136-93-2 belongs to class nitriles-buliding-blocks, and the molecular formula is C6H11NO2, Name: 2,2-Diethoxyacetonitrile.

Amini, Mohsen; Golabchifar, Ali A.; Dehpour, Ahmad R.; Pirali, Hamedani M.; Shafiee, Abbas published the artcile< Synthesis and calcium channel antagonist activity of new 1,4-dihydropyridine derivatives containing dichloroimidazolyl substituents>, Name: 2,2-Diethoxyacetonitrile, the main research area is calcium channel antagonist dihydropyridine derivative structure design lipophilicity; cardiovascular calcium channel antagonist dihydropyridine structure design.

A group of dialkyl, dicycloalkyl and diaryl ester analogs of nifedipine (CAS 21829-25-4), in which the ortho-nitrophenyl group at position 4 is replaced by a 4,5-dichloroimidazolyl 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 sym. esters in alkyl esters series showed that increasing the length of the methylene chain in C3 and C5 ester substituents (from n = 0 to n = 2) increased the activity. When increasing of the length was accompanied by increase of the hindrance, the activity decreased. In the unsym. diester series, the results showed when R1 is a small substituent (R1 = Me), increasing of the lipophilic property in R2 substituent increases the activity if this high lipophilicity is not accompanied by steric hindrance. The results demonstrate that in the unsym. series, several compounds (benzyl Me, benzyl iso-Pr and cyclohexyl ethyl) had activity similar to that of the reference drug nifedipine. In sym. diesters compounds, the most active compound was the diphenethyl ester derivative being more active than nifedipine. These structure-activity data indicate that the 4-(4,5-dichloroimidazolyl) moiety is the bioisoester of 3-nitrophenyl and 2,3-dichlorophenyl moieties.

Arzneimittel-Forschung published new progress about Calcium channel blockers. 6136-93-2 belongs to class nitriles-buliding-blocks, and the molecular formula is C6H11NO2, Name: 2,2-Diethoxyacetonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts