Synthesis of novel 2-[2-(substituted amino)phenethyl]-1 H-benzimidazoles; 3,4-dihydro and 1,2,3,4,-tetrahydropyrimido[1,6-a]-benzimidazoles as potential antiulcer agents.
In an effort to establish new antiulcer agents a series of 2-(2-substituted amino)-1 H-benzimidazoles 8, 9, 14; 1,3-disubstituted-3,4-dihydropyrimido[1,6-a]benzimidazoles 4, 7, 11, 12; 3-substituted-3,4-dihydropyrimido[1,6-a]benzimidazol-1 (2H)-thiones (or (2H)-ones) 10, 17 and 3-substituted-1,2,3,4-tetrahydropyrimido[1,6-a]benzimidazoles 15 were synthesized. Representative members were selected to evaluate their gastric antisecretory activity using an in vivo pylorus ligated rat method. Omeprazole was used as reference. The results indicated that the test compounds exhibit gastric antisecretory activity. The percent inhibition+/-SEM at the indicated dose level was demonstrated as omeprazole (59%+/-0.16 at 3 mg/kg) > 15a (53%+/-1.39 at 3 mg/kg) > 7a (51%+/-1.04 at 1 mg/kg) > 10a (50%+/-1.36 at 3 mg/kg).
Shafik
R M
RM
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, AR Egypt.
El-Din
S A Shams
SA
Eshba
N H
NH
El-Hawash
S A M
SA
Desheesh
M A
MA
Abdel-Aty
A S
AS
Ashour
H M
HM
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D001835:Body Weight; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D007202:Indicators and Reagents; D008297:Male; D009853:Omeprazole / Q000494:pharmacology; D011708:Pylorus / Q000502:physiology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D000897:Anti-Ulcer Agents; D001562:Benzimidazoles; D007202:Indicators and Reagents; D011743:Pyrimidines; D009853:Omeprazole