Irritable bowel syndrome (IBS) is a disorder associated with muscarinic receptors (M 3 ) and characterized by cramping, abdominal pain, bloating, constipation and/or diarrhea (1, 2). Pain and intestinal spasms are the common state in chronic colon conditions such as irritable bowel syndrome, diverticulitis, and colitis. The muscarinic antagonistic activities, mediated by M 3 receptors, are responsible for the smooth muscle spasm (3, 4). Antispasmodics are the most commonly used drugs, of which antimuscarinic agents are an important class. However, the efficacy of these agents is significantly limited due to lack of receptor subtype selectivity, resulting in unacceptable atropine--like side effects.M 3 -selective antimuscarinic agents were sucessfully used in the treatment of IBS with minimal atropine-like side effects (5). A series of 1-substituted imidazoles 1a-d and 2a-d were synthesized and screened for antispasmodic and antidiarrheal activities. Antispasmodic activity was tested at various concentrations on isolated tissue preparations; concentration-response curves were plotted and compared with atropine. All compounds were found to inhibit contraction of the guinea pig ileum. Castor oil-induced diarrhea model in rats was used for evaluation of antidiarrheal activity. Parameters such as intestinal transit and volume of intestinal fluid were measured for antidiarrheal activity at 40 mg kg -1 dose and compared with the standard drug loperamide at 6 mg kg -1 dose. Defecation frequency in the test group was found to be significantly lower (p < 0.01) compared to the control group and comparable with that of the standard. The present study reveals that the compounds exert antidiarrheal activity through possible inhibition of intestinal movement and reduction of capillary permeability in the abdominal cavity.