title: Synthesis, antispasmodic and antidiarrheal activities of some 1-substituted imidazole derivatives.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra Ranchi, Jharkhand-835215, India. lbaskii@gmail.com
authors.forename: Baskar
authors.initials: B
authors.lastname: Lakshmanan
authors.forename: Papiya Mitra
authors.initials: PM
authors.lastname: Mazumder
authors.forename: Dinakar
authors.initials: D
authors.lastname: Sasmal
authors.forename: Swastika
authors.initials: S
authors.lastname: Ganguly
mesh_terms: D000818:Animals; D000930:Antidiarrheals / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D018680:Cholinergic Antagonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D003967:Diarrhea / Q000139:chemically induced / Q000188:drug therapy; D015195:Drug Design; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D015394:Molecular Structure; D009126:Muscle Relaxation / Q000187:drug effects; D010276:Parasympatholytics / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship; D044366:Transition Temperature
chemical_list: D000930:Antidiarrheals; D018680:Cholinergic Antagonists; D007093:Imidazoles; D010276:Parasympatholytics