Synthesis of some new heterocycles from poenzimidazole - 2 - Acetonitrile and their antinicrobial activity

The reaction of benzimidazole-2-acetonitrile 2 with chalcones la and b gave the corresponding benzimidazolo substituted hydropyridines 3 and 5, benzimidazolyl substituted hydropyridines 7 and 8, benzimidazolyl substituted pyrone 4, benzimidazolyl substituted coumarin 6 and benzimidazolyl substituted cyclohexanol 9 depending on the catalyst used and reaction temperature. The analytical and spectral data were recorded and the biological activity of these products against some bacteria and fungi was screened

Preventive effect of lansoprazole on aspirin-induced castric mucosal damage

In this randomized, double-blind, placebo-controlled study, we tested the preventive effect of lansoprazole on aspirin-induced gastric mucosal damage. The subjects received 30 mg lansoprazole [n:20] or a placebo [n:16] at night, and 12 hours later received a placebo or 1 gm aspirin The gastric mucosa was graded by endoscopists 4 hours after the administration of aspirin using a seven-point endoscopic scale. The gastric mucosa of the subjects who had taken a placebo scored a damage of 4.1 +/- 0.4 [mean +/- SD]. Lansoprazole significantly prevented gastric mucosal injury [63%] with a mean endoscopic score of 1.5 +/- 0.3 compared to the placebo-aspirin group [p<0.0003]. This study demonstrates that lansoprazole has a statistically significant preventive effect on aspirin induced gastric lesions. The preventive effect of lansoprazole may prove to be very important clinically and warrants further investigation

Clinical trial of triclabendazole on human fascioliasis: long term follow-up

Following an outbreak of human fascioliasis in Gilan province of Iran in 1989, the benzimidazole derivative triclabendazole [TCBZ] was suggested as the drug of choice after finding out that routine drugs were not effective. Two studies were performed: a clinical trial [before/after type] in 1989 and a historical cohort [1989 - 1995] to examine the efficacy of the drug. TCBZ was administered to 94 patients in four groups [A, B, C and D] according to the drug's instructions [time, size and frequency of dose]. The patients were followed up clinically and paraclinically for 60 days. The highest cure rate, i.e., omission of eggs and improvement of clinical symptoms [86.6%] was observed in Group A [5 mg/kg-NPO, 3 days]. Minor epigastric pain and vomiting and some urticaria was reported a few days after administration of the drug. Just a few developed cholangitis and one toxic hepatitis who were all treated satisfactorily. The second study was a 6-year follow-up survey of 50 of the 94 patients. Five cases had epigastric pain, and eggs were detected in the stool exams of two of them. Thus, by demonstrating up to 94% efficacy in the treatment of human fascioliasis in Iran [p<0.002], TCBZ is recommended as the drug of choice

Triclabendazole in the treatment of established human fascioliasis

The tolerance and efficacy of triclabendazole CGP 23030, specially prepared for human use, were assessed in 50 patients in the chronic phase of fascioliasis. After clinical examination, investigation and ultrasonography of the liver and biliary system, triclabendazole 10 mg/kg, either as a single or split dose, was administered. The clinical picture was studied daily for six days and the investigations were repeated 6, 30 and 60 days after treatment. The drug was tolerated. Its side-effects, which included upper abdominal pain, mild fever and limited derangement of liver function, were considered negligible. The cure rate at 2 months was 94% when assessed by the disappearance of eggs in stools and 88% when assessed by both the absence of eggs in stools and of worms in the biliary system. The use of triclabendazole for the treatment of human fascioliasis was found to be justified

Triclabendazole and fascioliasis: a new drug to combat an age-old disease

The tolerance and efficacy of triclabendazole CGP 23030, specially prepared for human use, were assessed in 50 patients in the chronic phase of fascioliasis. After clinical examination, investigation and ultrasonography of the liver and biliary system, triclabendazole 10 mg/kg, either as a single or split dose, was administered. The clinical picture was studied daily for six days and the investigations were repeated 6, 30 and 60 days after treatment. The drug was tolerated. Its side-effects, which included upper abdominal pain, mild fever and limited derangement of liver function, were considered negligible. The cure rate at 2 months was 94% when assessed by the disappearance of eggs in stools and 88% when assessed by both the absence of eggs in stools and of worms in the biliary system. The use of triclabendazole for the treatment of human fascioliasis was found to be justified

Synthesis of some new benzimidazole derivatives with evaluation of their antimicrobial activity

A series of N1-p-[2-benzimidazoylamino] benzoyl] N2-arylidene hydrazine [3a-e], pyrazolone 4 pyrazole 5, carbothioamide 6a-c, 1,3,4-thiadiazol 7 and 1,3,4-triazoles 8 were prepared. Some of the new compounds showed considerable antimicrobial activity against Gram +ve, Gram -ve bacteria, yeast and fungi

Synthesis of some novel benzimidazole derivatives as antimicrobial agents

Synthesis of 2-[p-[5-aryl-1-[H or phenyl]-delta2 pyrazolin-3-yl] anilino] benzimidazoles [4a, b], 2-[p-aryl-2-isoxazolin-3-yl] anilino] benzimidazole [5], 2-[p-[6-aryl-2-[oxo or thioxo]-1,2,5,6- tetrahydropyrimidin-4-yl] anilino] benzimidazoles [6a,b] and 2-[p- sulfamoylanilino] benzimidazoles [7a-g] were synthesized. The new compounds showed inhibitory effect against the growth of Gram +ve, Gram -ve bacteria, yeast and fungi

Synthesis of 1,3,4-thiadiazole derivatives of benzimidazole as potential antimicrobial agents

Several novel benzimidazole derivatives containing 1, 3, 4-thiadiazoles were prepared in order to study their antimicrobial activity