A series of novel 3-cyclohexyl-2-substituted hydrazino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 3-cyclohexyl-2-hydrazino quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material, 3-cyclohexyl-2-hydrazino quinazolin-4(3H)-one, was synthesized from cyclohexyl amine. Title compounds were investigated for analgesic, anti-inflammatory and ulcer...

Nonsteroidal antiinflammatory drugs have been widely used for the management of inflammation, pain and nociception. Gastric intolerance caused by most of the nonsteroidal antiinflammatory drugs used today restricts their use. Several approaches have been proposed to modify the parent nonsteroidal antiinflammatory drugs molecule in order to reduce their gastric toxicity. Oral prodrug approach is...

In our previous study we reported that synthesis of ethyl (6-substituted-3(2H)-pyridazinon-2-yl)acetate derivatives which showed potent analgesic and anti-inflammatory activities. In the present paper, as an extension of our earlier work, we described acid IVa-h and amide Va-h analog of ethyl (6-substituted-3(2H)-pyridazinon-2-y) acetate derivatives. Except for IVa, all compounds were synthesiz...

A series of pyridazinone derivatives (19-34) were synthesized with an aim to synthesize safer anti-inflammatory agents. The compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation (LPO) actions. The percentage inhibition in edema at different time intervals indicated that compounds 20, 26, 28 and 34 exhibited good anti-inflammatory potential, comparab...

The effect of paracetamol against ulcerogenic agent, naprosyn on the gastric mucosa of albino rat was observed under dissecting as well as laboratory microscope. Paracetamol in a dose of 250 mg/kg body weight provided protection against the ulcerogenic effect of naprosyn under dissecting microscope. Under laboratory microscope, a significant increase in the mucosal thickness with the administra...

PURPOSE To synthesize a new series of 5-substituted-3-methylsulfanyl-1H-pyrazole-4-carboxylic acid ethyl esters for their analgesic and anti-inflammatory activity. METHODS The title compound synthesized by reacting the amino group of 5-amino-3-methylsulfanyl-1H-pyrazole-4-carboxylic acid ethyl ester with acid anhydrides, acid chlorides and phenyl dithiocarbamates. The synthesized compounds we...

A novel series of 3-(2-amino-6-pyrimidin-4-yl)-6-bromo-2H-chromen-2-one (5a-5j) were synthesized from 3-acetyl-6-bromo-2H-chromen-2-one (3). The structures of the synthesized compounds were elucidated by IR, H-NMR, C-NMR, and mass spectroscopic techniques. The synthesized compounds were screened for in-vivo analgesic activity at a dose of 20 mg/kg body weight. Among them, compounds 5a, 5b and 5...

Infection with Helicobacter pylori is the major cause for the development of peptic ulcer disease (PUD). In children, with no other etiology for the disease, this rare event occurs shortly after infection. In these young patients, habits of smoking, diet, consumption of alcohol and non-steroid anti-inflammatory drugs and stress, in addition to the genetic susceptibility of the patient, represen...

In rats, a single administration of acrylonitrile (vinyl cyanide) produces a rapidly occurring bilateral adrenal apoplexy. Structure-activity studies have shown that a close derivative, propionitrile (ethyl cyanide), causes duodenal ulcer without markedly affecting the adrenal glands. Prolonging the two-carbon chain of propionitrile by a methyl group (n-butyronitrile) enhances, replacing the me...

Small intestinal ulceration is a frequent and potentially serious condition associated with nonselective cyclooxygenase 1/2 inhibitors (nonsteroidal anti-inflammatory drugs, NSAIDs) including diclofenac (DCF). An initial topical effect involving mitochondria has been implicated in the pathogenesis, but the exact mechanisms of NSAID-induced enteropathy are unknown. We aimed at investigating whet...