PURPOSE An efficient method has been described for synthesis of 6-(substituted aryl)-4-(3,5-diphenyl-1H-1,2,4-triazol-1-yl)-1, 6-dihydropyrimidine-2-thiol, as a beneficial antimicrobial, anticonvulsant and anticancer agents. METHODS The clalcones of title compounds were synthesized in three steps and subsequently these chalcones were further reacted with thiourea in the presence of KOH in eth...

Acute esophagitis and esophageal strictures typically occur after local radiation therapy to the thoracic field. Toxicity is usually limited to the field of radiation and potentially augmented by concomitant use of chemotherapy, however esophageal stricturing due to chemotherapy alone is exceedingly rare. Gastrointestinal toxicity has been previously reported in the setting of 5-fluorouracil (5...

an efficient synthesis route to 1,4-dihydropyrimidine derivatives from reaction of divergent aldehydes with ethylacetoacetate and urea under solvent-free conditions by zno nanoparticles as a relative in expansive, eco-friendly, easy available, non-volatile, non-explosion, thermally robust, recyclable and easy to handle catalyst at 90°c with excellent yields is described. unenhanced reaction tim...

The kinetic properties and control mechanisms of 5-fluorouracil (5-FU), uracil, and thymine degradation by rat liver dihydropyrimidine dehydrogenase were studied in vitro. The calculated Michaelis constant (Km) for 5-FU was 3.49 +/- 0.41 (SE) microM, similar to those for uracil (2.26 +/- 0.28 microM) and for thymine (2.23 +/- 0.34 microM). However, the reduction of 5-FU appears to be most sensi...

A classic example of a rationally developed class of anticancer drugs, the fluoropyrimidines are now the focus of further rational approaches to cancer chemotherapy as they are transformed into oral formulations. Given alone, oral 5-fluorouracil (5-FU) has erratic absorption and nonlinear pharmacokinetics. However, when oral 5-FU is given as a prodrug and/or paired with a dihydropyrimidine dehy...

While the majority of patients can be treated safely with fluoropyrimidine, some experience severe fluoropyrimidine-associated toxicity. The frequency and severity of these adverse events vary from patient to patient and are partially explained by genetic polymorphism into the dihydropyrimidine dehydrogenase (DPYD) gene. Carriers of the rare allelic variants DPYD*2A, DPYD*13, and DPYD D949V are...

A 67-year-old man developed a suspected adverse drug reaction during treatment with topical 5-fluorouracil (5-FU) for multiple actinic keratosis of the face, neck, and forearms. The man received topical 5-FU at a dosage of 0.5% for the actinic keratoses. After 1 week, he developed extreme lethargy, fatigue, fever, and mouth erosions. Several days later, and after discontinuation of 5-FU, painfu...