Content area
Full text
Abstract
Wide range of biological activities is associated with 1, 4-dihydropyrimidines/ pyrimidines, individually or in combination. In view of this, the present study, was an attempt to synthesize a molecules, Ethyl-2 [(substituted thio) 1, 4 dihydro 6 methyl 4phenyl] 5 pyrimidine carboxylate, with improved biological activity, lesser toxicity with undesirable side effects in clinical use. All the synthesized compounds have been characterized by using IR, 1H NMR and elemental analysis. Further, some compounds were screened for anti-ulcer activity. Compound AT4 has shown maximum anti-ulcer activity as compared to control group.
Keywords: Anti-ulcer Activity, Dihydropyrimidines, Thioethers, tetrahydropyrimidines.
1. Introduction
An ulcer is a discontinuity or break in a bodily membrane that impedes the organ, of which that membrane is a part of, from continuing its normal functions. As many as 70-90% of such ulcers are associated with Helicobacter pylori, a spiral-shaped bacterium that lives in the acidic environment of the stomach; however, only 40% of those cases go to a doctor[1]. Among a wide variety of heterocylces that have been explored for developing pharmaceutically important molecules, pyrimidines[2] have played an important role in medicinal chemistry. Some of them have received considerable attention as potential anti-hypertensive agents. Moreover, pyrimidines acquired a special place in heterocyclic field because of their diversified activities such as anti-virus, anti-tumor, anti-bacterial agents[3-6] etc.
Further, dihydropyrimidines (DHPMs; popularly known as Biginelli's compounds) are associated with broad spectrum of biological activities ever since 4-Aryl-1, 4-dihydropyrimidines of nifedipine type were first introduced into clinical medicine in 1975. Even today they are the most potent calcium channel modulators available for the treatment of various cardiovascular diseases[7]. Several calcium channel blockers including nifedipine are reported with anti-ulcer activity[8-9]. The combination of an aldehyde , β-keto ester, and urea under acid catalysis to give a dihydropyrimidine was first reported by Pietro Biginelli in 1893.The Biginelli reaction, is a one-pot condensation reaction generates compounds with pharmacological activity, including calcium channel modulation, mitotic kinesin Eg5 inhibition, and antiviral and antibacterial activity. Although the original reaction conditions suffered from poor yields and a limited substrate scope, the recent discovery of dihydropyrimidine biological activity has led to a renewed exploration of the reaction conditions, revealing a variety of compatible solvents, acid catalysts1101.
Pyrimidine and its derivatives such as dihydropyrimidine and tetrahydropyrimidine...