Design, synthesis and pharmacological assay of novel azo derivatives of dihydropyrimidinones
نویسندگان
چکیده
The present work deals with the synthesis of some novel azo derivatives of dihydropyrimidinones. The structures of newly synthesized compounds were established on the basis of their FTIR, 1H NMR, Mass spectrometry and elemental analysis data results. The synthesized agents were assessed for their in vivo anti-inflammatory activity on the Wistar albino rats. The compounds were also screened for their anthelmintic activity on Indian earthworms and anti-bacterial activity against some Gram-positive and Gram-negative strains of bacteria. This pharmacological activity appraisal unveils that among all the compounds screened, compounds 4b, 4c and 4g were found to have potential anti-inflammatory activity. Furthermore, compounds 4b and 4c exhibited appreciable anthelmintic properties while compounds 4b and 4d showed leading anti-bacterial activity against the selected pathogenic strains of bacteria. Subjects: Drug Design & Development; Microbiology; Pharmaceutical Medicine
منابع مشابه
Design, Synthesis and Pharmacological Evaluation of Novel 2-[2-(2-Chlorophenoxy) phenyl]-1,3,4-oxadiazole Derivatives as Benzodiazepine Receptor Agonists
New derivatives of 2-[2-(2-Chlorophenoxy)phenyl]-1,3,4-oxadiazole as candidates for agonistic effect on benzodiazepine receptors were synthesized. Conformational analysis and superimposition of energy minima conformers of the novel compounds on estazolam, a known benzodiazepine agonist, revealed that the main proposed benzodiazepine pharmacophores were well matched. In pharmacological eval...
متن کاملDesign, Synthesis and Pharmacological Evaluation of Novel 2-[2-(2-Chlorophenoxy) phenyl]-1,3,4-oxadiazole Derivatives as Benzodiazepine Receptor Agonists
New derivatives of 2-[2-(2-Chlorophenoxy)phenyl]-1,3,4-oxadiazole as candidates for agonistic effect on benzodiazepine receptors were synthesized. Conformational analysis and superimposition of energy minima conformers of the novel compounds on estazolam, a known benzodiazepine agonist, revealed that the main proposed benzodiazepine pharmacophores were well matched. In pharmacological eval...
متن کاملSynthesis and Pharmacological Evaluation of Some Novel Isatin Derivatives for Antimicrobial Activity
In the present work, a series of new 5-substituted-3-(4-arylimino)-1-[5-mercapto(1,3,4-oxadiazolyl)]-methyl-indol-2-one (4a-g) have been synthesized by heterocyclization of 5-substituted-3-(4-arylimino)-2-oxo-1-indole acetylhyrazide (3a-g) on treatment with CS2 in ethanolic KOH. The compound 4a was characterized by its elemental analysis, IR, 1HNMR and Mass Spectroscopy. The synthesized compoun...
متن کاملGreen procedure for synthesis of 3, 4 dihydropyrimidinones using 12-molybdophosphoric acid, as a catalyst and solvent free condition under microwave irradiation
Simple and improved conditions have been found to carry out the Biginelli reaction for the synthesis of 3, 4-dihydropyrimidin-2(1H) - one derivatives. This synthesis was performed in the presence of 12-molybdophosphoric acid (H3PMo12O40) as catalyst. These reactions were performed under solvent free conditions with microwave irradiation as the energy source. Compared with the classical Biginell...
متن کاملDesigning and Synthesis of Novel Celecoxib Derivatives with Aminosulfonylmethyl and Azidomethyl Substituents as Selective Cyclooxygenase-2 Inhibitors
Introduction: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are used in treating pathologic conditions such as fever, pain and inflammation by inhibiting cyclooxygenase and consequently prostaglandin production. Recently , the discovery of different isoforms of this enzyme, Cyclooxygenase-1 (COX-1) and Cyclooxygense-2 (COX-2), has led to the synthesis and introduction of novel drugs with selec...
متن کامل