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- Title
Synthesis and Pharmacological Evaluation of Substituted Thiazolopyrimidine Derivatives.
- Authors
Kashyap, Shiv Jee; Dudhe, Rupesh; Singh, Gurdeep
- Abstract
Thiazolopyrimidine considered as thia-analogues of the natural purine bases such as adenine and guanine. Six different kinds of thiazolo-pyrimidine can be possible, with [4,5-d], [3,2-a], [3,4-a], [3,2-c], [3,4-c], and [5,4-d] ring fusion with different biological activities. A series of novel thiazolo[3,2-a]pyrimidine derivatives were synthesized using various substituted benzaldehydes and acetophenone as a starting materials followed by condensation reaction with thiourea and cyclization reaction with chloroacetic acid. The structures of these newly synthesized compounds were confirmed by TLC, melting point, IR and 1H NMR spectral data. All the synthesized compounds were evaluated for their antioxidant, anti-inflammatory, analgesic, ulcerogenic and antibacterial activity. DPPH free radical scavenging method was used to assess the antioxidant activity and it was found that compounds K1, K4, K5, K8, K9, K10, K12, K13 and K16 exhibited 50-60% radical scavenging activity at a concentration of 100 μg/ml. Compound 7-(2,4- dichlorophenyl)-5-phenyl-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one (K9) has shown potent antiinflammatory activity carried out by carrageenan-induced paw edema model, Acetic acid induced writhing method was used for analgesic activity and it revealed that compound 7-(3,4,5- trimethoxyphenyl)-5-phenyl-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one (K5) was found to be potent analgesic agent. Ulcerogenic activity was investigated as a side effect of oral administration of test compounds and it evaluated that the compound 7-(2,4-dichlorophenyl)-5-phenyl-2Hthiazolo[ 3,2-a]pyrimidin-3(7H)-one (K9) produce lesser ulcerogenic effects.
- Subjects
THIOUREA; PYRIMIDINES; CHLOROACETIC acids; MELTING points; CONDENSATION reactions; ACETIC acid; PYRIMIDINE derivatives; CARRAGEENANS
- Publication
International Journal of Pharmacy & Life Sciences, 2020, Vol 11, Issue 7, p38
- ISSN
0976-7126
- Publication type
Article