4958-06-9Relevant academic research and scientific papers
Rational design, synthesis and SAR study of novel warfarin analogous of 4-hydroxy coumarin-beta-aryl propanoic acid derivatives as potent anti-inflammatory agents
Gudimani, Parashuram,Joshi, Shrinivas,Kumbar, Vijay M.,Pawar, Varsha,Shastri, Lokesh A.,Sunagar, Vinay
, (2022/01/19)
Synthesis of highly potent and enhanced safety profiled antiinflammatory drugs has become a challenging task in the drug discovery process. A library of warfarin analogue 3-(4?hydroxy-2-oxo-2H-chromen-3-yl)-3-arylpropanoic acid derivatives have been synthesised and their structures were established by availing different analysis techniques. The invitro COX-1/COX-2 study revealed the effective potency of the selective compounds 2b(IC50=180.45 μl/ml), 2c(IC50=21.03 μl/ml) and 2f(IC50=120.45 μl/ml) against COX-2 compared to reference drug aspirin (IC50=121.60 μl/ml). Compound 2c is more selective towards COX-2 with a high selective index of 7.42 than standard aspirin with a selective index of 4.14. Further, the target molecules were assessed for their antiinflammatory activity against MMP2 and MMP9, the results revealing a high percentage of inhibition. While, protein denaturation study displayed high potency of the compounds 2a (IC50=13.32 μg/ml), 2 g (IC50=11.14 μg/ml) and 2l (IC50=4.71 μg/ml) as compared with aspirin (IC50=13.42 μl/ml). The docking studies were established to understand the structural features responsible for biological activity and the outcome of the docking studies are indeed following the experimental results.
Materials and methods for treating coagulation disorders
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, (2008/06/13)
This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention
Materials and methods for treating coagulation disorders
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, (2008/06/13)
This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention
