- Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
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Hybrid systems containing pyrazole moiety show a wide spectrum of biological activities. To access novel hybrids with pyrazole ring, in this work we synthesized twenty pyrazole-carboxylic acids and twenty pyrazole-carboxamides, using simple synthetic methods, to be used as building blocks in the development of new structures.
- Ferreira, Byanca Silva,Silva, Rafaela Corrêa,Souto, Bernardo Araújo,Dos Santos, Maurício Silva
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p. 335 - 343
(2021/09/07)
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- Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes
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We report the design, synthesis, biological activity and docking studies of series of novel pyrazolo[3,4-d]pyrimidinones as DPP-IV inhibitors in diabetes. Molecules were synthesized and evaluated for their DPP-IV inhibition activity. Compounds 5e, 5k, 5o and 6a were found to be potent inhibitors of DPP-IV enzyme. Amongst all the synthesized compounds, 6-methyl-5-(4-methylpyridin-2-yl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one (5k) was found to be the most active based on in vitro DPP-IV studies and also exhibited promising in vivo blood glucose lowering activity in male Wistar rats.
- Sagar, Sneha R.,Agarwal, Jessica K.,Pandya, Dhaivat H.,Dash, Ranjeet Prasad,Nivsarkar, Manish,Vasu, Kamala K.
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supporting information
p. 4428 - 4433
(2015/10/12)
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- 3-AMINO-PYRAZOLE-4-CARBOXAMIDE DERIVATIVES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them
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Page/Page column 41
(2008/12/05)
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