Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
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.
Design, synthesis, biological evaluation and in silico studies of pyrazole‐based nh2‐acyl oseltamivir analogues as potent neuraminidase inhibitors
Oseltamivir represents one of the most successful neuraminidase (NA) inhibitors in the current anti‐influenza therapy. The 150‐cavity of NA was identified as an additional binding pocket, and novel NA inhibitors have been designed to occupy the 150‐cavity
Ye, Jiqing,Lin, Lin,Xu, Jinyi,Chan, Paul Kay-Sheung,Yang, Xiao,Ma, Cong
(2021/05/05)
COMPOSITIONS AND METHODS FOR TREATING CANCER
Disclosed herein, inter alia, are compositions and methods for modulating Ras and treating cancer.
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Paragraph 0746; 0747
(2018/09/11)
Synthesis and leishmanicidal activities of 1-(4-X-phenyl)-N′-[(4-Y- phenyl)methylene]-1H-pyrazole-4-carbohydrazides
1H-pyrazole-4-carbohydrazides were synthesized and their leishmanicidal in vitro activities and cytotoxic effects were investigated. The drugs prototypes of these new compounds (ketoconazole, benznidazole, allopurinol and pentamidine) were also tested. It
Bernardino, Alice M.R.,Gomes, Adriana O.,Charret, Karen S.,Freitas, Antonio C.C.,Machado, Gerzia M.C.,Canto-Cavalheiro, Marilene M.,Leon, Leonor L.,Amaral, Veronica F.
p. 80 - 87
(2007/10/03)
Synthesis and structure - Activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors
A series of 1-phenylpyrazoles was evaluated for inhibitory activity against xanthine oxidase in vitro. Of the compounds prepared, 1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid (Y-700) had the most potent enzyme inhibition and displayed longer-lasting hypouricemic action than did allopurinol in a rat model of hyperuricemia induced by the uricase inhibitor potassium oxonate.
3-(1-SUBSTITUTED-PYRAZOYL)-2-OXINDOLE DERIVATIVES, COMPOSITIONS AND USE
This invention relates to novel 3-(1-substituted-pyrazoyl)-2-oxindole derivatives which are inhibitors of prostaglandin H2 synthease, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H
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(2008/06/13)
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