138907-80-9Relevant academic research and scientific papers
Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
Dos Santos, Maurício Silva,Ferreira, Byanca Silva,Silva, Rafaela Corrêa,Souto, Bernardo Araújo
, p. 335 - 343 (2021/09/07)
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
Ye, Jiqing,Lin, Lin,Xu, Jinyi,Chan, Paul Kay-Sheung,Yang, Xiao,Ma, Cong
, (2021/05/05)
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
Discovery and optimization of pyrazole amides as antagonists of CCR1
Harcken, Christian,Sarko, Christopher,Mao, Can,Lord, John,Raudenbush, Brian,Razavi, Hossein,Liu, Pingrong,Swinamer, Alan,Disalvo, Darren,Lee, Thomas,Lin, Siqi,Kukulka, Alison,Grbic, Heather,Patel, Mita,Patel, Monica,Fletcher, Kim,Joseph, David,White, Della,Amodeo, Laura,Berg, Karen,Brown, Maryanne,Thomson, David S.
, p. 435 - 440 (2018/11/23)
A HTS screen for CCR1 antagonists afforded a novel sub-micromolar hit 5 containing a pyrazole core. In this report the design, optimization, and SAR of novel CCR1 antagonists based on a pyrazole core motif is presented. Optimization led to the advanced ca
PROTEOSTASIS REGULATORS
-
, (2013/02/27)
The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.
Synthesis and structure - Activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors
Ishibuchi, Seigo,Morimoto, Hiroshi,Oe, Takanori,Ikebe, Tsuguo,Inoue, Hiroyoshi,Fukunari, Atsushi,Kamezawa, Miho,Yamada, Ichimaro,Naka, Yoichi
, p. 879 - 882 (2007/10/03)
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.
