1204772-85-9Relevant academic research and scientific papers
A facile route to 1: H- A nd 2 H-indazoles from readily accessible acyl hydrazides by exploiting a novel aryne-based molecular rearrangement
Shamsabadi, André,Chudasama, Vijay
supporting information, p. 11180 - 11183 (2018/10/15)
Herein we report the transformation of readily synthesised acyl hydrazides into 2-hydrazobenzophenones via a novel molecular rearrangement pathway using aryne chemistry. The developed reaction protocol is performed under relatively mild conditions and is
Elemental step thermodynamics of various analogues of indazolium alkaloids to obtaining hydride in acetonitrile
Lei, Nan-Ping,Fu, Yan-Hua,Zhu, Xiao-Qing
supporting information, p. 11472 - 11485 (2015/12/04)
A series of analogues of indazolium alkaloids were designed and synthesized. The thermodynamic driving forces of the 6 elemental steps for the analogues of indazolium alkaloids to obtain hydride in acetonitrile were determined using an isothermal titration calorimeter (ITC) and electrochemical methods, respectively. The effects of molecular structure and substituents on the thermodynamic driving forces of the 6 steps were examined. Meanwhile, the oxidation mechanism of NADH coenzyme by indazolium alkaloids was examined using the chemical mimic method. The result shows that the oxidation of NADH coenzyme by indazolium alkaloids in vivo takes place by one-step concerted hydride transfer mechanism.
Discovery of 2-(1H-indazol-1-yl)-thiazole derivatives as selective EP 1 receptor antagonists for treatment of overactive bladder by core structure replacement
Atobe, Masakazu,Naganuma, Kenji,Kawanishi, Masashi,Morimoto, Akifumi,Kasahara, Ken-Ichi,Ohashi, Shigeki,Suzuki, Hiroko,Hayashi, Takahiko,Miyoshi, Shiro
, p. 1327 - 1333 (2014/03/21)
We have designed a series of potent EP1 receptor antagonists. These antagonists are a series of 2-(1H-indazol-1-yl)-thiazoles in which the core structure was replaced with pyrazole-phenyl groups. In preliminary conscious rat cystometry experiments, two representative candidates, 2 and 22, increased bladder capacity. In particular, the increase using 22 was approximately 2-fold that of the baseline. More detailed profiling of this compound and further optimization of this series promises to provide a novel class of drug for treating overactive bladder (OAB).
ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
Youngsaye, Willmen,Hartland, Cathy L.,Morgan, Barbara J.,Ting, Amal,Nag, Partha P.,Vincent, Benjamin,Mosher, Carrie A.,Bittker, Joshua A.,Dandapani, Sivaraman,Palmer, Michelle,Whitesell, Luke,Lindquist, Susan,Schreiber, Stuart L.,Munoz, Benito
, p. 1501 - 1507 (2013/10/22)
The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substances inherently toxic to either mammalian or fungal cells. A substituted indazole possessing the desired bioactivity profile was selected for further development, and initial investigation of structure-activity relationships led to the discovery of ML212.
BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS
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Page/Page column 38, (2010/03/02)
A nitrogen-containing bicyclic heterocyclic compound represented by the following formula (1) is provided. When the compound or a salt thereof is administered to a human being or an animal, the compound has a strong antagonistic action against EP1 recepto
