نتایج جستجو برای: piperazines

تعداد نتایج: 199  

2016
Anand Kumar Mary Drozd Ruby Pina-Mimbela Xiulan Xu Yosra A. Helmy Janet Antwi James R. Fuchs Corey Nislow Jillian Templeton Patrick J. Blackall Gireesh Rajashekara

Campylobacter is a leading cause of foodborne bacterial gastroenteritis worldwide and infections can be fatal. The emergence of antibiotic-resistant Campylobacter spp. necessitates the development of new antimicrobials. We identified novel anti-Campylobacter small molecule inhibitors using a high throughput growth inhibition assay. To expedite screening, we made use of a "bioactive" library of ...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2011
Sabrina Pagliarusco Silvia Martinucci Ellenia Bordini Lidia Miraglia Domenico Cufari Luca Ferrari Mario Pellegatti

Casopitant [1-piperidinecarboxamide,4-(4-acetyl-1-piperazinyl)-N-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)-ethyl)-2-(4-fluoro-2-methylphenyl)-N-methyl-(2R,4S)] has been shown to be a potent and selective antagonist of the human neurokinin 1 receptor, the primary receptor for substance P. During long-term toxicity studies conducted in rat and dog, evidence of cardiomyopathy and increased cardiac ...

Journal: :Drug testing and analysis 2014
Madeleine J Swortwood W Lee Hearn Anthony P DeCaprio

Since the introduction of synthetic heroin, designer drugs have been increasing in prevalence in the United States drug market over the past few decades. Recently, 'legal highs' sold as 'bath salts' have become a household term for one such class of designer drugs. While a number of federal and state bans have been enacted, the abuse of these designer drugs still continues. Few assays have been...

2017
Michelle F. Corrêa Álefe J. R. Barbosa Larissa B. Teixeira Diego A. Duarte Sarah C. Simões Lucas T. Parreiras-e-Silva Aleksandro M. Balbino Richardt G. Landgraf Michel Bouvier Claudio M. Costa-Neto João P. S. Fernandes

The histamine receptors (HRs) are traditional G protein-coupled receptors of extensive therapeutic interest. Recently, H3R and H4R subtypes have been targeted in drug discovery projects for inflammation, asthma, pain, cancer, Parkinson's, and Alzheimer's diseases, which includes searches for dual acting H3R/H4R ligands. In the present work, nine 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazi...

2015
Antonio Iudici Gianluca Castelnuovo Elena Faccio

The abuse of legal and illegal drugs is a complex and constantly evolving phenomenon. In recent years the polydrug use, term that refers to the use of two or more psychoactive drugs in combination to achieve a particular effect, has been on the rise. In many cases, one drug (amphetamine, cocaine, or heroin) is used as a base, with additional drugs being added to compensate for the side effects ...

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