21389-46-8Relevant articles and documents
N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases
Otrubova, Katerina,Chatterjee, Shreyosree,Ghimire, Srijana,Cravatt, Benjamin F.,Boger, Dale L.
, p. 1693 - 1703 (2019/03/21)
A series of N-acyl pyrazoles was examined as candidate serine hydrolase inhibitors in which the active site acylating reactivity and the leaving group ability of the pyrazole could be tuned not only through the nature of the acyl group (reactivity: amide
3-Phenylalkyl-2H-chromenes and -chromans as novel rhinovirus infection inhibitors
Conti, Cinzia,Proietti Monaco, Luca,Desideri, Nicoletta
, p. 2074 - 2083 (2017/03/23)
Following our studies on structure-activity relationships of anti-rhinovirus chromene and chroman derivatives, we designed and synthesized new series of 3-phenylalkyl-2H-chromenes and -chromans bearing differently sized, aliphatic linker chains between the two cycles. The cytotoxicity and the antiviral activity of the new compounds on human rhinovirus (HRV) serotype 1B and 14 infection were evaluated in HeLa cell cultures. Most of the tested compounds interfered with HRV1B multiplication in the micromolar or submicromolar concentrations while HRV14 was less susceptible. 3-[3-(4-Chlorophenyl)propyl]chroman (9c) was selected for preliminary mechanism of action studies due to its potent activity against both serotypes (IC50 of 0.48?μM and 1.36?μM towards HRV1B and 14, respectively) coupled with high selectivity (SI?=?206.18 and 73.26, respectively). Results of time of addition/removal studies suggest that 9c, similarly to related derivatives, behaves as a capsid binder interfering with some early events of the HRV1B infectious cycle.
Inhibition of bacterial biofilms and microbial growth with imidazole derivatives
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Page/Page column 40; 41, (2016/04/26)
Disclosure is provided for imidazole derivative compounds useful to inhibit the formation of biofilms and/or inhibit microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same.