94038-18-3Relevant academic research and scientific papers
Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents
González-Calderón, Davir,Mejía-Dionicio, María G.,Morales-Reza, Marco A.,Ramírez-Villalva, Alejandra,Morales-Rodríguez, Macario,Jauregui-Rodríguez, Bertha,Díaz-Torres, Eduardo,González-Romero, Carlos,Fuentes-Benítes, Aydeé
, p. 60 - 65 (2016)
Seven miconazole analogs involving 1,4,5-tri and 1,5-disubstituted triazole moieties were synthesized by azide-enolate 1,3-dipolar cycloaddition. The antifungal activity of these compounds was evaluated in vitro against four filamentous fungi, including A
THERAPEUTIC INHIBITORS OF THE REVERSE MODE OF ATP SYNTHASE
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Page/Page column 22, (2018/08/12)
Compounds of the following formula, and pharmaceutically-acceptable salts, solvates, hydrates and prodrugs thereof, formula (A) are useful to preferentially inhibit the ATP-hydrolysing mode of ATP synthase, and are thereby useful for treating various dise
A convergent, scalable and stereoselective synthesis of azole CYP51 inhibitors
Lepesheva, Galina,Christov, Plamen,Sulikowski, Gary A.,Kim, Kwangho
, p. 4248 - 4250 (2017/10/12)
The study and development of azole-based CYP51 inhibitors is an active area of research across disciplines of biochemistry, pharmacology and infectious disease. Support of in vitro and in vivo studies require the development of robust asymmetric routes to single enantiomer products of this class of compounds. Herein, we describe a scalable and enantioselective synthesis to VNI and VFV, the two potent inhibitors of protozoan sterol 14α-demethylase (CYP51) that are currently under consideration for clinical trials for Chagas disease. A key transformation is the Jacobsen Hydrolytic Kinetic Resolution (HKR) reaction. The utility of the synthetic route is illustrated by the preparation of >25 g quantities of single enantiomers of VNI and VFV.
N-[1-Aryl-2-(1-imidazolo)ethyl]-guanidine derivatives as potent inhibitors of the bovine mitochondrial F1F0 ATP hydrolase
Atwal, Karnail S.,Ahmad, Saleem,Ding, Charles Z.,Stein, Philip D.,Lloyd, John,Hamann, Lawrence G.,Green, David W.,Ferrara, Francis N.,Wang, Paulina,Rogers, W. Lynn,Doweyko, Lidia M.,Miller, Arthur V.,Bisaha, Sharon N.,Schmidt, Joan B.,Li, Ling,Yost, Kenneth J.,Lan, Hsi-Jung,Madsen, Cort S.
, p. 1027 - 1030 (2007/10/03)
A series of substituted guanidine derivatives were prepared and evaluated as potent and selective inhibitors of mitochondrial F1F0 ATP hydrolase. The initial thiourethane derived lead molecules possessed intriguing in vitro pharmacological profiles, though contained moieties considered non-drug-like. Analogue synthesis efforts led to compounds with maintained potency and superior physical properties. Small molecules in this series which potently and selectivity inhibit ATP hydrolase and not ATP synthase may have utility as cardioprotective agents.
