77103-01-6Relevant academic research and scientific papers
Cinnamonitrile adjuvants restore susceptibility to β-lactams against methicillin-resistant staphylococcus aureus
Speri, Enrico,Kim, Choon,De Benedetti, Stefania,Qian, Yuanyuan,Lastochkin, Elena,Fishovitz, Jennifer,Fisher, Jed F.,Mobashery, Shahriar
, p. 1148 - 1153 (2019/08/27)
β-Lactams are used routinely to treat Staphylococcus aureus infections. However, the emergence of methicillin-resistant S. aureus (MRSA) renders them clinically precarious. We describe a class of cinnamonitrile adjuvants that restore the activity of oxacillin (a penicillin member of the β-lactams) against MRSA. The lead adjuvants were tested against six important strains of MRSA, one vancomycin-intermediate S. aureus (VISA) strain, and one linezolid-resistant S. aureus strain. Five compounds out of 84 total compounds showed broad potentiation. At 8 μM (E)-3-(5-(3,4-dichlorobenzyl)-2-(trifluoromethoxy)phenyl)-2-(methylsulfonyl)acrylonitrile (26) potentiated oxacillin with a >4000-fold reduction of its MIC (from 256 to 0.06 mg·L-1). This class of adjuvants holds promise for reversal of the resistance phenotype of MRSA.
Synthesis and Biological Evaluation of Furo[3,2-c]pyrazole-5-carbimidates
Siliveri, Sravanthi,Vamaraju, Harinadha Babu,Shivaraj
, p. 2389 - 2393 (2019/09/04)
In the present work, novel pyrazole fused dihydrofurans synthesized via a chronological addition of N-chloro succinimide and base piperidine to pyrano[3,2-c]pyrazole carbonitrile derivatives in methanol medium. Oxidative difunctionalization was done with
A highly efficient protocol for the regio- and stereo-selective synthesis of spiro pyrrolidine and pyrrolizidine derivatives by multicomponent reaction
Dandia, Anshu,Jain, Anuj K.,Laxkar, Ashok K.,Bhati, Dharmendra S.
, p. 3180 - 3184 (2013/06/27)
A series of novel spiro[acenaphthylene-1,2′-pyrrolidine] (4), spiro[acenaphthylene-1,2′-pyrrolizidine] (7), and spiro[indoline-3, 2′-pyrrolidine] derivatives (9) containing cyano group were successfully synthesized via a three-component 1,3-dipolar cycloaddition reaction of acenaphthenequinone or isatin, sarcosine or proline, and Knoevenagel adducts in refluxing aqueous methanol. In this intermolecular three-component combinatorial process it is amazing that three stereogenic centers with one spiro carbon are controlled very well. The structure and relative stereo-chemistry of cycloadducts were carried out by single crystal X-ray diffraction, as well as by the help of 1H, 13C, and HMBC spectroscopy.
Structural simplification of bioactive natural products with multicomponent synthesis. 4. 4H-Pyrano-[2,3-b]naphthoquinones with anticancer activity
Magedov, Igor V.,Kireev, Artem S.,Jenkins, Aaron R.,Evdokimov, Nikolai M.,Lima, Dustin T.,Tongwa, Paul,Altig, Jeff,Steelant, Wim F. A.,Van Slambrouck, Severine,Antipin, Mikhail Yu.,Kornienko, Alexander
experimental part, p. 5195 - 5198 (2012/09/07)
4H-Pyrano-[2,3-b]naphthoquinone is a structural motif commonly found in natural products manifesting anticancer activities. As part of a program aimed at structural simplification of bioactive natural products utilizing multicomponent synthetic processes,
Eco-friendly synthesis and biological evaluation of substituted pyrano[2,3-c]pyrazoles
Mandha, Santhosh Reddy,Siliveri, Sravanthi,Alla, Manjula,Bommena, Vittal Rao,Bommineni, Madhava Reddy,Balasubramanian, Sridhar
supporting information; experimental part, p. 5272 - 5278 (2012/09/07)
An ecofriendly green approach for synthesis of substituted pyrano[2,3-c]pyrazoles has been developed via a multicomponent one pot approach in aqueous ethanol medium under totally non-catalytic conditions. The synthesized compounds were evaluated for their
