66126-16-7Relevant academic research and scientific papers
Structure-Activity Relationships of Benzamides and Isoindolines Designed as SARS-CoV Protease Inhibitors Effective against SARS-CoV-2
Welker, Armin,Kersten, Christian,Müller, Christin,Madhugiri, Ramakanth,Zimmer, Collin,Müller, Patrick,Zimmermann, Robert,Hammerschmidt, Stefan,Maus, Hannah,Ziebuhr, John,Sotriffer, Christoph,Schirmeister, Tanja
supporting information, p. 340 - 354 (2020/10/19)
Inhibition of coronavirus (CoV)-encoded papain-like cysteine proteases (PLpro) represents an attractive strategy to treat infections by these important human pathogens. Herein we report on structure-activity relationships (SAR) of the noncovalent active-site directed inhibitor (R)-5-amino-2-methyl-N-(1-(naphthalen-1-yl)ethyl) benzamide (2 b), which is known to bind into the S3 and S4 pockets of the SARS-CoV PLpro. Moreover, we report the discovery of isoindolines as a new class of potent PLpro inhibitors. The studies also provide a deeper understanding of the binding modes of this inhibitor class. Importantly, the inhibitors were also confirmed to inhibit SARS-CoV-2 replication in cell culture suggesting that, due to the high structural similarities of the target proteases, inhibitors identified against SARS-CoV PLpro are valuable starting points for the development of new pan-coronaviral inhibitors.
A Spiroalkylation Method for the Stereoselective Construction of α-Quaternary Carbons and Its Application to the Total Synthesis of (R)-Puraquinonic Acid
Elmehriki, Adam A. H.,Gleason, James L.
supporting information, p. 9729 - 9733 (2019/12/02)
Cyclic α-quaternary carbon stereocenters were prepared from biselectrophillic substrates and an easily prepared chiral bicyclic sulfonyl lactam. This was achieved in two steps by spiroalkylation, employing biphasic reaction conditions with a phase-transfer catalyst, followed by reduction and alkylation with a series of alkyl halide electrophiles. The products of this method were isolated in good yields with with high levels of diastereoselectivity. This methodology was employed in the enantioselective total synthesis of (R)-puraquinonic acid (1) for a late-stage installation of the α-quaternary carbon stereocenter. This enabled the shortest synthesis of 1 to date, an eight-pot sequence providing an overall yield of 14%.
Pyrimidine heterocyclic compounds, pyrimidine heterocyclic compound salts, and preparation method and application thereof
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Paragraph 0207; 0208; 0209; 0210, (2017/07/26)
The invention provides pyrimidine heterocyclic compounds, pyrimidine heterocyclic compound salts, and a preparation method and application thereof. According to the pyrimidine heterocyclic compounds provided by the invention, specific Rq is selected, so that the obtained compounds have favorable drug resistance and long half life when being used as the medicine for treating or preventing HIV. The compounds have the advantages of high activity, low toxicity and high stability.
AZOLINE COMPOUNDS SUBSTITUTED BY A CONDENSED RING SYSTEM
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Page/Page column 119, (2016/07/27)
The present invention relates to compounds of formula I wherein the variables are as defined in the claims and the description. The invention further relates to the use of these compounds for controlling invertebrate pests and to plant propagation materia
METHOD FOR PRODUCING 2-(HALOGENOMETHYL)-3-METHYLNITROBENZENE
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Paragraph 0126, (2016/12/07)
Position-1 halogen can be selectively reduced by reacting a compound represented by formula (3): [wherein X represents a chlorine atom, a bromine atom, or an iodine atom] with halogen in the presence of a heterogeneous transition metal catalyst to produce 2-(halogenomethyl)-1-methyl-3-nitrobenzene represented by formula (1): [wherein the symbol is as defined above].
Benzosulfones as photochemically activated sulfur dioxide (SO2) donors
Malwal, Satish R.,Chakrapani, Harinath
, p. 2399 - 2406 (2015/03/04)
Sulfur dioxide (SO2) is a gaseous environmental pollutant which is routinely used in industry as a preservative and antimicrobial. Recent data suggests that SO2 may have value as a therapeutic agent. However, due to its gaseous nature, localizing SO2 generation is challenging. Herein, various 1,3-dihydrobenzo[c]thiophene 2,2-dioxides (benzosulfones) were prepared as candidates for photochemically activated sulfur dioxide (SO2) generation. These compounds were found to be stable in buffer but were photolysed upon irradiation with UV light to generate SO2. Our data indicates that photolysis of benzosulfones depends on substituents, and that the presence of electron donating groups results in an enhanced yield of SO2. This journal is
Synthesis and redox-enzyme modulation by amino-1,4-dihydro-benzo[d][1,2]dithiine derivatives
Espinosa, Sandraliz,Solivan, Melissa,Vlaar, Cornelis P.
body text, p. 3023 - 3026 (2009/10/04)
A convenient method to prepare a series of benzodithiine derivatives was developed, via the synthesis of cyclic disulfide building blocks containing an amino-group linker. Some of the novel cyclic disulfide compounds are shown to modulate the activity of the redox-enzyme glutathione reductase.
SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS PPAR MODULATORS FOR THE TREATMENT OF NON-ALCOHOLIC STEATOHEPATITIS
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Page/Page column 15, (2008/12/07)
Disclosed herein are new methods of treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver in a subject by modulating PPARδ with sulfonyl-substituted bicyclic compounds and co
METHODS FOR THE MODULATION OF CRP BY THE SELECTIVE MODULATION OF PPAR DELTA
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Page/Page column 12, (2010/11/29)
The present invention discloses methods to reduce C-reactive protein (CRP) in patients in need thereof comprising the selective modulation of PPARδ.
Synthesis of chromanyl and dihydrobenzofuranyl piperazines
Favor, David A.,Johnson, Douglas S.,Powers, James J.,Li, Tingsheng,Madabattula, Rambabu
, p. 3039 - 3041 (2008/02/06)
The synthesis of a series of regioisomeric chromanyl and dihydrobenzofuranyl piperazines is described.
