682813-61-2Relevant academic research and scientific papers
Silver/palladium relay catalyzed 1,3-dipole annulation/allylation reactions to access fully substituted allyl imidazolidines
Han, Ruiping,Ding, Yue,Jin, Xueke,Li, Er-Qing
supporting information, p. 646 - 649 (2020/02/11)
A silver/palladium relay catalyzed 1,3-dipole annulation/allylation reaction of iminoesters and Baylis-Hillman acetates for the construction of fully substituted allyl imidazolidines is reported. The reaction of both iminoesters and Baylis-Hillman acetate
Fe(III)-Catalyzed Hydroallylation of Unactivated Alkenes with Morita-Baylis-Hillman Adducts
Qi, Jifeng,Zheng, Jing,Cui, Sunliang
supporting information, p. 1355 - 1358 (2018/03/09)
An Fe(III)-catalyzed hydroallylation of unactivated alkenes with Morita-Baylis-Hillman adducts via an Fe-catalyzed process is described. A variety of alkenes, including mono-, di-, and trisubstituted alkenes, could all smoothly convert to structural diver
Methylsulfenylation of Electrophilic Carbon Atoms: Reaction Development, Scope, and Mechanism
Pereira, Adriane A.,Pereira, Amanda S.,de Mello, Amanda C.,Carpanez, Arthur G.,Horta, Bruno A. C.,Amarante, Giovanni W.
supporting information, p. 1578 - 1582 (2017/04/06)
An innovative method for the methylsulfenylation of electrophilic carbons was explored. Cheap and commercially available dimethyl sulfoxide (DMSO) was used as a source of the –SCH3 group. Chalcone, dibenzylideneacetone, and Morita–Baylis–Hillma
Development of an Acrylate Derivative Targeting the NLRP3 Inflammasome for the Treatment of Inflammatory Bowel Disease
Cocco, Mattia,Pellegrini, Carolina,Martínez-Banaclocha, Helios,Giorgis, Marta,Marini, Elisabetta,Costale, Annalisa,Miglio, Gianluca,Fornai, Matteo,Antonioli, Luca,López-Castejón, Gloria,Tapia-Abellán, Ana,Angosto, Diego,Hafner-Bratkovi?, Iva,Regazzoni, Luca,Blandizzi, Corrado,Pelegrín, Pablo,Bertinaria, Massimo
, p. 3656 - 3671 (2017/05/17)
Pharmacological inhibition of NLRP3 inflammasome activation may offer a new option in the treatment of inflammatory bowel disease. In this work, we report the design, synthesis, and biological screening of a series of acrylate derivatives as NLRP3 inhibitors. The in vitro determination of reactivity, cytotoxicity, NLRP3 ATPase inhibition, and antipyroptotic properties allowed the selection of 11 (INF39), a nontoxic, irreversible NLRP3 inhibitor able to decrease interleukin-1β release from macrophages. Bioluminescence resonance energy transfer experiments proved that this compound was able to directly interfere with NLRP3 activation in cells. In vivo studies confirmed the ability of the selected lead to alleviate the effects of colitis induced by 2,4-dinitrobenzenesulfonic acid in rats after oral administration.
PYRIDOPYRIMIDINE BASED DERIVATIVES AS POTENTIAL PHOSPHODIESTERASE 3 (PDE3) INHIBITORS AND A PROCESS FOR THE PREPARATION THEREOF
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Paragraph 0082; 0103; 0104; 0110, (2014/08/19)
The present invention provides compounds of formula 1 as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula 1 can be employed as therapeutics in human and veterinary medicine, where
INDOLIZINONE BASED DERIVATIVES AS POTENTIAL PHOSPHODIESTERASE 3 (PDE3) INHIBITORS AND A PROCESS FOR THE PREPARATION THEREOF
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Paragraph 0077, (2014/10/16)
The present invention provides compounds of general formula A useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula A can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
Synthesis and evaluation of novel 2-pyridone derivatives as inhibitors of phosphodiesterase3 (PDE3): A target for heart failure and platelet aggregation
Ravinder, Mettu,Mahendar, Budde,Mattapally, Saidulu,Hamsini, Kommi Venkata,Reddy, Thatikonda Narendar,Rohit, Chilappa,Srinivas, Kolupula,Banerjee, Sanjay Kumar,Rao, Vaidya Jayathirtha
, p. 6010 - 6015 (2012/11/07)
Twenty-six 2-pyridone derivatives (8a-8z), which are structurally analogous to amrinone and milrinone two important cardiotonic drugs, are synthesized and characterized. The synthesis of 2-pyridone derivatives involves addition, followed by cyclization be
Trifluoroacetic acid: a more effective and efficient reagent for the synthesis of 3-arylmethylene-3,4-dihydro-1H-quinolin-2-ones and 3-arylmethyl-2-amino-quinolines from Baylis-Hillman derivatives via Claisen rearrangement
Pathak, Richa,Madapa, Sudharshan,Batra, Sanjay
, p. 451 - 460 (2007/10/03)
Trifluoroacetic acid has been discovered to be a highly effective and efficient reagent for the tandem Claisen rearrangement and cyclization reaction to yield 3-arylmethylene-3,4-dihydro-1H-quinolin-2-ones from compounds obtained from the SN2 r
Sodium hydride mediated cascade reaction towards the synthesis of 1,5-disubstituted uracil from cyanamides derived from Baylis-Hillman adducts
Nag,Yadav,Maulik,Batra
, p. 911 - 917 (2007/12/27)
The substituted cyanamides generated from Baylis-Hillman adducts afford 1,5-disubstituted uracils via a sodium hydride induced cascade reaction involving sequential intramolecular attack of the hydroxy group on the nitrile group, cyclization of the result
Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors
Tanaka, Taisaku,Muto, Tsuyoshi,Maruoka, Hiroshi,Imajo, Seiichi,Fukami, Harukazu,Tomimori, Yoshiaki,Fukuda, Yoshiaki,Nakatsuka, Takashi
, p. 3431 - 3434 (2008/02/10)
A novel series of 6-substituted 4-sulfonyl-1,4-diazepane-2,5-diones were designed, synthesized and evaluated as human chymase inhibitors. Structure-activity relationship studies led to the identification of a potent inhibitor, (6S)-6-(5-chloro-2-methoxybe
