3416-59-9Relevant academic research and scientific papers
Novel benzenesulfonamide and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives as potential selective COX-2 inhibitors
Taher, Ehab S.,Ibrahim, Tarek S.,Fares, Mohamed,AL-Mahmoudy, Amany M.M.,Radwan, Abdullah F.,Orabi, Khaled Y.,El-Sabbagh, Osama I.
, p. 372 - 382 (2019)
Two new series of 1,2-benzisothiazol-3(2H)-one-1,1-dioxide derivatives containing either five membered heterocyclic rings or aryl hydrazones were synthesized and evaluated for their in vitro COX-1/COX-2 inhibitory activity. In vivo anti-inflammatory evalu
In situ Generation and Utilization of CO: An Efficient Route towards N-Substituted Saccharin via Carbonylative Cyclization of 2-Iodosulfonamides
Chavan, Sujit P.,Adithyaraj,Bhanage, Bhalchandra M.
supporting information, p. 2000 - 2003 (2017/09/13)
The present protocol demonstrates the synthesis of N-substituted saccharines via carbonylative cyclization of 2-iodosulfonamides using a Pd(OAc) 2 /Xantphos catalyst system and phenyl formate as a CO source. A variety of saccharin derivatives is synthesized under milder reaction conditions.
N-Substituted and ring opened saccharin derivatives selectively inhibit transmembrane, tumor-associated carbonic anhydrases IX and XII
Ivanova, Jekaterīna,Carta, Fabrizio,Vullo, Daniela,Leitans, Janis,Kazaks, Andris,Tars, Kaspars,?alubovskis, Raivis,Supuran, Claudiu T.
, p. 3583 - 3589 (2017/05/29)
A series of N-substituted saccharins incorporating aryl, alkyl and alkynyl moieties, as well as some ring opened derivatives were prepared and investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). The widespread cytosolic is
Metal-free C-N cross-coupling of electrophilic compounds and N-haloimides
Zhang, Luyan,Li, Yanru,Jin, Long-Yi,Liang, Fushun
, p. 65600 - 65603 (2015/08/18)
When DBU is added, the cross-coupling reaction between alkyl halides (halogen = Cl, Br and I) and N-haloimides (halogen = Cl, Br) occurs, resulting in the formation of aminated products. A halogen bond activated nucleophilic substitution mechanism was proposed. The methodology represents an elegant example of applying the halogen bond activation strategy in an organic transformation.
Decarbonylative C-C bond-forming reactions of saccharins by nickel catalysis: Homocoupling and cycloaddition
Mi, Pengbing,Liao, Peiqiu,Tu, Tao,Bi, Xihe
supporting information, p. 5332 - 5336 (2015/03/30)
Decarbonylation of saccharins by nickel catalysis enables two kinds of C-C bond-forming reactions; homocoupling of saccharins to form biaryls and cycloaddition with alkynes to form benzosultams. The former represents the first reported nickel-catalyzed decarbonylative C-C homocoupling reaction, whereas the latter constitutes a powerful method to pharmaceutically relevant benzosultams. The reactions proceed with good functional-group tolerance and excellent regioselectivity.
Regioselective alkylation of saccharin with alcohols under Mitsunobu conditions
Wang, Xiaolong,Ma, Yanying,Ju, Tingting
, p. 417 - 419 (2013/09/12)
The regioselective Mitsunobu alkylation of saccharin with various alcohols has been examined. The N/O-alkylation is dependent on the steric hindrance of the alcohols, that is, less sterically hindered alcohol preferentially afford N-alkylated saccharin an
TiCl4-mediated direct N-alkylation of sulfonamides with inactive ethers
Chen, Jiayan,Dang, Ling,Li, Qiang,Ye, Yong,Fu, Shaomin,Zeng, Wei
supporting information; experimental part, p. 595 - 600 (2012/03/27)
A TiCl4-mediated intermolecular or intramolecular direct N-alkylation reaction of sulfonamides with inactive ethers as alkylating agents was successfully achieved. This method provides a novel approach towards N-alkyl sulfonamides from inactive ethers via an easy workup procedure. Georg Thieme Verlag Stuttgart · New York.
DUAL MODULATION OF ENDOCANNABINOID TRANSPORT AND FATTY-ACID AMIDE HYDROLASE FOR TREATMENT OF EXCITOTOXICITY
-
, (2010/09/18)
The endocannabinoid transporter and FAAH are sites of modulation that allow pharmacological enhancement of protective endocannabinergic signals. Selective inhibitors of the transporter and inhibitors of FAAH caused additive augmentation of endogenous signaling events mediated by the cannabinoid CB1 receptor.Disruption of such signals has been shown to prevent neuronal maintenance processes and increase vulnerability to brain damage. Here, blocking endocannabinoid inactivation enhanced cannabinergic activity and ameliorated cellular disturbances associated with excitotoxicity. Modulating the endocannabinoid system in this way also prevented excitotoxic behavioral abnormalities including memory impairment. Collectively, these results indicate that increasing endocannabinoid responses by inhibiting the endocannabinoid transported and/or the inhibiting FAAH leads to molecular, cellular, and functional protection against excitotoxic insults like stroke and traumatic brain injury.
MONOACYLGLYCEROL LIPASE INHIBITORS FOR MODULATION OF CANNABINOID ACTIVITY
-
Page/Page column 128-129, (2009/05/28)
Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
Hydrogenation of N-acylcarbamates and N-acylsulfonamides catalyzed by a bifunctional [Cp*Ru(PN)] complex
Ito, Masato,Koo, Lee Wei,Himizu, Akio,Kobayashi, Chika,Sakaguchi, Ayaka,Ikariya, Takao
supporting information; experimental part, p. 1324 - 1327 (2009/06/30)
Awakening of the Cp one: the bifunctional complex 1 facilitates the interaction with substrates bearing less electrophilic carbon atoms than ketones, epoxides, and imides. The title reaction was applicable to the reduction of Evans' asymmetric alkylation products to the chiral alcohols along with gtood recovery of the chiral oxazolidinone auxiliary. EWG=electron- withdrawing group.
