52147-98-5Relevant academic research and scientific papers
Antioxidant, Anti-inflammatory, and Neuroprotective Effects of Novel Vinyl Sulfonate Compounds as Nrf2 Activator
Choi, Ji Won,Shin, Su Jeong,Kim, Hyeon Ji,Park, Jong-Hyun,Kim, Hyeon Jeong,Lee, Elijah Hwejin,Pae, Ae Nim,Bahn, Yong Sun,Park, Ki Duk
supporting information, p. 1061 - 1067 (2019/06/24)
The main pathway responsible for cellular regulation against oxidative stress is nuclear factor E2-related factor-2 (Nrf2) signaling. We previously synthesized and reported a novel vinyl sulfone (1) as an Nrf2 activator with therapeutic potential for Parkinson's disease (PD). In this study, we changed the vinyl sulfone to vinyl sulfonamide or vinyl sulfonate to improve Nrf2 activating efficacy. We observed that the introduction of vinyl sulfonamide led to a reduction of the effects on Nrf2 activation, whereas vinyl sulfonate compounds exhibited superior activity compared to the vinyl sulfone compounds. Among the vinyl sulfonates, 3c exhibited 6.9- and 83.5-fold higher effects on Nrf2 activation than the corresponding vinyl sulfone (1) and vinyl sulfonamide (2c), respectively. Compound 3c was confirmed to induce expression of the Nrf2-dependent antioxidant enzymes at the protein level in cells. In addition, 3c mitigated PD-associated behavioral deficits by protecting DAergic neurons in the MPTP-induced mouse model of PD.
[3+2] Cycloaddition of an Azomethyne Ylide and Vinyl Sulfonyl Fluorides ― an Approach to Pyrrolidine-3-sulfonyl Fluorides
Mykhalchuk, Volodymyr L.,Yarmolchuk, Vladimir S.,Doroschuk, Roman O.,Tolmachev, Andrey A.,Grygorenko, Oleksandr O.
, p. 2870 - 2876 (2018/06/21)
[3+2] Cycloaddition reactions of vinyl sulfonyl fluorides with an in-situ generated nonstabilized azomethine ylide is described for the first time. The resulting pyrrolidine-3-sulfonyl fluorides were obtained in 50–83 % yield on a scale of up to 25 g. Their utility as reagents for sulfur(VI)–fluoride exchange (SuFEx) and some other transformations was also demonstrated.
Desulfonylation-Initiated Distal Alkenyl Migration in Copper-Catalyzed Alkenylation of Unactivated Alkenes
Wang, Xiaoyang,Liu, Jing,Yu, Ze,Guo, Minjie,Tang, Xiangyang,Wang, Guangwei
supporting information, p. 6516 - 6519 (2018/10/20)
A novel and efficient protocol for desulfonylation-initiated distal alkenyl migration and its application to the elusive alkenylation of unactivated alkenes have been presented. This radical cascade process has successfully achieved the vicinal difluoroal
Sulfonamide lactam inhibitors of FXa and method
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Page 21, (2010/02/08)
Sulfonamide lactams of the following formula wherein X, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R7 and R8 are as described herein, are provided which inhibitors of Factor Xa and are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.
AROMATIC COMPOUNDS HAVING CYCLIC AMINO OR SALTS THEREOF
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, (2008/06/13)
Compounds represented by general formula (I) or salts thereof which specifically inhibit FXa, exert a potent anticoagulant effect and thus are useful as medicinal compositions, wherein G1 to G4, X and Y represent each CH or N; Z1 represents -SO2- or -CH2 -; Q represents aryl or heteroaryl; and R1 to R9 represent each hydrogen or a substituent.
Tetrahydro-1,4-thiazine-1,1-dioxides: Part IV - Synthesis and conformational analysis of some 2,3,5-trisubstituted tetrahydro-1,4-thiazine-1,1-dioxides
Reddy, D. Bhaskar,Reddy, M. Muralidhar,Subbaraju, Gottumukkala V.
, p. 816 - 822 (2007/10/03)
A series of new 2-aroyl-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxides (2) has been synthesized either from phenacylsulfonylacetic acids (1) or phenacylstyrylsulfones (3), which in turn are obtained from the substituted acetophenones or styrenes, respecti
