14378-06-4Relevant articles and documents
Lithium bromide as a new catalyst for carbon-carbon bond formation in the solid state
Prajapati, Dipak,Lekhok, Kushal C.,Sandhu, Jagir S.,Ghosh, Anil C.
, p. 959 - 960 (1996)
Lithium bromide catalyses the condensation of carbonyl compounds with active methylene compounds in the absence of solvent, to afford olefinic products in high yields. Copyright 1996 by the Royal Society of Chemistry.
Permanganate Ion Oxidations. 16. Substituent Effects on the Rate of Oxidation of α,β-Unsaturated Carboxylate Ions
Freeman, Fillmore,Kappos, John C.
, p. 1654 - 1657 (1986)
The kinetics of the permanganate ion oxidation of substituted α,β-unsaturated carboxylate ions were investigated in phosphate buffered solutions (pH 6.83 +/- 0.03).Although the rate of oxidation is not very sensitive to electronic effects, steric factors
trans-Selective hydrocyanation of ynoates, ynones and ynoic acids catalyzed by nucleophilic phosphines
Meyer, Maximilian,Peri?, Milica,Sch?mberg, Fritz,Vilotijevi?, Ivan
supporting information, (2021/10/04)
trans-Selective hydrocyanation of ynoates and ynones in the presence of TMSCN and an alcohol additive are catalyzed by nucleophilic phosphines. The trisubstituted E-olefin products of anti-addition of hydrogen cyanide to the alkyne are produced with high regio- and stereoselectivity. The alcohol additive reacts with TMSCN to produce hydrogen cyanide in situ. Ynoic acids undergo the phosphine catalyzed hydrocyanation in the presence of TMSCN under aprotic conditions only. In these reactions, TMSCN reacts with the acid to generate hydrogen cyanide and the silyl ester which, unlike the acid, undergoes phosphine catalyzed hydrocyanation and gives the stereo-defined E-2-cyano-acrylic acids after work up.
Development of Novel Mitochondrial Pyruvate Carrier Inhibitors to Treat Hair Loss
Liu, Xiaoguang,Flores, Aimee A.,Situ, Lisa,Gu, Wen,Ding, Hui,Christofk, Heather R.,Lowry, William E.,Jung, Michael E.
, p. 2046 - 2063 (2021/02/16)
Herein, we report the synthesis and evaluation of novel analogues of UK-5099 both in vitro and in vivo for the development of mitochondrial pyruvate carrier (MPC) inhibitors to treat hair loss. A comprehensive understanding of the structure-activity relationship was obtained by varying four positions of the hit compound, namely, the alkyl group on the N1 position, substituents on the indole core, various aromatic and heteroaromatic core structures, and various Michael acceptors. The major discovery was that the inhibitors with a 3,5-bis(trifluoromethyl)benzyl group at the N1 position were shown to have much better activity than JXL001 (UK-5099) to increase cellular lactate production. Additionally, analogue JXL069, possessing a 7-azaindole heterocycle, was also shown to have significant MPC inhibition activity, which further increases the chemical space for drug design. Finally, more than 10 analogues were tested on shaved mice by topical treatment and promoted obvious hair growth on mice.
COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH
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Page/Page column 78-79; 82, (2020/07/21)
The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.
Discovery of Novel Celastrol Derivatives as Hsp90-Cdc37 Interaction Disruptors with Antitumor Activity
Li, Na,Xu, Manyi,Wang, Bing,Shi, Zhixian,Zhao, Zihao,Tang, Yunqing,Wang, Xinyue,Sun, Jianbo,Chen, Li
, p. 10798 - 10815 (2019/12/25)
To develop novel and efficient heat shock protein 90-cell division cycle 37 (Hsp90-Cdc37) interaction disruptors, several lipophilic fragments were introduced into celastrol (CEL) to synthesize 48 new CEL derivatives. Among all the target compounds, 41 wa
Development of the First Two-Pore Domain Potassium Channel TWIK-Related K+ Channel 1-Selective Agonist Possessing in Vivo Antinociceptive Activity
Vivier, Delphine,Soussia, Ismail Ben,Rodrigues, Nuno,Lolignier, Stéphane,Devilliers, Ma?ly,Chatelain, Franck C.,Prival, Laetitia,Chapuy, Eric,Bourdier, Geoffrey,Bennis, Khalil,Lesage, Florian,Eschalier, Alain,Busserolles, Jér?me,Ducki, Sylvie
supporting information, p. 1076 - 1088 (2017/02/19)
The TWIK-related K+ channel, TREK-1, has recently emerged as an attractive therapeutic target for the development of a novel class of analgesic drugs, suggesting that activation of TREK-1 could result in pain inhibition. Here, we report the synthesis of a series of substituted acrylic acids (1-54) based on our previous work with caffeate esters. The analogues were evaluated for their ability to modulate TREK-1 channel by electrophysiology and for their in vivo antinociceptive activity (acetic acid-induced writhing and hot plate assays), leading to the identification of a series of novel molecules able to activate TREK-1 and displaying potent antinociceptive activity in vivo. Furyl analogue 36 is the most promising of the series.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Paragraph 00611, (2016/01/25)
Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Activation of C-H bonds α to nitriles for combinatorial chemistry: Ruthenium-catalyzed aldol and Michael reactions of polymer-supported nitriles
Takaya,Murahashi
, p. 991 - 994 (2007/10/03)
Catalytic activation of C-H bonds adjacent to nitriles supported by Wang resin can be performed with ruthenium dihydride complex RuH2(PPh3)4 (1). Aldol and Michael reactions of the solid-supported cyanoacetates proceed to
Synthesis and transformations of derivatives and analogs of α-cyanocinnamic acid
Ganushchak,Lesyuk,Fedorovich,Obushak,Murarash
, p. 1677 - 1682 (2007/10/03)
A reaction of ethyl α-cyanoacetate with 5-arylfurfurals, furfural, and 4-methoxybenzaldehyde in alkaline water medium gives rise to 3-substituted 2-cyanoacrylic acids in high yield. The reaction of the corresponding acyl chlorides with diethylamine and an
