149550-21-0Relevant articles and documents
Basic Ionic Liquid Promoted Domino Knoevenagel–Thia-Michael Reaction: An Efficient and Multicomponent Strategy for Synthesis of 1,3-Thiazines
Siddiqui,Rahila,Shamim, Shayna,Rai, Pragati,Shireen,Waseem, Malik A.,Srivastava, Arjita,Srivastava, Anjali
, p. 1284 - 1291 (2016)
An efficient, three-component strategy for synthesis of 1,3-thiazines with high atom economy in one-pot mediated by room temperature basic ionic liquid is described here. The strategy involves basic ionic liquid, [bmim]OH-catalyzed Knoevenagel condensatio
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.
Kinetic insights of DNA/RNA segment salts catalyzed knoevenagel condensation reaction
Li, Weina,Fedosov, Sergey N.,Tan, Tianwei,Xu, Xuebing,Guo, Zheng
, p. 3294 - 3300 (2014/12/11)
In this work, we demonstrated that (i) salts of RNA/DNA segments were capable of catalyzing Knoevenagel condensation at physiological pH 7.0 with efficiency comparable to one of the best enzymes, porcine pancreatic lipase (PPL); and (ii) a broad scope of
