32542-59-9Relevant articles and documents
A Highly Regio- and Diastereoselective Four-Component Reaction to Construct Polycyclic Bispiroindolines from 2-Isocyanoethylindoles and Isocyanates
Li, Longhai,Liu, Jiaxin,Shi, Min
, p. 7076 - 7079 (2018)
A one-pot multicomponent domino reaction between 2-isocyanoethylindoles and isocyanates for the diastereoselective construction of polycyclic bispiroindolines was developed. Fused polycyclic bispiroindolines containing two contiguous spiral atoms were afforded in moderate to good yields with excellent regio- and diastereoselectivities through a four-component Ugi-type reaction (U-4CR) under mild conditions.
Design, synthesis and biological evaluation of N-substituted indole-thiazolidinedione analogues as potential pancreatic lipase inhibitors
George, Ginson,Auti, Prashant S.,Paul, Atish T.
, p. 49 - 59 (2021/05/04)
Pancreatic Lipase (PL) is a key enzyme responsible for the digestion of 50%–70% of dietary triglycerides, hence its inhibition is considered as a viable approach for the management of obesity. A series of indole-TZD hybrid analogues were synthesized, characterized and evaluated for their PL inhibitory activity. Knoevenagel condensation of various substituted indole-3-carboxaldehyde with substituted thiazolidinediones resulted in the formation of titled analogues. Analogues 6d and 6e exerted potent PL inhibitory activity (IC50-6.19 and 8.96?μM, respectively). Further, these analogues exerted a competitive mode of PL inhibition. Moreover, molecular modelling studies were in agreement with the in vitro results (Pearson's r?=.8682, p?.05). The fluorescence spectroscopic analysis further supported the strong binding affinity of these analogues with PL. A molecular dynamics study (20?ns) indicated that these analogues were stable in a dynamic environment. Thus, the present study highlighted the potential role of indole-thiazolidinedione hybrid analogues as potential PL inhibitors and further optimization might result in the development of new PL inhibitory lead candidates.
COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH
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Page/Page column 43-44, (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.