Molybdenum hexacarbonyl mediated synthesis of indolin-2-one & azaindolin-2-one under catalyst free conditions
摘要:
Syntheses of indolin-2-ones and azaindolin-2-ones have been realized. The strategy involves the formation of tosylhydrazone from tosylhydrazine and 2-amino aryl or pyridyl aldehydes/ketones which then undergo intramolecular aminocarbonylation to afford indolin-2-ones and azaindolin-2-ones. The generality of the method was demonstrated by synthesizing C3 substituted and unsubstituted indolin-2-one and azaindolin-2-one derivatives. (C) 2015 Elsevier Ltd. All rights reserved.
Method for Determining the Activity of a Protease in a Sample
申请人:Blomgren Anders
公开号:US20100021940A1
公开(公告)日:2010-01-28
There is provided a method for determining the activity of a protease in a sample. The method comprises (i) admixing said sample with a substrate, wherein the substrate has the formula (1a) wherein: R
1
is a hydrocarbyl group; R
2
is a first peptide moiety; R
3
is a second peptide moiety and X is selected from the group consisting of O, S and NH; Y
1
is a suitable substituent; Y
2
is a suitable substituent; and (ii) determining the activity of said protease by detecting the presence of a reporter having the formula H—X—R
1
, wherein: X is selected from the group consisting of O, S and NH; R
1
is a hydrocarbyl group. The substrate and reporter are useful for determining the efficacy of protease-modulators and candidate protease-modulators and in the diagnosis of a disease or disorder in a subject.
antifungal target. Using docking-based virtual screening and structure-basedinhibitor design, a series of novel SAP2 inhibitors were successfully identified. Among them, indolone derivative 24a showed potent SAP2 inhibitory activity (IC50 = 0.92 μM). It blocked fungi biofilm and hypha formation by down-regulating the expression of genes SAP2, ECE1, ALS3 and EFG1. As a virulence factor inhibitor, compound
Molybdenum hexacarbonyl mediated synthesis of indolin-2-one & azaindolin-2-one under catalyst free conditions
作者:Vikas S. Patil、Shyam S. Pal、Ramdas S. Pathare、L.K.K. Reddy、Arunendra Pathak
DOI:10.1016/j.tetlet.2015.09.123
日期:2015.11
Syntheses of indolin-2-ones and azaindolin-2-ones have been realized. The strategy involves the formation of tosylhydrazone from tosylhydrazine and 2-amino aryl or pyridyl aldehydes/ketones which then undergo intramolecular aminocarbonylation to afford indolin-2-ones and azaindolin-2-ones. The generality of the method was demonstrated by synthesizing C3 substituted and unsubstituted indolin-2-one and azaindolin-2-one derivatives. (C) 2015 Elsevier Ltd. All rights reserved.