1229245-32-2Relevant academic research and scientific papers
Regioselective synthesis of 4-substituted indoles via C-H activation: A ruthenium catalyzed novel directing group strategy
Lanke, Veeranjaneyulu,Ramaiah Prabhu, Kandikere
, p. 6262 - 6265 (2013)
A highly regioselective functionalization of indole at the C-4 position by employing an aldehyde functional group as a directing group, and Ru as a catalyst, under mild reaction conditions (open flask) has been uncovered. This strategy to synthesize 4-substituted indoles is important, as this class of privileged molecules serves as a precursor for ergot alkaloids and related heterocyclic compounds.
Discovery of indol-6-yl-pyrrolo[2,3-c]pyridin-7-one derivatives as bromodomain-containing protein 4 (BRD4) inhibitors for the treatment of kidney fibrosis
Fu, Ping,Guo, Fan,Ma, Liang,Tao, Shaohua,Tao, Sibei,Zhang, Lidan,Zhao, Lifeng
, (2022/02/10)
Uncovering new therapeutics for kidney fibrosis hold promise for chronic kidney disease (CKD). Considerable studies confirmed that BRD4 inhibition ameliorated kidney injury and fibrosis. In the study, we synthesized a series of indol-6-yl-pyrrolo[2,3-c]pyridin-7-one derivatives and biologically evaluated against BRD4 for structure-activity relationship (SAR). Notably, compound 3r (ZLD2218) exhibited the most potent inhibitory activity against BRD4, with the IC50 value of 107 nM, which was comparative to 92 nM of positive control JQ-1. Importantly, at the dose of 15 and 30 mg/kg/d for consecutive 8 days, ZLD2218 alleviated kidney injury and fibrosis in unilateral ureteral obstruction (UUO) mice, with the 30 mg/kg/d being competitive to 100 mg/kd/d of JQ1. Mechanically, ZLD2218 inhibited BRD4 expression and further suppressed fibrotic signaling in the kidneys of UUO mice and TGF-β1-stimulated TCMK-1 cells. Furthermore, ZLD2218 at the dose of 30 mg/kg/d for 8 days to C57BL/6J mice did not affect liver, kidney function and organ pathological changes. Collectively, compound 3r (ZLD2218) might be a promising lead compound of BRD4 inhibitor for the treatment of kidney fibrosis.
Catalytic Enantioselective Diels-Alder Reactions of Benzoquinones and Vinylindoles with Chiral Magnesium Phosphate Complexes
Bai, Yujia,Yuan, Jinping,Hu, Xiaoyue,Antilla, Jon C.
supporting information, p. 4549 - 4553 (2019/06/27)
Tetrahydrocarbazole and its derivatives have received much attention due to the prevalence of this scaffold in natural products and their use in organic synthesis. We have developed a Diels-Alder reaction of benzoquinones and 3-vinylindoles catalyzed by c
3, 4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS
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, (2009/12/27)
The present invention relates to 3,4-substituted piperidinyl - based renin inhibitor compounds bearing at 4-position lsoqumolone and having the Formula (I) : The invention further relates to pharmaceutical compositions containing said compounds, as well a
3, 4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS
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, (2010/01/29)
The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.
