5444-91-7Relevant academic research and scientific papers
Synthesis and characterization of 3-substituted indole derivatives as novel mannich bases
Erdag
, p. 781 - 784 (2021/04/09)
In this study, ten 3-substituted indole derivatives at the 3rdposition of indole nucleus were synthesized via Mannich reaction with microwave assisted synthesis and the conventional reflux heating method. Microwave assisted synthesis is more pr
Bioactivity-guided synthesis of gramine derivatives as new MT1 and 5-HT1A receptors agonists
Yin, Xiu-Juan,Huang, Xiao-Yan,Ma, Yun-Bao,Geng, Chang-An,Li, Tian-Ze,Chen, Xing-Long,Yang, Tong-Hua,Zhou, Jun,Zhang, Xue-Mei,Chen, Ji-Jun
, p. 610 - 622 (2017/05/26)
Twenty-four gramine derivatives were synthesized and evaluated on MT1 and 5-HT1A receptors in vitro. Among them, seven derivatives (7, 8, 16, 19, 20, 21, and 24) exhibited higher agonisting activities on MT1 or 5-HT1A
Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT6) Receptor Antagonist for Potential Treatment of Alzheimer’s Disease
Nirogi, Ramakrishna,Shinde, Anil,Kambhampati, Rama Sastry,Mohammed, Abdul Rasheed,Saraf, Sangram Keshari,Badange, Rajesh kumar,Bandyala, Thrinath Reddy,Bhatta, Venugopalarao,Bojja, Kumar,Reballi, Veena,Subramanian, Ramkumar,Benade, Vijay,Palacharla, Raghava Choudary,Bhyrapuneni, Gopinadh,Jayarajan, Pradeep,Goyal, Vinod,Jasti, Venkat
, p. 1843 - 1859 (2017/03/17)
Optimization of a novel series of 3-(piperazinylmethyl) indole derivatives as 5-hydroxytryptamine-6 receptor (5-HT6R) antagonists resulted in identification of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate (5al, SUVN-502) as a clinical candidate for potential treatment of cognitive disorders. It has high affinity at human 5-HT6R (Ki = 2.04 nM) and selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins. It has high selectivity over 5-HT2A receptor. It is orally bioavailable and brain penetrant with robust preclinical efficacy. The combination of 5al, donepezil, and memantine (triple combination) produces synergistic effects in extracellular levels of acetylcholine in the ventral hippocampus. Preclinical efficacy in triple combination and high selectivity over 5-HT2A receptors are the differentiating features which culminated in selection of 5al for further development. The Phase-1 evaluation of safety and pharmacokinetics has been completed, allowing for the initiation of a Phase-2 proof of concept study.
An efficient eco-friendly synthesis of Indole-Mannich base
Khan, Khalid Mohammed,Rahim, Fazal,Ambreen, Nida,Taha, Muhammad,Iqbal, Sarosh,Haider, Syed Moazzam,Perveen, Shahnaz
experimental part, p. 748 - 757 (2012/08/07)
An efficient and simplified protocol for three component Mannich reaction of indoles in water without using any catalyst is described. Different functionalized indole Mannich base synthesized in relatively short time with moderate to good yields. The adva
N-ARYLSULFONYL-3-SUBSTITUTED INDOLES HAVING SEROTONIN RECEPTOR AFFINITY, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITION CONTAINING THEM
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, (2010/02/07)
The present invention relates to novel N-arylsulfonyl-3-substituted indole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their geometric forms, their N-oxides, their polymorphs, their pharmaceutically acceptable
A general synthesis of 1-(dialkylaminomethyl)indoles
Love, Brian E.,Nguyen, Binh T.
, p. 1123 - 1125 (2007/10/03)
1-(N,N-Dialkylamino)methylindoles are prepared from the corresponding 1-(dialkylaminomethyl)benzotriazoles by treatment with indole and base. The aminoalkylation proceeds in high yield with good regioselectivity.
