19462-22-7Relevant academic research and scientific papers
The Plasmodium falciparum eIK1 kinase (PfeIK1) is central for melatonin synchronization in the human malaria parasite. Melatotosil blocks melatonin action on parasite cell cycle
Alves, Marina Rangel Rodrigues,Costa da Silva Almeida, Fahyme,Dias, Bárbara K. M.,Garcia, Celia R. S.,Jord?o, Alessandro Kappel,Nakabashi, Myna,Portella, Danielle Pagliaminuto,Ribeiro, Ramira Yuri,Schuck, Desiree C.,dos Santos, Benedito Matheus
, (2020/08/10)
Melatonin and its indoles derivatives are central in the synchronization of malaria parasites. In this research, we discovered that melatonin is unable to increase the parasitemia in the human malaria Plasmodium falciparum that lacks the kinase PfeIK1. Th
Rational design of a new class of toll-like receptor 4 (tlr4) tryptamine related agonists by means of the structure- and ligand-based virtual screening for vaccine adjuvant discovery
Honegr, Jan,Dolezal, Rafael,Malinak, David,Benkova, Marketa,Soukup, Ondrej,De Almeida, Joyce S. F. D.,Franca, Tanos C. C.,Kuca, Kamil,Prymula, Roman
, (2018/01/26)
In order to identify novel lead structures for human toll-like receptor 4 (hTLR4) modulation virtual high throughput screening by a peta-flops-scale supercomputer has been performed. Based on the in silico studies, a series of 12 compounds related to tryptamine was rationally designed to retain suitable molecular geometry for interaction with the hTLR4 binding site as well as to satisfy general principles of drug-likeness. The proposed compounds were synthesized, and tested by in vitro and ex vivo experiments, which revealed that several of them are capable to stimulate hTLR4 in vitro up to 25% activity of Monophosphoryl lipid A. The specific affinity of the in vitro most potent substance was confirmed by surface plasmon resonance direct-binding experiments. Moreover, two compounds from the series show also significant ability to elicit production of interleukin 6.
Synthesis of Nb-acyltryptamines and their 1-hydroxy-tryptamine derivatives as new α2-blockers
Yamada, Koji,Tanaka, Yoshio,Somei, Masanori
experimental part, p. 635 - 645 (2009/12/26)
Nb-Acyl- and Nb-acyl-1-hydroxytryptamines are found to be novel and structurally simple (α2-blocker for the treatment of erectile dysfunction.
Asymmetric transfer hydrogenation of imines and iminiums catalyzed by a water-soluble catalyst in water
Wu, Jiashou,Wang, Fei,Ma, Yaping,Cui, Xin,Cun, Linfeng,Zhu, Jin,Deng, Jingen,Yu, Bangliang
, p. 1766 - 1768 (2008/03/27)
The first asymmetric transfer hydrogenation of cyclic imines and iminiums in water was successfully performed in high yields and enantioselectivities with sodium formate as the hydrogen source and CTAB as an additive catalyzed by a water-soluble and recyc
PEPTIDE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, METHOD FOR PRODUCING THE SAME, USE OF SAID DERIVATIVES AND PHARMACEUTICAL COMPOSITION
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, (2008/06/13)
Derivatives of peptides of general formula or pharmaceutically acceptable salts thereof, their use as the agents possessing antioxidant, antiasthmatic, antihypoxic, antiinflammatory, antiviral, antibacterial, lipid-regulating, antitumor, antimetastatic, g
A ROMPGEL-supported N-hydroxysuccinimide: A host of acylations with minimal purification
Barrett, Anthony G. M.,Cramp, Susan M.,Roberts, Richard S.,Zecri, Frederic J.
, p. 261 - 264 (2007/10/03)
(formula presented) amides, carbamates, ureas, Weinreb amides, hydroxamic acids Yields 89-98% Purity > 95% A novel N-hydroxysuccinimide ring-opening metathesis polymer is described as a recyclable supported acyl transfer reagent. Amides, carbamates, ureas, Weinreb amides, and hydroxamic acids are all obtained in excellent yields and purities from amines with minimal purification.
Azepino [1,2,3-lm]-β-carboline compounds and pharmaceutical composition thereof
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, (2008/06/13)
An azepino[1,2,3-lm]-β-carboline compound of the formula: STR1 wherein R1 is hydrogen, cycloalkyl of 3 to 7 carbon atoms, phenyl, hydroxy, alkoxycarbonyl of 2 or 3 carbon atoms or alkanoyl of 2 or 3 carbon atoms, and A is single bond or straigh
