19313-88-3Relevant articles and documents
Synthesis, in silico Study and Antileishmanial Evaluation of New Selenides Derived from 7-Chloro-quinoline and N-Phenylacetamides
Huang, Min-Fu N.,Luis, José A.S.,da Silva, Alison P.,Rocha, Juliana C.,Lima, Tatjana K.S.,Scotti, Marcus T.,Scotti, Luciana,de Oliveira, Rafael F.,Souza, Helivaldo D.S.,de Athayde-Filho, Petr?nio F.,Barbosa-Filho, José M.
, p. 712 - 721 (2021/03/17)
This study describes a virtual screening performed for two series of selenides (28 compounds), derived from N-phenylacetamides chlorides and 7-chloro-quinoline, to determine their potential for leishmanicidal activity against Leishmania amazonensis and Leishmania donovani. Seven compounds were predicted as potential leishmanicides; therefore, they were synthesized from elemental selenium, as a precursor for the production of NaHSe, and subsequent reactions with 4,7-dichloro-quinoline and N-phenylacetamides chlorides were performed. The compounds were characterized by infrared (IR), 1H and 13C nuclear magnetic resonance (NMR), and sent for in vitro cytotoxicity tests against L. amazonensis and were found to be active and selective, and two compounds presented half-maximal inhibitory concentrations (IC50) of 5.67 and 10.81 μg mL-1. They also presented good interaction energies in the docking study, suggesting that may exert their effects by inhibiting the N-myristoyltransferase and O-acetylserine sulfhydrylase enzymes in parasites.
Synthesis of some 1,2,4-triazoles as potential anti-tubercular agents
Vijayaraghavan,Shirodkar
, p. 1149 - 1153 (2015/09/28)
A series of 5-(N-substituted carboxamidoethylthio)-3-(3'pyridyl)-4- amino-1,2,4-triazole derivatives 6a-j have been synthesized and evaluated for anti-tubercular activity. They are screened in-vitro at 10μg/mL concentration against Mycobacterium tuberculosis H37RV (ATCC 27294). All the compounds are showing antitubercular activity when compared with the standard drug Amikacin. Compounds 6e and 6h are found active as they displayed IC50 and IC90 values at 100μg/mL.
Synthesis and characterization of 1H-phenanthro[9,10-d]imidazole derivatives as multifunctional agents for treatment of Alzheimer's disease
Liu, Jinggong,Qiu, Jun,Wang, Mingxue,Wang, Ling,Su, Lijuan,Gao, Jinbo,Gu, Qiong,Xu, Jun,Huang, Shi-Liang,Gu, Lian-Quan,Huang, Zhi-Shu,Li, Ding
, p. 2886 - 2903 (2014/07/21)
Background Alzheimer's disease (AD) is a progressive neurodegenerative brain disorder that is characterized by dementia, cognitive impairment, and memory loss. Diverse factors are related to the development of AD, such as increased level of β-amyloid (Aβ), acetylcholine, metal ion deregulation, hyperphosphorylated tau protein, and oxidative stress. Methods The following methods were used: organic syntheses of 1H-phenanthro[9,10-d] imidazole derivatives, inhibition of self-mediated and metal-induced Aβ1-42 aggregation, inhibition studies for acetylcholinesterase and butyrylcholinesterase, anti-oxidation activity studies, CD, MTT assay, transmission electron microscopy, dot plot assay, gel electrophoresis, Western blot, and molecular docking studies. Results We synthesized and characterized a new type of 1H-phenanthro[9,10-d]imidazole derivatives as multifunctional agents for AD treatment. Our results showed that most of these derivatives exhibited strong Aβ aggregation inhibitory activity. Compound 9g had 74% Aβ1-42 aggregation inhibitory effect at 10 μM concentration with its IC50 value of 6.5 μM for self-induced Aβ1-42 aggregation. This compound also showed good inhibition of metal-mediated (Cu2 + and Fe2 +) and acetylcholinesterase-induced Aβ1-42 aggregation, as indicated by using thioflavin T assay, transmission electron microscopy, gel electrophoresis, and Western blot. Besides, compound 9g exhibited cholinesterase inhibitory activity, with its IC50 values of 0.86 μM and 0.51 μM for acetylcholinesterase and butyrylcholinesterase, respectively. In addition, compound 9g showed good anti-oxidation effect with oxygen radical absorbance capacity (ORAC) value of 2.29. Conclusions Compound 9g was found to be a potent multi-target-directed agent for Alzheimer's disease. General significance Compound 9g could become a lead compound for further development as a multi-target-directed agent for AD treatment.