1615-02-7Relevant articles and documents
Structural elucidation and bioassays of newly synthesized pentavalent antimony complexes
Iftikhar, Tuba,Rauf, Muhammad Khawar,Sarwar, Sidra,Badshah, Amin,Waseem, Durdana,Tahir, Muhammad Nawaz,Khan, Amjad,Khan, Khalid Mohammad,Khan, Gul Majid
, p. 89 - 96 (2017)
Antimony (V) organometallics (1–5) have been synthesized with general formula [SbR′3(O2CR)2], where R' = phenyl, p-tolyl and O2CR are substituted cinnamates. These complexes have been characterized by FT-IR analysis, multinuclear (1H, 13C) NMR spectroscopy and single crystal X-ray diffraction analysis. The crystal structures of [Sb(phenyl)3(4-ClC6H4C2H2O2C)2] (1) and [Sb(p-tol)3(4-OCH3C6H4C2H2O2C)2].CHCl3 (5) displayed distorted geometry between trigonal bipyramidal and square pyramidal with monomeric structure at a five coordinated Sb center. Starting reagents and complexes were evaluated for anticancer, antileishmanial, antibacterial and alpha amylase inhibition potentials. It was observed that complexes 3, 4 and 5 showed significant (p 0.05) antileishmanial and anticancer activities against Leishmania tropica KWH23 promastigotes and HepG2 cell lines respectively. Antibacterial activity of compound 3 was also significant against E. coli (MIC: 5.55 μg/mL), K. pneumoniae (MIC: 16.66 μg/mL), S. aureus (MIC: 5.55 μg/mL) and P. aeruginosa (MIC: 50 μg/mL). Hence, these new antimony complexes can act as good drug candidates.
A novel phenylalanine ammonia-lyase from Pseudozyma antarctica for stereoselective biotransformations of unnatural amino acids
Varga, Andrea,Csuka, Pál,Sonesouphap, Orlavanah,Bánóczi, Gergely,To?a, Monica Ioana,Katona, Gabriel,Molnár, Zsófia,Bencze, László Csaba,Poppe, László,Paizs, Csaba
, p. 185 - 194 (2020/04/28)
A novel phenylalanine ammonia-lyase of the psychrophilic yeast Pseudozyma antarctica (PzaPAL) was identified by screening microbial genomes against known PAL sequences. PzaPAL has a significantly different substrate binding pocket with an extended loop (26 aa long) connected to the aromatic ring binding region of the active site as compared to the known PALs from eukaryotes. The general properties of recombinant PzaPAL expressed in E. coli were characterized including kinetic features of this novel PAL with L-phenylalanine (S)-1a and further racemic substituted phenylalanines rac-1b-g,k. In most cases, PzaPAL revealed significantly higher turnover numbers than the PAL from Petroselinum crispum (PcPAL). Finally, the biocatalytic performance of PzaPAL and PcPAL was compared in the kinetic resolutions of racemic phenylalanine derivatives (rac-1a-s) by enzymatic ammonia elimination and also in the enantiotope selective ammonia addition reactions to cinnamic acid derivatives (2a-s). The enantiotope selectivity of PzaPAL with o-, m-, p-fluoro-, o-, p-chloro- and o-, m-bromo-substituted cinnamic acids proved to be higher than that of PcPAL.
Method for preparing alpha, beta-unsaturated carboxylic acid compound
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Paragraph 0103-0104; 0463-0478, (2021/05/05)
The invention discloses a method for preparing an alpha, beta-unsaturated carboxylic acid compound, which comprises the following steps: 1) in an atmosphere containing carbon dioxide, heating and reacting a mixture containing hydrosilane and a copper catalyst to obtain a system I; and 2) adding a raw material containing alkyne and a nickel catalyst into the system I in the step 1), and heating to react. The method has the advantages of simple, easily available, cheap and stable raw materials, common, easily available and stable catalyst, mild reaction conditions, simple post-treatment, high yield and the like.
Larvicidal activity and in silico studies of cinnamic acid derivatives against Aedes aegypti (Diptera: Culicidae)
Bezerra Fran?a, Saraliny,Carine Barros de Lima, Luana,Rychard da Silva Cunha, Cristhyan,Santos Anuncia??o, Daniela,Ferreira da Silva-Júnior, Edeildo,Ester de Sá Barreto Barros, Maria,José da Paz Lima, Dimas
, (2021/07/07)
Cinnamic acid derivatives (CAD's) represent a great alternative in the search for insecticides against Aedes aegypti mosquitoes since they have antimicrobial and insecticide properties. Ae. aegypti is responsible for transmitting Dengue, Chikungunya, and Zika viruses, among other arboviruses associated with morbimortality, especially in developing countries. In view of this, in vitro analyses of n-substituted cinnamic acids and esters were performed upon 4th instar larvae (L4) of Ae. aegypti, as well as, molecular docking studies to propose a potential biological target towards this mosquitoes species. The larvicide assays proved that n-substituted ethyl cinnamates showed a more pronounced activity than their corresponding acids, in which p-chlorocinnamate (3j) presented a LC50 value of 8.3 μg/mL. Thusly, external morphologic alterations (rigid and elongated body, curved bowel, and translucent or darkened anal papillae) of mosquitoes’ group exposed to compound 3j, were observed by microscopy. In addition, an analytical method was developed for the quantification of the most promising analog by using high-performance liquid chromatography with UV detection (HPLC-UV). Molecular docking studies suggested that the larvicide action is associated with inhibition of acetylcholinesterase (AChE) enzyme. Therefore, expanding the larvicidal study with the cinnamic acid derivatives against the vector Ae. aegypti is important for finding search for more effective larvicides and with lower toxicity, since they have already shown good larvicidal properties against Ae. aegypti.