2491-36-3Relevant articles and documents
3-Imidazolyl-substituted flavans as potential antifungal agents: Synthesis, stereochemical properties, and antifungal activity
Emami, Saeed,Foroumadi, Alireza
, p. 541 - 545 (2009)
A new series of 3-imidazolyl-substituted flavan derivatives being equipped with a N-(phenethyl)-azole scaffold as the common pharmacophore of azole antifungals, were synthesized. The stereochemical and conformational properties of compounds were also characterized by 1H-NMR data. The results of the antifungal evaluation of trans-3-imidazolyl-substituted flavan-4-ones and (Z)-trans-3-imidazolyl-substituted flavan-4-one oximes in comparison with the reference drug fluconazole indicated that most target compounds possessed significant in-vitro antifungal activities against the tested fungi, comparable or superior to fluconazole.
Synthesis, characterization, reactivity, and catalytic studies of heterobimetallic vanadium(V) complexes containing hydrazone ligands
Borthakur, Rosmita,Dhanpat, Shobha A.,Kumar, Arvind,Kurbah, Sunshine D.,Lal, Ram A.,Syiemlieh, Ibanphylla
supporting information, (2020/10/21)
Six heterobimetallic alkali metal dioxidovanadium(V) coordination polymer complexes {[M6{VO(μ-O)}2(μ-OH)4(μ4-slox/nph)].n DMF}∞ where M = Na, K, and Cs; n = 1 for (1), 0 for (2)-(6) of two dihydrazone ligands, disalicylaldehydeoxaloyldihydrazone (H4slox) and bis(2-hydroxy-1-naphthaldehyde)oxaloyldihydrazone (H4nph) are reported. All the complexes have been characterized by various physicochemical techniques such as elemental analyses, molar conductance, IR, NMR, UV–vis, and cyclic voltammetry. The IR, 1HNMR, and 13CNMR spectral data suggest that the dihydrazones are coordinated through phenolate/naphtholate oxygen, enolate oxygen, and azine nitrogen atoms to the metal centres. The structure of complex {[Na6{VO(μ-O)}2(μ-OH)4(μ4-slox)].DMF}∞ (1) is also determined by single-crystal X-ray data, which revealed that the H4slox coordinated via all possible dative sites to metal centres as tetrabasic octadentate ligand. The vanadium metal centres adopted distorted square-pyramidal coordination geometries, and the sodium atoms are also in five coordination atmospheres. The electronic spectra of the complexes showed LMCT bands in addition to intra-ligand π → π* and n → π* transitions. As evident from the cyclic voltammetry, the complexes showed two metal-centred electron transfer reactions {[(VVVV(slox)2?/VVVIV(slox)3?] and [(VVVIV(slox)3?/VVVIV(slox)4?]}, in addition to the ligand centred electron transfer reactions. Further, bovine serum albumin (BSA interaction studies of the complexes {[Na6{VO(μ-O)}2(μ-OH)4(μ4-slox)].DMF}∞ (1) and [Na6{VO(μ-O)}2(μ-OH)4(μ4-nph)]∞ (4) revealed strong binding affinity. Moreover, the catalytic studies of the complexes (1) and (4) were found to be effective for the oxidation of alcohols into their corresponding aldehydes and ketones and bromination of some organic substrates in the presence of H2O2 as an oxidizing agent.
Preparation method of neticonazole hydrochloride
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Paragraph 0075-0097; 0164-0175; 0187-0192, (2021/01/20)
The invention discloses a preparation method of neticonazole hydrochloride. The preparation method comprises the following steps: (1) taking a compound as shown in a formula III and bromopentane as reaction raw materials, reacting under an alkaline condition, extracting a product obtained by the reaction, reacting the extracted and separated organic product with hydrogen chloride to form a salt soas to obtain neticonazole hydrochloride; optionally (2) refining the obtained neticonazole hydrochloride. According to the method disclosed by the invention, the reaction conditions for preparing each intermediate, the intermediate post-treatment process and the neticonazole hydrochloride refining process are strictly controlled, so that the prepared neticonazole hydrochloride is high in purity,very low in residual solvent and impurity content, and excellent in stability.
Nucleus-independent chemical shift (NICS) as a criterion for the design of new antifungal benzofuranones
González-Chávez, Marco Martín,González-Chávez, Rodolfo,Méndez, Francisco,Martínez, Roberto,Ni?o-Moreno, Perla Del Carmen,Ojeda-Fuentes, Luis Enrique,Richaud, Arlette,Zerme?o-Macías, María de los ángeles
, (2021/08/30)
The assertion made by Wu et al. that aromaticity may have considerable implications for molecular design motivated us to use nucleus-independent chemical shifts (NICS) as an aromaticity criterion to evaluate the antifungal activity of two series of indol-4-ones. A linear regression analysis of NICS and antifungal activity showed that both tested variables were significantly related (p –1 for Candida glabrata, Candida krusei and Candida guilliermondii with compounds 15-32, 15-15 and 15-1. The MIC for filamentous fungi was 1.95 μg·mL–1 for Aspergillus niger for compounds 15-1, 15-33 and 15-34. The results obtained support the use of NICS in the molecular design of compounds with antifungal activity.
