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1.
Dhoolesh Gangaram Kokare Krishna Naik Anupama Nevrekar Avinash Kotian Vinayak Kamat Vidyanand K. Revankar 《应用有机金属化学》2016,30(4):181-187
Mononuclear divalent complexes of Co, Ni, Cu and Zn derived from a benzofuran‐based novel hydrazone tridentate ligand were synthesized and characterized using various spectroscopic methods. Elemental analysis reveals that the metal‐to‐ligand ratio is 1:2 which is supported by mass spectrometry results. Conductivity measurements suggest that all the complexes are non‐electrolytic in nature. The ligand and complexes were evaluated for their antimicrobial potency. Bioassay of all hydrazone chelates shows enhanced activity as compared to that of the ligand. The complex with cobalt ion as the metal centre shows better activity against fungi than the standard. Also, ligand and complexes were screened for antituberculosis activity; some analogues (Ni, Cu, Zn) are eight times more active than the standard. Both ligand and complexes show moderate ability to cleave calf thymus DNA. Copyright © 2015 John Wiley & Sons, Ltd. 相似文献
2.
Nargis Jamila Melati Khairuddean Sadiq Noor Khan Naeem Khan 《Magnetic resonance in chemistry : MRC》2014,52(7):345-352
The genus Garcinia is reported to possess antimicrobial, anti‐inflammatory, anticancer, hepatoprotective and anti‐HIV activities. Garcinia hombroniana in Malaysia is used to treat itching and as a protective medicine after child birth. This study was aimed to isolate the chemical constituents from the bark of G. hombroniana and explore their possible pharmacological potential. Ethyl acetate extract afforded one new (1) and six (2–7) known 3 → 8 rotameric biflavonoids. Their structures were elucidated by UV, IR and NMR (1D and 2D) spectroscopy together with electron ionization/ESI mass spectrometric techniques and were identified as (2R, 3S) volkensiflavone‐7‐O‐rhamnopyranoside (1), volkensiflavone (2), 4″‐O‐methyl‐volkensiflavone (3), volkensiflavone‐7‐O‐glucopyranoside (4), morelloflavone (5), 3″‐O‐methyl‐morelloflavone (6) and morelloflavone‐7‐O‐glucopyranoside (7). The absolute configuration of compound 1 was assigned by circular dichroism spectroscopy as 2R, 3S. The coexistence of conformers of isolated biflavonoids in solution at 25 °C in different solvents was confirmed by variable temperature NMR studies. At room temperature (25 °C), compounds 1–7 exhibited duplicate NMR signals, while at elevated temperature (90 °C), a single set of signals was obtained. Compound 5 showed significant in vitro antioxidant activities against 1,1‐diphenyl‐2‐picrylhydrazyl and 2,2′‐azino‐bis‐3‐ethyl benzthiazoline‐6‐sulfonic acid radicals. The antibacterial studies showed that compounds 5 and 6 are the most active against Staphylococcus aureus, Bacillus subtilis and Escherichia coli. Compounds 3 and 6 also showed moderate antituberculosis activity against H38Rv. Based on the research findings, G. hombroniana could be concluded as a rich source of flavanone–flavone (3 → 8) biflavonoids that exhibit rotameric behaviour at room temperature and display significant antioxidant and antibacterial activities. Copyright © 2014 John Wiley & Sons, Ltd. 相似文献
3.
Tetramic acid derivatives and polyphenols from sponge-derived fungus and their biological evaluation
Jun-Feng Wang Xiaochu Qin Fu-Quan Xu Tianyu Zhang Shengrong Liao Xiuping Lin 《Natural product research》2015,29(18):1761-1765
Fifteen compounds, including two tetramic acid derivatives, penicillenol A1 (1) and penicillenol A2 (2), six polyphenols containing both phenolic bisabolane sesquiterpenoid and diphenyl ether units, expansols A–F (3–8), together with six phenolic bisabolane sesquiterpenoids (9–14) and diorcinol (15), were isolated from the fermentation broth of the marine-derived fungus ZSDS1-F11 isolated from the sponge Phakellia fusca Thiele collected in the Yongxing island of Xisha. Their structures were elucidated mainly by using extensive NMR spectroscopic and mass spectrometric analyses. Compounds 3–5, 7 and 8 showed potent COX-1 inhibitory activity with IC50 values of 5.3, 16.2, 30.2, 41.0 and 56.8 μM, respectively. Meanwhile, compounds 3–8 showed potent COX-2 inhibitory activity with IC50 values of 3.1, 5.6, 3.0, 5.1, 3.2 and 3.7 μM, respectively. In addition, compound 1 exhibited antituberculosis activity with 96.1% inhibition at concentration of 10 μM. 相似文献
4.
Ana Flvia Borsoi Josiane Delgado Paz Kenia Pissinate Raoní Scheibler Rambo Víctor Zajaczkowski Pestana Cristiano Valim Bizarro Luiz Augusto Basso Pablo Machado 《Molecules (Basel, Switzerland)》2021,26(5)
Tuberculosis (TB) has been described as a global health crisis since the second half of the 1990s. Mycobacterium tuberculosis (Mtb), the etiologic agent of TB in humans, is a very successful pathogen, being the main cause of death in the population among infectious agents. In 2019, it was estimated that around 10 million individuals were contaminated by this bacillus and about 1.2 million succumbed to the disease. In recent years, our research group has reported the design and synthesis of quinoline derivatives as drug candidates for the treatment of TB. These compounds have demonstrated potent and selective growth inhibition of drug-susceptible and drug-resistant Mtb strains. Herein, a new synthetic approach was established providing efficient and rapid access (15 min) to a series of 4-alkoxy-6-methoxy-2-methylquinolines using ultrasound energy. The new synthetic protocol provides a simple procedure utilizing an open vessel system that affords the target products at satisfactory yields (45–84%) and elevated purities (≥95%). The methodology allows the evaluation of a larger number of molecules in assays against the bacillus, facilitating the determination of the structure–activity relationship with a reduced environmental cost. 相似文献
5.
S. G. Taran I. V. Ukrainets L. V. Sidorenko O. V. Gorokhova N. A. Jaradat 《Chemistry of Heterocyclic Compounds》2000,36(8):944-947
Treatment of 1-R-2-oxo-4-hydroxyquinolin-3-ylamides of -halogen-substituted carboxylic acids with sodium methoxide leads to the formation of 2-R-3-oxomorpholino-[5,6-c]-6-R-quinolin-5-ones. The antituberculosis activity of the compounds synthesized was studied.For Communication 43, see [1].National Pharmaceutical Academy of Ukraine, Kharkov 310002; e-mail: igor@uiv.kharkov.ua. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1080–1083, August, 2000. 相似文献
6.
M. I. Merlani L. Sh. Amiranashvili K. G. Mulkidzhanyan A. R. Shelar F. V. Manvi 《Chemistry of Natural Compounds》2008,44(5):618-620
The antituberculosis activity of several steroidal compounds of various structure was studied. Severa compounds that were
active toward M. tuberculosis were found in in vitro tests.
Translated from Khimiya Prirodnykh Soedinenii, No. 5, pp. 500–501, September-October, 2008. Original article submitted July
10, 2008. 相似文献
7.
N. C. Desai Amit Trivedi Hardik Somani Krunalsinh A. Jadeja Darshita Vaja Laxman Nawale 《合成通讯》2018,48(5):524-540
A series of pyridine clubbed 1,3,4-oxadiazole derivatives were efficiently synthesized, characterized by standard spectral techniques and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra and Mycobacterium bovis BCG in active and dormant state using an established methods. Compounds 5a, 5m, and 5t were identified as the most active compounds against MTB. Molecular docking was performed against MTB enoyl-ACP (CoA) reductase (FabI/ENR/InhA) enzyme to predict the binding modes and affinity. The theoretical predictions from molecular docking could establish a link between the observed biological activity and the binding affinity shedding light into specific bonded and non-bonded interactions influencing the activity. The active compounds were studied for cytotoxicity against three cell lines and were found to be non-cytotoxic. Specificity of these compounds was checked by screening them for their antibacterial activity against four bacterial strains. 相似文献
8.
A series of newly synthesized coumarin‐based mixed‐ligand copper complexes with 1,10‐phenanthroline (Ph) were investigated by means of thermogravimetry, differential thermogravimetry, differential scanning calorimetry (DSC), electronic spectra and magnetic measurements. Structural and spectroscopic properties of neutral bidentate ligands as well as all complexes were studied on the basis of mass spectra, NMR (1H and 13C) spectra, FT‐IR spectrophotometry and elemental analyses. IR spectral data suggest tetra‐coordinated N2O2 bonding of ligand toward metal ion. Dynamic scan of DSC experiments for copper complexes were obtained at different heating rates (2.5–20°C min?1). Isoconversion methods of Kissinger and Ozawa were used for the determination of the pre‐exponential factor (A), activation energy (Ea) and order of reaction (n). Kinetic parameters for second‐step degradation obtained by Kissinger's and Ozawa's methods are in good agreement. The results indicate that complexes are much stronger free radical scavenger and antioxidant compounds than ligands. Antimycobacterial screening of ligand and its copper compound against Mycobacterium tuberculosis shows clear enhancement in antitubercular activity upon copper complexation. Also good antimicrobial activities of the complexes against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Salmonella typhus, Aspergillus niger, Candida albicans and Aspergillus clavatus have been found compared to its free ligands. Copyright © 2012 John Wiley & Sons, Ltd. 相似文献
9.
Bedaquiline is a novel adenosine triphosphate synthase inhibitor anti-tuberculosis drug. Bedaquiline belongs to the class of diarylquinolines, which are antituberculosis drugs that are quite different mechanistically from quinolines and flouroquinolines. The fact that relatively similar chemical drugs produce different mechanisms of action is still not widely understood. To enhance discrimination in favor of bedaquiline, a new approach using eight-score principal component analysis (PCA), provided by a ChemGPS-NP model, is proposed. PCA scores were calculated based on 35 + 1 different physicochemical properties and demonstrated clear differences when compared with other quinolines. The ChemGPS-NP model provided an exceptional 100 compounds nearest to bedaquiline from antituberculosis screening sets (with a cumulative Euclidian distance of 196.83), compared with the different 2Dsimilarity provided by Tanimoto methods (extended connective fingerprints and the Molecular ACCess System, showing 30% and 182% increases in cumulative Euclidian distance, respectively). Potentially similar compounds from publicly available antituberculosis compounds and Maybridge sets, based on bedaquiline’s eight-dimensional similarity and different filtrations, were identified too. 相似文献
10.
Anisimova Y.V. Gelperina S.I. Peloquin C.A. Heifets L.B. 《Journal of nanoparticle research》2000,2(2):165-171
This is the first report evaluating the nanoparticle delivery system for three antituberculosis drugs: isoniazid, rifampin, and streptomycin. The typical particle size is 250 nm. We studied accumulation of these drugs in human monocytes as well as their antimicrobial activity against Mycobacterium tuberculosis residing in human monocyte-derived macrophages. Nanoparticle encapsulation increased the intracellular accumulation (cell-association) of all three tested drugs, but it enhanced the antimicrobial activity of isoniazid and streptomycin only. On the other hand, the activity of encapsulated rifampin against intracellular bacteria was not higher than that of the free drug. 相似文献