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1.
I. V. Ukrainets L. V. Sidorenko O. V. Gorokhova N. A. Jaradat 《Chemistry of Heterocyclic Compounds》2006,42(4):475-487
Various methods of synthesizing amides of 2-hydroxy-4-imino-1,4-dihydroquinoline-3-carboxylic acids have been studied. Results
of investigations on the antitubercular and antiinflammatory activity of the obtained compounds are discussed.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 542–555, April, 2006. 相似文献
2.
I. V. Ukrainets A. A. Tkach L. V. Sidorenko O. V. Gorokhova 《Chemistry of Heterocyclic Compounds》2006,42(10):1301-1307
1-R-4-Hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid anilides have been prepared. It has been shown experimentally that
these compounds are brominated by molecular bromine in glacial acetic acid at position 4 of the anilide fragment. The antitubercular
properties of the compounds synthesized are discussed.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1508–1516, October, 2006. 相似文献
3.
I. V. Ukrainets E. V. Kolesnik L. V. Sidorenko O. V. Gorokhova A. V. Turov 《Chemistry of Heterocyclic Compounds》2007,43(3):326-333
A preparative method has been developed and the synthesis has been effected of anilides and heterylamides of 4-hydroxy-6-methyl-2-oxo-1-propyl-1,2,5,6,7,8-hexahydroquinoline-3-carboxylic
acid. A comparative analysis has been carried out of the structure and antitubercular properties of the synthesized compounds
and their analogs unsubstituted in the quinoline nucleus.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 3, pp. 405–414, March, 2007. 相似文献
4.
I. V. Ukrainets E. V. Mospanova L. V. Sidorenko 《Chemistry of Heterocyclic Compounds》2007,43(7):863-870
An improved method is reported for the synthesis of a series of 1-hydroxy-3-oxo-5,6-dihydro-3H-pyrrolo[3,2,1-ij]quinoline-2-carboxylic
acid hetarylamides. The antitubercular activity of all of the compounds prepared has been studied. The structure-biological
activity dependence revealed is discussed.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 1023–1033, July, 2007. 相似文献
5.
Some new biologically potent coumarin derivatives 7a–f, 8a–f, and 9a–f bearing modified pyridine moieties (indeno[1,2-b]pyridine, 4-azaphenanthrene and benzofuro [3,2-b]pyridine) at the sixth position were designed and synthesized. All the synthesized compounds were assayed for their antimicrobial efficiency against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Salmonella typhi, Candida albicans, and Aspergillus niger. Most of the compounds showed appreciable antimicrobial activity against the tested strains. Compounds 8b, 8c, 9b, 9d, and 9f emerged as most proficient members of the series. The antitubercular activity for all the synthesized compounds was performed against Mycobacterium tuberculosis H37Rv. Compounds 8f, 9b, and 9f exhibited promising antitubercular activity. Consequently, synthesized derivatives were found to be worthy of further investigation. 相似文献
6.
Kok Tong Wong Hasnah Osman Thaigarajan Parumasivam Unang Supratman Mohammad Tasyriq Che Omar Mohamad Nurul Azmi 《Molecules (Basel, Switzerland)》2021,26(7)
A total of fourteen pyrazoline derivatives were synthesized through cyclo-condensation reactions by chalcone derivatives with different types of semicarbazide. These compounds were characterized by IR, 1D-NMR (1H, 13C and Distortionless Enhancement by Polarization Transfer - DEPT-135) and 2D-NMR (COSY, HSQC and HMBC) as well as mass spectroscopy analysis (HRMS). The synthesized compounds were tested for their antituberculosis activity against Mycobacterium tuberculosis H37Ra in vitro. Based on this activity, compound 4a showed the most potent inhibitory activity, with a minimum inhibitory concentration (MIC) value of 17 μM. In addition, six other synthesized compounds, 5a and 5c–5g, exhibited moderate activity, with MIC ranges between 60 μM to 140 μM. Compound 4a showed good bactericidal activity with a minimum bactericidal concentration (MBC) value of 34 μM against Mycobacterium tuberculosis H37Ra. Molecular docking studies for compound 4a on alpha-sterol demethylase was done to understand and explore ligand–receptor interactions, and to hypothesize potential refinements for the compound. 相似文献
7.
A five point pharmacophore was generated using PHASE for a series of nitroaromatic compounds and their congeners as antitubercular agents. The generated pharmacophore yielded significant 3D‐QSAR model with r2 of 0.890 for a training set of 92 molecules. The model also showed excellent predictive power with correlation coefficient Q2 of 0.857 for a test set of 31 compounds. The pharmacophore indicated that presence of a nitro group, a piperazine moiety, one aromatic ring feature and two acceptor features are necessary for potent antitubercular activity. The pharmacophore was supported by electronic property analysis using density functional theory (DFT) at B3LYP/3–21*G level. Molecular electrostatic profile of the compounds was consistent with the generated pharmacophore model, particularly appearance of localized negative potential regions near both the oxygen atoms of nitro group extending laterally to the isoxazole ring system/amide bond in the most active compounds. Calculated data further revealed that all active compounds have smaller LUMO energies located over the nitro group, furan ring, and isoxazole ring/amide bond attached to it. Higher negative values of LUMO energies concentrated over the nitro group are indicative of the electron acceptor capacity of the compounds, suggesting that these compounds are prodrugs and must be activated by TB‐nitroreductase. The results obtained from this study should aid in efficient design and development of nitroaromatic compounds as antitubercular agents. © 2009 Wiley Periodicals, Inc. J Comput Chem, 2010 相似文献
8.
Vijay K. Agrawal Shahnaz Bano Keshav C. Mathur Padmakar V. Khadikar 《Journal of Chemical Sciences》2000,112(2):137-146
The paper gives a brief account of the recently introduced Szeged index (Sz). Using this index antitubercular activities of
N-2,4-difluorophenyl quinolones are subjected to quantitative structure-activity relationship analysis. The potential of Sz
related to the Wiener index (W) is critically discussed. In addition, Huckel molecular orbital energies:E
HOMO,E
LUMO andE
total were also used for comparing and modelling antitubercular activities of the quinolones. The results, based on univariate
as well as multivariate regressions, have shown that W, SZ andE
total give better results and that the correlations improve in multivariate regression analyses. 相似文献
9.
A series of new 4-thiazolidinones have been synthesized from 2-[S-(benzothiazoI-2′)]-mercapto acetic hydrazide (I) as starting
material. The reaction mechanism has been examined. These biheterocycles and their precursors were screened for their antimicrobial
activity against different strains and were also screened for antitubercular activity. 相似文献
10.
Robert Ebeh Messanga Auguste Abouem A. Zintchem Mbabi Nyemeck II Norbert Moni Ndedi Esther Del Florence Betote Diboué Patrick Hervé 《Natural product research》2018,32(16):1971-1976
The chemical investigation of the extract of the dried leaves of Rauvolfia caffra (Sond) (synonym Rauvolfia macrophylla) (Apocynaceae) led to isolation of a new glycoside derivative, rauvolfianine (1) as well as six known compounds: oleanolic acid (2), sitosterol-3-O-β-D-glucopyranoside (3), betulinic acid (4), vellosimine (5), sarpagine (6) and D-fructofuranosyl-β-(2→1)-α-D-glucopyranoside (7). Compounds 1, 2, 3, 4 and 7 were evaluated for antitubercular activity. Compounds 1 and 2 were the most active (MIC = 7.8125 and 31.25 μg/mL) towards the Isoniazid resistant strain of Mycobacterium tuberculosis AC45. Their structures and relative stereochemistry were elucidated by spectroscopic methods. 相似文献