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1.
Nasser R. El-Brollosy 《Monatshefte für Chemie / Chemical Monthly》2008,139(12):1483-1490
The present study describes synthesis and antimicrobial evaluation of a series of novel 6-azauracil non-nucleosides. Reaction
of silylated 6-azauracils with the appropriate chloroethers gave the corresponding non-nucleosides. 1-(Allyloxymethy)-6-azauracils
and non-nucleosides bearing indanyl, cyclohexenyl, and cyclohexyl moieties were obtained via silylation of 6-azauracils followed by treatment with the appropriate acetals. Selected compounds were tested for their in vitro antimicrobial activity against a panel of standard strains of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Four compounds showed marked inhibitory activity particularly against the tested Gram-positive bacteria.
Correspondence: Nasser R. El-Brollosy, Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University,
P.O. Box 2457, Riyadh 11451, Saudi Arabia. 相似文献
2.
Silvio Cunha Fernando C. MacedoJr Giselle A. N. Costa Manoel T. RodriguesJr Rosival B. V. Verde Lourdes C. de Souza Neta Ivo Vencato Carlito Lariucci Fernando P. Sá 《Monatshefte für Chemie / Chemical Monthly》2007,138(5):511-516
Summary. The antimicrobial activity of six N-phenyl- and fourteen N-benzoylthiourea derivatives were evaluated from their Minimal Inhibitory Concentration (MIC) values using the microdilution procedure against ten microorganisms. Most of the compounds exhibited selective activity
against fungi and Gram-positive bacteria, which were very effectively inhibited by some of the tested thioureas. Additionally, SAR considerations and four novel X-ray diffraction structures of N-benzoylthioureas are included. 相似文献
3.
Nasir Ahmad Nasir Iqbal Christy Munir 《Monatshefte für Chemie / Chemical Monthly》2000,124(3):1067-1072
The synthesis and characterization of homobimetallic complexes of VO(IV), Cr(II), Co(II), Ni(II), and Cu(II) with the chiral Schiff base (1S,2S)-N,N-1,2-Diphenylethylene-bis-(5-imino-1-phenyl-1,3-hexa-nedione) is reported. The metal ions occupy both compartments of the ligand; water molecules fill the coordination spheres to provide an octahedral environment around the central atoms. The antibacterial activity of both mono- and bimetallic complexes against a number of Gram-positive as well as Gram-negative bacteria has been tested and is discussed. 相似文献
4.
Nocardicin A analogues 30, 34 , and 38 as well as the highly strained quinone methide 43 were synthesized. β -Lactam 34 was found biologically active against several Gram-negative microorganisms in vitro; pyridinium N-oxide derivative 38 possessed activity against Gram-positive S. aureus bacterium. Masked p-quinone methide β -lactam 43 exhibited significant antimicrobial activity in vitro. A mechanism involving an oxidation in vivo is proposed for the unprecedented biological properties of nocardicins. 相似文献
5.
Asu Usta Ahmet Yaşar Nagihan Yılmaz Canan Güleç Nuran Yaylı Şengül Alpay Karaoğlu Nurettin Yaylı 《Helvetica chimica acta》2007,90(8):1482-1490
Nine new thiazachalcone‐based drugs, compounds 1 – 9 , were prepared and fully characterized. The configurations of the photochemical‐dimerization products 7 – 9 were rationalized by semi‐empirical calculations. Both the experimental data and the theoretical calculations showed that the δ‐truxinic acid type dimer is the most stable isomer of all. All compounds were tested for their antibacterial and antifungal activities. The N‐alkylated congeners 4 – 6 showed strong antimicrobial activities against various bacteria and a yeast‐like fungus. The MIC and MBC values were as low as 0.1 μg/ml. All the compounds were active against the Gram‐positive bacterium Staphylococcus aureus. 相似文献
6.
A. G. B. Azebaze B. M. W. Ouahouo J. C. Vardamides A. Valentin V. Kuete L. Acebey V. P. Beng A. E. Nkengfack M. Meyer 《Chemistry of Natural Compounds》2008,44(5):582-587
The phytochemical study of the stem bark of Allanblackia gabonensis has resulted in the isolation and characterization of one new xanthone derivative, named allanxanthone D, together with ten
known compounds, including six xanthone derivatives, allanxanthone A, 1,5-dihydroxyxanthone, 1,7-dihydroxyxanthone and 1,3,6,7-tetrahydroxy-2-(3-methylbut-2-enyl)xanthone,
forbexanthone, 6-deoxyisojacareubin, one polyisoprenylated benzophenone, guttiferone F, one flavanol, epicathechin, two phytosterols,
β-sitosterol, and campesterol. The structures of these compounds were established on the basis of one- and two-dimensional
NMR homo- and heteronuclear evidence. These compounds were evaluated for their activity against Leishmania amazonensis in vitro and antimicrobial activities against a range of Gram-negative and Gram-positive bacteria.
Published in Khimiya Prirodnykh Soedinenii, No. 5, pp. 471–475, September-October, 2008. 相似文献
7.
Nasir Ahmad Nasir Iqbal Christy Munir 《Monatshefte für Chemie / Chemical Monthly》2000,131(10):1067-1072
Summary. The synthesis and characterization of homobimetallic complexes of VO(IV), Cr(II), Co(II), Ni(II), and Cu(II) with the chiral
Schiff base (1S,2S)-N,N-1,2-Diphenylethylene-bis-(5-imino-1-phenyl-1,3-hexa-nedione) is reported. The metal ions occupy both compartments of the ligand; water molecules fill
the coordination spheres to provide an octahedral environment around the central atoms. The antibacterial activity of both
mono- and bimetallic complexes against a number of Gram-positive as well as Gram-negative bacteria has been tested and is discussed.
Received March 28, 2000. Accepted May 26, 2000 相似文献
8.
E. Bayer K. H. Gugel K. Hgele H. Hagenmaier S. Jessipow W. A. Knig H. Zhner 《Helvetica chimica acta》1972,55(1):224-239
From cultures of Streptomyces viridochromogenes a new antibiotic, phosphinothricylalanyl-alanine, has been isolated. The new amino acid phosphinothricin is 2-amino-4-methyl-phosphino-butyric acid, its structure is confirmed by synthesis. The tripeptide is highly active against Gram-positive and Gram-negative bacteria and against the fungus Botrytis cinerea. Phosphinothricin is an active glutamine synthetase inhibitor. 相似文献
9.
Summary. Several derivatives of 5-arylmethylenebis(1-methyl-6-amino-2-thiouracils) and 5-aryldipyrimidopyridines were prepared by stirring
of 6-amino-1-methyl-2-thiouracil and 6-amino-1-benzyluracil with different aromatic aldehydes in ethanol in the presence of
HCl or refluxing with AcOH. On the other hand, 6-alkylthio-3,9-dimethylpurine-2-ones were synthesized by the alkylation of 3,9-dimethyl-6-thioxanthine
which was prepared by treatment of 3,9-dimethylxanthine with P2S5. The structures of the novel compounds were characterized by spectroscopic methods. The effects of the novel compounds on
both HAV and HSV type 1 were investigated. Also, some compounds showed inhibitory effects on Gram-positive and Gram-negative bacteria as well as yeast and fungi.
On leave from Chemistry Department, Faculty of Science, Zagazig University, Zagazig, Egypt 相似文献
10.
(+)-Pisiferic acid ( 1 ), an antibiotic active against Gram-negative and Gram-positive bacteria, was synthesized starting from dehydroabietic acid ( 2 ) or abietic acid ( 26 ). The terpene ring system was functionalized and a Barton reaction used to oxidize Me(20). The intermediates of this photochemical reaction were isolated and characterized. 相似文献
11.
One‐Pot Synthesis of (1,2,3‐Triazolyl)methyl 3,4‐Dihydro‐2‐oxo‐1H‐pyrimidine‐5‐carboxylates as Potentially Active Antimicrobial Agents
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Minoo Dabiri Peyman Salehi Mahboubeh Bahramnejad Majid Koohshari Atousa Aliahmadi 《Helvetica chimica acta》2014,97(3):375-383
A simple and efficient one‐pot four‐component procedure has been developed for the synthesis of a wide range of compounds containing the (triazolyl)methyl oxo‐pyrimidine‐carboxylate system from propargyl β‐keto esters, various azides, aldehydes, and urea in the presence of catalytic amounts of (AcO)2Cu/sodium ascorbate in AcOH. The method worked well with different aryl and heteroaryl aldehydes, and for a variety of substituents in the triazolyl part of the molecule. The antimicrobial activities of the products were evaluated against two Gram‐positive and Gram‐negative bacteria, and one fungus. Compound 5j was active against Staphylococcus aureus and Candida albicans. 相似文献
12.
A new series of 1-((1-(1H-benzo[d]imidazol-2-yl)ethylidene)amino)-6-((arylidene)amino)-2-oxo-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles (4a–o) have been synthesized for the development of antimicrobial agents. Newly synthesized compounds were evaluated for their in vitro antibacterial activity against Gram-positive bacteria (Pseudomonas aeruginosa, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Staphylococcus aureus), and antifungal activity (Candida albicans, Aspergillus niger, Aspergillus clavatus). These compounds were characterized by infrared, 1H NMR, 13C NMR, and mass spectra. The synthesized compounds 4b, 4e, 4 h, and 4k showed potent antimicrobial activity against tested microorganisms. 相似文献
13.
A series of novel racemic 2‐(1,3‐diaryl‐3‐hydroxypropyl)cyclohexan‐1‐ol derivatives were synthesized from 1,5‐diketones. All the synthesized compounds were characterized by spectroscopic methods. The antibacterial activities of obtained chiral 1,5‐diols were investigated against four Gram‐positive and three Gram‐negative bacteria by determining of minimum inhibitory concentrations (MICs) in vitro. Compounds 3b , 3c , and 3d were found to be active against Enterococcus faecalis and Escherichia coli. In addition, compound 3j were found to be moderately active against all tested bacterial strains. 相似文献
14.
Aydin Tavman Naz M. Agh-Atabay Sadik Guner Fahrettin Gucin Basaran Dulger 《Transition Metal Chemistry》2007,32(2):172-179
2-(5-H/Me/Cl-1H-benzimidazol-2-yl)-phenol ligands form 1:1 electrolytes, 5-coordinate monometallic complexes with iron(III) nitrate. The geometry of the [Fe(L)(OH)(H2O)2](NO3) complexes was derived from theoretical calculation in DGauss/DFT level (DZVP basis set) on CACHE. In all of the complexes
the ligands are bidentate, via one imine nitrogen atom and phenolate oxygen atom. The coordination is completed with a hydroxide ion, and two water molecules,
adopting a distorted square pyramidal geometry. The structures of the compounds were confirmed on the basis of elemental analysis,
molar conductivity, magnetic moment, FT-Raman, FT-IR (mid-IR, far-IR), EPR and u.v.–vis. The antimicrobial activities of the
free ligands, their hydrochloride salts, and the complexes were evaluated using the disk diffusion method in dimethyl sulfoxide
(DMSO) as well as the minimal inhibitory concentration (MIC) dilution method, against nine bacteria and the results are compared
with several known antibiotic agents. Antifungal activities were reported for Candida albicans, Kluyveromyces fragilis, Rhodotorula rubra, Debaryomyces hansenii, Hanseniaspora guilliermondii, and the results were referenced against nystatin, ketaconazole, and clotrimazole antifungal agents. In most cases, the compounds
tested showed broad-spectrum (Gram+ & Gram− bacteria) activities that were either more active or as potent as the references. 相似文献
15.
Here we redesigned the branches of polyamidoamine (PAMAM) dendrimers by moving the amide carbonyl group on the other side of the amide nitrogen atom, transforming the β-alaninyl-amidoethylamine branch, which easily undergoes retro-Michael reactions and renders PAMAMs intrinsically unstable, into a more stable glycyl-amidopropylamine branch. The resulting inverse PAMAM (i-PAMAM) dendrimers have the same carbon framework as PAMAMs and only differ by the position of the carbonyl group. In contrast to PAMAMs which are prepared in solution and are difficult to purify, we synthesize i-PAMAMs using high-temperature solid-phase peptide synthesis by iterative coupling and deprotection of the commercially available N,N-bis(N′-Fmoc-3-aminopropyl)glycine and purify them preparative reverse phase HPLC. Our i-PAMAM dendrimers show no detectable degradation over time. We demonstrate this new class of dendrimers with the synthesis of antimicrobial dendrimers with potent yet non-membrane disruptive activities against both Gram-negative and Gram-positive bacteria. 相似文献
16.
Ya Wu Cong‐Jun Liu Xu Liu Gui‐Fu Dai Jin‐Yu Du Jing‐Chao Tao 《Helvetica chimica acta》2010,93(10):2052-2069
Considerable interests have been attracted by isosteviol and its derivatives because of their large variety of bioactivities. In this project, a series of novel 15‐ and 16‐substituted isosteviol derivatives were stereoselectively prepared by means of functional interconversions in ring D of the tetracyclic diterpene isosteviol. All compounds synthesized were characterized by analysis of NMR, IR, HR‐MS data, and the configurations of 33 and 37 were confirmed by X‐ray crystallographic analysis. The antibacterial activities in vitro of these isosteviol derivatives were investigated; the synthetic compounds were more active against Gram‐positive than Gram‐negative bacteria, and were especially active against Bacillus subtilis. Among them, compound 27 (MIC=1.56 μg/ml) exhibited the highest antibacterial activity and thus may be exploitable as a lead compound for the development of potent antibacterial agents. 相似文献
17.
Biljana Dekić Vidoslav Dekić Niko Radulović Rastko Vukićević Radosav Palić 《Chemical Papers》2010,64(3):354-359
A series of new coumarin derivatives has been synthesized by condensation of 4-chloro-3-nitrocoumarin and the appropriate
arylamine and sulfonamide in ethyl acetate in the presence of triethylamine. The synthesized compounds were screened for their
in vitro antimicrobial activity against thirteen strains of bacteria and three fungal/yeast strains using disk diffusion assays.
They were shown to possess a wide range of activities from almost completely inactive compounds to medium active ones. (4-[(5-Chloropyridin-2-yl)amino]-3-nitro-2H-chromen-2-one) showed similar activity against Klebsiella pneumoniae as tetracycline. 相似文献
18.
The present communication deals with the synthesis of 1,3,4‐oxadiazole‐2‐thiol derivatives containing cyclic secondary amines such as morpholine, N‐methyl piperizine, and piperizine. The structural elucidation is based on the spectral data (IR, 1H NMR, and 13C NMR) .The newly synthesized compounds were then tested for their antimicrobial activity against a representative panel of micro‐organisms such as Bacillus subtilis, Escherichia coli and Candida albicans by using ciprofloxacin and fluconazole as reference drugs for bacteria and fungi, respectively. These synthesized compounds showed moderate to potential antibacterial and antifungal activity in the range of 6–50 μM against the selected bacteria and 12–50 μM against the most common fungi, respectively. 相似文献
19.
Festus Basden Chiedu Okoye Matthias Onyebuchi Agbo Chukwuemeka Sylvester Nworu Ngozi Justina Nwodo Charles Okechukwu Esimone Patience Ogoamaka Osadebe 《Natural product research》2015,29(2):109-115
Further investigation of the methanol leaf extract of Maytenus senegalensis led to the isolation of six compounds, including mayselignoside (1) and an unusual benzoyl malic acid derivative, benzoyl R-(+)-malic acid (2). Two known lignan derivatives (+)-lyoniresinol (3) and ( ? )-isolariciresinol (4), a known neolignan derivative dihydrodehydrodiconiferyl alcohol (5) and the triterpenoid, β-amyrin (6) were also isolated. The structures of these compounds were elucidated by a combination of 1D and 2D NMR and mass spectroscopy. All compounds were tested for cytotoxicity against mouse lymphoma cell line (L5178Y) and for antimicrobial activity against strains of bacteria and fungi. None of the compounds showed promising cytotoxic and/or antimicrobial activities. 相似文献
20.
Nadia A. A. Elkanzi Rania B. Bakr Amira A. Ghoneim 《Journal of heterocyclic chemistry》2019,56(2):406-416
Novel derivatives of pyrano[2,3‐b]pyridine and pyrrolo[2,3‐b]pyrano[2.3‐d]pyridine were prepared, and their structures were elucidated by spectral and elemental analyses. The newly prepared candidates were evaluated for their antimicrobial activity against Candida sp., Aspergillus multi, Aspergillus niger, Escherichia coli, and Staphylococcus aureus. All the tested compounds revealed potent to moderate activity toward all tested microorganisms; especially, candidate 10 showed comparable antifungal activity as that showed by the standard drug ketoconazole toward Candida sp., and ethyl 4‐methyl‐1,7,8,9‐tetrahydropyrano[2,3‐b]pyrrolo[2,3‐d]pyridine‐3‐carboxylate ( 12 ) was the most active compound against all the tested bacteria. Furthermore, the newly synthesized compounds are subjected to molecular docking study for the inhibition of the enzyme L‐glutamine: D‐fructose‐6‐phosphate amidotransferase [GlcN‐6‐P], which is a new target for antimicrobials to explain action mode of these target compounds as leads for discovering other antimicrobial agents. 相似文献