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1.
We describe herein an extension of the halogenation of 1,2 or 1,3-diols via a cyclic thionocarbonate functionality by reaction with an allyl halide instead of methyl iodide, which is usually used. This investigation was successfully carried out under both conventional heating and microwave solvent-free conditions with some alditol, thioanhydroalditol, and aldose derivatives. 相似文献
2.
Singh BK Yadav AK Kumar B Gaikwad A Sinha SK Chaturvedi V Tripathi RP 《Carbohydrate research》2008,343(7):1153-1162
5-azido-5-deoxy-xylo-, ribo-, and arabinofuranoses were prepared by the reaction of the respective 5-O-(methanesulfonyl) or p-toluenesulfonyl derivatives with NaN3 in DMF. The intermediate 5-azido-5-deoxy glycofuranoses on 1,3-cycloaddition with different alkynes in the presence of CuSO4 and sodium ascorbate gave the corresponding sugar triazoles in very good yields. The synthesized sugar triazoles were evaluated for their antitubercular activity against Mycobacterium tuberculosis H37Rv, where one of the compounds displayed mild antitubercular activity in vitro with MIC 12.5 microg/mL. 相似文献
3.
Several dicarbonyl and tricarbonyl sugars were prepared by the use of fungal enzymes and the antimicrobial effects of their
N,N-diphenylhydrazine derivatives were tested. G+ bacteria were more sensitive than G- bacteria especially in the group of
disubstitued compounds. Peracetyled derivatives were not active. No inhibition of yeast growth was found. 相似文献
4.
Preparation of some starch-based neutral chelating agents 总被引:6,自引:0,他引:6
Various neutral starch derivatives have been prepared by reacting maize starch with mono- and dimethylol resins based on urea, thiourea, and melamine. The factors affecting these reactions were studied. These factors include curing duration, catalyst, and resin concentrations. The starch derivatives so prepared were used in heavy-metal removal from solutions. The sorption ability of those derivatives depends on resin type and metal ions. The sorption values of different starch derivatives follow the order (a) monomethylol resin-starch > dimethylol resin starch; (b) thiourea resin-starch > urea resin-starch > melamine resin-starch. The sorption efficiency (%) of starch derivatives increases with increasing nitrogen content, reaching a maximum value and then decreasing. The sorption values of Hg2+ (mmol/mol resin) of different starch monomethylol derivatives at the maximum values were 1135, 2624, and 2538 for urea, thiourea, and melamine derivatives, respectively. This indicates that urea derivatives act as bidentate ligands, while thiourea and melamine act as tridentate ligands. 相似文献
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Tuba Kul Kprülü Salih
kten aban Tekin Osman akmak 《Journal of biochemical and molecular toxicology》2019,33(3)
Due to a great deal of biological activities, quinoline derivatives have drawn attention for synthesis and biological activities in the search for new anticancer drug development. In this work, a variety of substituted (phenyl, nitro, cyano, N‐oxide, and methoxy) quinoline derivatives ( 3 ‐ 13 ) were tested in vitro for their biological activity against cancer cell lines, including rat glioblastoma (C6), human cervical cancer cells (HeLa), and human adenocarcinoma (HT29). 6‐Bromo‐5‐nitroquinoline ( 4 ), and 6,8‐diphenylquinoline (compound 13 ) showed the greatest antiproliferative activity as compared with the reference drug, 5‐fluorouracil (5‐FU), while the other compounds showed low antiproliferative activity. 6‐Bromo‐5‐nitroquinoline ( 4 ) possesses lower cytotoxic activity than 5‐FU in HT29 cell line. Due to its the apoptotic activity 6‐Bromo‐5‐nitroquinoline ( 4 ) has the potential to cause cancer cell death. 相似文献
8.
Abdalla MM Al-Omar MA Al-Salahi RA Amr AG Sabrye NM 《International journal of biological macromolecules》2012,51(1-2):56-63
We herein report the anti-Alzheimer activity of some synthesized heterocyclic pyrimidine and thiopyrimidine derivatives fused with steroidal structure. Twenty-one of these compounds were synthesized and conveniently screened for their anti-Alzheimer activities using of Flurbiprofen as the reference drug. Some of these compounds were demonstrated to exhibit remarkable activity and their β-amyloid (Aβ) lowering results as IC(50) values reported. 相似文献
9.
Bekhit AA Hymete A Damtew A Mohamed AM Bekhit Ael-D 《Journal of enzyme inhibition and medicinal chemistry》2012,27(1):69-77
Two series of pyridine derivatives were synthesised and evaluated for their in vivo anti-malarial activity against Plasmodium berghei. The anti-malarial activity was determined in vivo by applying 4-day standard suppressive test using chloroquine (CQ)-sensitive P. berghei ANKA strain-infected mice. Compounds 2a, 2g and 2h showed inhibition of the parasite multiplication by 90, 91 and 80%, respectively, at a dose level of 50 μmol/kg. Moreover, The most active compounds (2a, 2g and 2h) were tested in vitro against CQ-resistant Plasmodium falciparum RKL9 strains where compound 2g showed promising activity with IC(50)?=?0.0402 μM. The compounds were non-toxic at 300 and 100?mg/kg through the oral and parenteral routes, respectively. The docking pose of the most active compounds (2a, 2g and 2h) in the active site of dihydrofolate reductase enzyme revealed several hydrogen and hydrophobic interactions that contribute to the observed anti-malarial activities. 相似文献
10.
Adnan A. Bekhit Hayam M. A. Ashour Hamdy M. Abdel-Rahman Salma A. Bekhit 《Journal of enzyme inhibition and medicinal chemistry》2013,28(1):296-309
Four series of pyrazolylbenzenesulfonamide derivatives were synthesized and evaluated for their anti-inflammatory activity using cotton pellet induced granuloma and carrageenan-induced rat paw edema bioassays. Moreover, COX-1 and COX-2 inhibitory activity, ulcerogenic effect and acute toxiCIT000y were also determined. Furthermore, the target compounds were screened for their in-vitro antimicrobial activity against Eischerichia coli, Staphylococcus aureus and Candida albicans. Compounds 4-(3-Phenyl-4-cyano-1H-pyrazol-1-yl)benzenesulfonamide 9a and 4-(3-Tolyl-4-cyano-1H-pyrazol-1-yl)benzenesulfonamide 9b were not only found to be the most active dual anti-inflammatory antimicrobial agents in the present study with good safety margin and minimal ulcerogenic effect but also exhibited good selective inhibitory activity towards COX-2. A docking pose for 9a and 9b separately in the active site of the human COX-2 enzyme was also obtained. Therefore, these compounds would represent a fruitful matrix for the development of dual anti-inflammatory antimicrobial candidates with remarkable COX-2 selectivity. 相似文献
11.
Bekhit AA Ashour HM Bekhit Ael-D Abdel-Rahman HM Bekhit SA 《Journal of enzyme inhibition and medicinal chemistry》2009,24(1):296-309
Four series of pyrazolylbenzenesulfonamide derivatives were synthesized and evaluated for their anti-inflammatory activity using cotton pellet induced granuloma and carrageenan-induced rat paw edema bioassays. Moreover, COX-1 and COX-2 inhibitory activity, ulcerogenic effect and acute toxicity were also determined. Furthermore, the target compounds were screened for their in-vitro antimicrobial activity against Eischerichia coli, Staphylococcus aureus and Candida albicans. Compounds 4-(3-Phenyl-4-cyano-1H-pyrazol-1-yl)benzenesulfonamide 9a and 4-(3-Tolyl-4-cyano-1H-pyrazol-1-yl)benzenesulfonamide 9b were not only found to be the most active dual anti-inflammatory antimicrobial agents in the present study with good safety margin and minimal ulcerogenic effect but also exhibited good selective inhibitory activity towards COX-2. A docking pose for 9a and 9b separately in the active site of the human COX-2 enzyme was also obtained. Therefore, these compounds would represent a fruitful matrix for the development of dual anti-inflammatory antimicrobial candidates with remarkable COX-2 selectivity. 相似文献
12.
To develop natural-product-based pesticidal agents, a series of monosaccharide-related ester derivatives (17a–q and 18a–f), glucose (xylose)-piperic acid/piperic acid-like conjugates, were synthesized. Three-dimensional structures of compounds 17b, 17g, 17h, and 17n were unambiguously determined by single-crystal X-ray diffraction. Especially compounds 18e and 18f exhibited the most potent insecticidal and acaricidal activities against Mythimna separata and Tetranychus cinnabarinus. Their structure-activity relationships were also discussed. 相似文献
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(4R)-2,3-O-Isopropylidene-methylspiro[4,6-dideoxy-alpha-L-lyxo+ ++-hexopyranosid-4,5'-imidazolidin]-2',4'-dione and (4R)-2,3-O-isopropylidene-methylspiro[4,6-dideoxy-beta-D-ribo-h exopyranosid-4,5'-imidazolidin]-2',4'-dione were prepared under various reaction conditions starting from methyl 6-deoxy-2,3-O-isopropylidene-alpha-L-lyxo-hexopyranosid-4-++ +ulose. Corresponding alpha-amino acids methyl (4R)-4-amino-4-C-carboxy-4,6-dideoxy-alpha-L-lyxo-hexopyranosid e and methyl (4R)-4-amino-4-C-carboxy-4,6-dideoxy-beta-D-ribo-hexopyranoside were obtained from the above hydantoins by selective acid hydrolysis of the isopropylidene group, followed by basic hydrolysis of the hydantoin ring. The crystal structures of both hydantoin derivatives are also presented. 相似文献
15.
Cathepsins have emerged as promising molecular targets in a number of diseases such as Alzeimer’s, inflammation and cancer. Elevated cathepsin’s levels and decreased cellular inhibitor concentrations have emphasized the search for novel inhibitors of cathepsins. The present work is focused on the design and synthesis of some acetophenone phenylhydrazone based pyrazole derivatives as novel non peptidyl inhibitors of cathepsins B, H and L. The synthesized compounds after characterization have been explored for their inhibitory potency against cathepsins B, H and L. The results show that some of the synthesized compounds exhibit anti-catheptic activity with Ki value of the order of 10−10 M. Differential inhibitory effects have been observed for cathepsins B, H and L. Cathepsin L is inhibited more pronounced than cathepsin B and cathepsin H in that order. 相似文献
16.
Nishimura S 《Current opinion in chemical biology》2001,5(3):325-335
There has been an exponential growth in interest of the functional roles of carbohydrates and cell surface glycoconjugates in the past 10 years. The importance of glycoconjugates as mediators of biosignals has stimulated investigation into simple and versatile methods for their synthesis. The synthesis of carbohydrates and glycoconjugates by combinatorial chemistry has gained considerable interest. 相似文献
17.
The preparation of three carbonates and two carbamates of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) are described. Due to instability of the carbonates and the very low solubility of the carbamates these compounds could not be submitted to biological testing. 相似文献
18.
Kishor H. Chikhalia Dhaval B. Vashi 《Journal of enzyme inhibition and medicinal chemistry》2013,28(3):617-622
In an effort to discover new candidates with improved antimicrobial activities we report here the synthesis and in vitro biological evaluation of various series of 2-{(3,4,5-trimethoxy phenyl-1,3,4-oxadiazolyl)-5-thio}-4-(morpholino)-6-(phenyl ureido)-s-triazine (7a-i) and 2-{(3,4,5-trimethoxy phenyl-1,3,4-oxadiazolyl)-5-thio}-4-(morpholino)-6-(phenyl thioureido)-s-triazine (8a-g). Antimicrobial properties of the title compounds were investigated against two Gram ( + ve) bacteria (S. aureus, B. subtilis), two Gram ( ? ve) bacteria (P. aeruginosa, E. coli) and yeast-like fungi (C. albicans) using the broth microdilution method. 相似文献
19.
《Journal of enzyme inhibition and medicinal chemistry》2013,28(4):565-571
The synthesis of a new series of 1-[(benzazole-2-yl)thioacetyl]-3,5-diaryl-2-pyrazoline derivatives was obtained by reacting 1-(chloroacetyl)-3,5-diaryl-pyrazolines with 2-mercaptobenzimidazole/benzoxazole/benzothiazole. The chemical structures of the compounds were elucidated by 1H-NMR, 13C-NMR, and FAB+-MS spectral data. Their antifungal activities against Candida albicans, Candida glabrata, Candida utilis, Candida tropicalis, Candida krusei, and Candida parapsilosis were investigated. A significant level of activity was observed. 相似文献
20.
Chikhalia KH Vashi DB Patel MJ 《Journal of enzyme inhibition and medicinal chemistry》2009,24(3):617-622
In an effort to discover new candidates with improved antimicrobial activities we report here the synthesis and in vitro biological evaluation of various series of 2-{(3,4,5-trimethoxy phenyl-1,3,4-oxadiazolyl)-5-thio}-4-(morpholino)-6-(phenyl ureido)-s-triazine (7a-i) and 2-{(3,4,5-trimethoxy phenyl-1,3,4-oxadiazolyl)-5-thio}-4-(morpholino)-6-(phenyl thioureido)-s-triazine (8a-g). Antimicrobial properties of the title compounds were investigated against two Gram (+ ve) bacteria (S. aureus, B. subtilis), two Gram (- ve) bacteria (P. aeruginosa, E. coli) and yeast-like fungi (C. albicans) using the broth microdilution method. 相似文献