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1.
A new series of novel compounds [10-substituted 6H, 7H-indolo[2,3-c]isoquinolin-5-one-6-yl]carbohydrazides (3a–c), 1-[10-substituted 6H, 7H-indolo[2,3-c]isoquinolin-5-one-6-yl]fomyl-, -3′,5′-dimethylpyrazoles (4a–c), -3′,5′-diphenylpyrazoles (5a–c), -3′-methylpyrazol-5′-ones (6a–c) and -1′,3′,4′-oxidiazole-2′-thiones (7a–c) linked to indoloisoquinoline at position-6 through formyl bridge was prepared. The structures of these newly synthesized compounds were confirmed by their spectral studies and elemental analysis. These compounds have been screened for their antimicrobial and antioxidant activities. Compounds 4a, 4b, 5a, 5b, 5c, 6b, 7a, and 7c exhibited the maximum zone of inhibition against A. niger, A. flavus, and A. fumigatus. Compounds 4a, 5a, 5c, 6b, 6c, 7a, and 7b showed good antibacterial activity. Compounds 4b, 4c, 5b, 5c, 6a, 6b, 7a, 7b, and 7c showed good radical scavenging activity compared with standards.  相似文献   

2.
A new series of phenolic esters 2(aj) and amides 3(ac) of 2-(1-benzofuran-2-yl) quinoline-4-carboxylic acid were synthesized by the reaction of 2-(1-benzofuran-2-yl)-quinoline-4-carboxylic acid (1) with various substituted phenols and secondary amines using ethyl-(N′,N′-dimethylamino)propyl carbodiimide hydrochloride (EDC.HCl) as a coupling agent. The newly synthesized compounds were evaluated for in vitro antioxidant and antibacterial activity. Among all tested compounds 2a, 2c, 2e, and 2h showed good chelating ability with Fe+2 ions, whereas compounds 2g and 2j exhibited good scavenging activity with DPPH free radicals. Concerning antibacterial activities compounds 2a, 2b, 2c, and 2h were found to be equipotent to ampicillin against Enterococcus sp and Staphylococcus aureus, while compound 2e is found to be as potent as ampicillin against Pantoea Dispersa and Ochrobactrum sp. amide derivatives 3(ac) were found to be less potent when compared to standard.  相似文献   

3.
A series of new pyrazoline compounds bearing a pyridyl moiety (4ai) were synthesized by condensing appropriate chalcones with hydrazine hydrate and tested for antimicrobial and antioxidant activities. According to in vitro antimicrobial activity against Bacillus subtilis, Staphylococcus epidermidis, Proteus vulgaris, Pseudomonas aeruginosa, Aspergillus niger and Penicillium chrysogenum and antioxidant activity by DPPH method, the compounds 4a, 4d, 4i and 4e, 4f, 4h showed maximum antimicrobial and antioxidant activities, respectively. Physiochemical properties and Lipinski’s ‘Rule of Five’ analysis predicted higher intrinsic quality of the synthesized compounds and revealed that these compounds have good bioavailability and druglikeness properties.  相似文献   

4.
A series of 7-hydroxy-2-aryl-6-aryldiazenyl-4H-chromen-4-one derivatives (6am) was synthesized in quantitative yields and their structures were corroborated on the basis of FT-IR, 1H, 13C NMR, ESI–MS, and elemental analysis data. The synthesized compounds were screened for in vitro antibacterial activities against a representative panel of Gram-positive and Gram-negative bacteria, as well as to evaluate their antioxidant potential using DPPH assay method. Bio-evaluation studies revealed that compounds 6c, 6d, 6e, 6j, and 6l exhibited moderate to good antibacterial activity against all the tested bacterial strains. Furthermore, from the antioxidant screening results, it has been observed that compounds 6c, 6e, and 6g manifested profound antioxidant potential (IC50 <7.68 μM) in comparison to the standard antioxidant ascorbic acid.  相似文献   

5.
The synthesis of novel series of benzofuran derivatives, containing barbitone moiety, 5-[(2/4-substitutedphenyl)(5-substituted-1-benzofuran-2-yl) methylidene]pyrimidin-2,4,6(1H,3H,5H)-trione (4ai) and thiobarbitone moiety, 5-[(2/4-substitutedphenyl)(5-substituted-1-benzofuran-2-yl)methylidene]-2-thioxodihydropyrimidin-4,6(1H, 5H)-dione (5ai) have been reported. The target compounds (4ai) and (5ai) were synthesized by the Knoevenagel condensation of (5-substituted-1-benzofuran-2-yl)(2/4-substitutedphenyl) methanone (3ai) with barbituric acid and thiobarbituric acid, respectively, in acid medium. These compounds were screened for the antimicrobial and antioxidant activities. From antimicrobial activity results it was found that compounds 4a, 5a, 4c, and 5c displayed good antibacterial and antifungal activity against all tested strains. Further, the synthesized compounds were studied for docking on the enzyme, Glucosamine-6-phosphate synthase and the compounds 4c and 5c have emerged has an active antimicrobial agent with least binding energy (?5.27 and ?4.85 kJ mol?1). Compounds 4e, 4f, 5e, and 5f showed promising free radical scavenging activity and compounds 5a and 5b showed good chelating ability with Fe2+ ions.  相似文献   

6.
Two novel series of heterocyclic compounds have been synthesized. In first series, isatin was allowed to react with substituted aromatic/cyclic carbonyl compounds to get desired mannich bases (2ae). In second series, 4,5-disubstituted oxazoles (6ap) were synthesized. Eight compounds (2c, 6a, 6e, 6f, 6i, 6j, 6m, and 6n) were screened for anticancer activity in 60 cell lines. Compound 2c, 1-[(4,7,7-trimethyl-3-oxobicyclo[2.2.1]heptan-2-yl)methyl]indoline-2,3-dione, showed maximum activity and thus, selected for further evaluation at five dose level screening. Furthermore, molecular docking studies of compounds 2c into the colchicine-binding site of tubulin, revealed possible mode of inhibition by the compound.  相似文献   

7.
A series of new 5-chloro-8-bromo-3-aryl-1,2,4-triazolo[4,3-c]pyrimidines (4aj) have been accomplished in excellent yields by the oxidative cyclization of pyrimidinylhydrazines (3aj) of various aryl aldehydes with one equivalents of iodobenzene diacetate in methanol. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, 1H NMR, 13C NMR, and mass spectral studies. Ten new compounds (4aj) were tested in vitro for their antimicrobial activity against clinically isolated strains. Variable and modest activities were observed against the investigated strains of bacteria and fungi. Compounds 4f, 4i, and 4j demonstrated good antimicrobial activity against all the tested microbial strains.  相似文献   

8.
A series of substituted pyrazole derivatives were prepared from N1-[4-(cinnamoyl) phenyl]-5-chloro-2-methoxybenzamides 2ac, which were prepared from N-(4-acetylphenyl)-5-chloro-2-methoxybenzamide as starting material. Treating of compound 2ac with methylhydrazine or phenylhydrazine afforded the corresponding N-substituted pyrazoline derivatives 3ac and 4ac, respectively. The acryloyl derivatives 2ac were reacted with hydrazine hydrate in dioxane afforded a pyrazoline 5ac, which was acetylated with acetyl chloride in dioxane to yield the N-acetyl analogue 6ac. In addition, pyrazoline 5c was reacted with morpholine in the presence of paraformaldehyde to give the corresponding N-substituted pyrazoline derivative 7. The structure assignments of the new compounds are based on chemical and spectroscopic evidence. The pharmacological screening showed that many of these compounds have less toxicity and good anti-inflammatory activities.  相似文献   

9.
The present study is concerned with the synthesis, anticancer and antimicrobial screening of several new 3-substituted or 2,3-disubstituted-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamide derivatives. Three compounds (4b, 8c, and 11b) were selected by the National Cancer Institute and were first evaluated at a single-dose primary anticancer assay against 60 human cancer cell lines for their in vitro anticancer activity. Compound 8c which passed the criteria for activity in this assay was evaluated against the full panel of 60 human cancer cell lines at five concentrations at tenfold dilutions where it showed non-selective broad-spectrum activity against all cancer cell lines. Furthermore, compounds 4b, 6, 8c, 8d, and 16 showed pronounced antibacterial activities comparable to ampicillin against P. aeruginosa. Therefore, it was concluded that compound 8c may serve as a useful lead compound in search for powerful dual anticancer-antimicrobial agents.  相似文献   

10.
A series of phenothiazine clubbed pyrazolo[3,4-d]pyrimidines have been synthesized by using the Biginelli multi-component cyclocondensation reaction and their ability to inhibit growth of Mycobacterium tuberculosis in vitro have been determined. The results show that compounds 4b, 4d, and 4f exhibited excellent anti-tubercular activity with percentage inhibition of 93, 91, and 96, respectively, at a minimum inhibitory concentration (MIC) of <6.25?μg/ml, whereas compounds 4a, 4c, 4e, 4g, and 4h exhibited moderate to good anti-tubercular activity with percentage inhibition of 75, 68, 74, 54, and 63, respectively at a MIC of >6.25?μg/ml.  相似文献   

11.
A series of β-amino carbonyl compounds containing coumarin (4ah) and benzofuran (6ai) moieties was synthesized by a three component Mannich reaction of 3-acetyl-2H-chromen-2-one (1) or 1-(1-benzofuran-2-yl) ethanone (5) with p-substituted aromatic aldehydes (2ag) and aromatic amines (3ab) in the presence of cerric ammonium nitrate as a catalyst. The newly synthesized compounds were screened for antimicrobial and antioxidant activities. Compounds 4b, 4e, 4f, 6f, 6g, and 6i showed microbial inhibition with minimal inhibition concentration ranging between 0.040 and 0.500 mg/mL, compounds 4b, 4c, 6c, 6e, and 6i showed promising free radical scavenging activity and compounds 4b, 4f, 6c, 6d, and 6h showed good chelating ability with Fe2+ ions. The synthesized compounds were studied for docking on the enzyme, glucosamine-6-phosphate synthase to predict the binding affinity and orientation at the active site of the receptor.  相似文献   

12.
New series of [1,3,4]thiadiazolo[3,2-a]pyrimidines, [1,3,4]thiadiazolo[2,3-b]quinazolines, and pyrimido[2,1-b][1,3]benzothiazoles have been synthesized and characterized by analytical and spectrometrical methods (IR, MS, 1H, and 13C NMR). Sixteen of the synthesized compounds; namely, 3a, b, 5af, 8a, b, 10, 11ac, and 13a, b were screened for antibacterial activity against Escherichia coli, Staphylococcus aureus, and Bacillus cereus. They were found to be either moderately active, slightly active or inactive against the selected microorganisms. The antifungal activity of these compounds were also tested against Candida albicans, Aspergillus fumigatus 293, and Aspergillus flavus 3375. Compound 11a showed potent antifungal activity against the three selected fungi; the rest of the tested compounds displayed either weaker activity or were completely inactive. The same compounds were examined for antiquorum-sensing activity against Chromobacterium violaceum ATCC 12472, where compounds 3a, 10, 11a, and 13a, b exhibited promising activity. The in vitro cytotoxic activity of these compounds was also studied by brine shrimp lethality bioassay, and results indicated that compounds 3a, 11a, and 13a have the highest cytotoxic activity.  相似文献   

13.
Chalcone is a unique template that is associated with several biological activities. Claisen–Schmidt condensation of olefin aldehyde 3 and various mono, disubstituted and heterocyclic acetophenones afforded novel olefin chalcones. Synthesized compounds were subjected for ADME prediction by computational method which revealed that these molecules can be considered as a potential drug. Out of the 21 compounds screened, compounds 5u, 5g, 5c and 5e have shown significant cytotoxicity against Hep 3BPN 7, compounds 5j, 5i, 5n and 5o showed good cytotoxicity against HL 60 P 58. Compounds 5f, 5c, 5e and 5b showed potent cytotoxicity against Hela B 75. Antioxidant activity was assessed using three methods, namely, 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl radical scavenging and ferric reducing antioxidant power (FRAP). The result shows that all these compounds possess significant antioxidant activity. Compounds 5k, 5s, 5a and 5c showed promising antibacterial activity. Compounds 5k, 5u and 5f could be considered as chemopreventive agents.  相似文献   

14.
A novel series of new flurbiprofen hydrazide derivatives 2-(2-fluorobiphenyl-4-yl)-N′-[(substituted phenyl/5-nitro-2-furyl)methylene]propanehydrazide (3ak), 2-(2-fluorobiphenyl-4-yl)-N-(2-substituted-4-oxo-1,3-thiazolidine-3-yl)propanamide (4ab, 4dk), 2-[2-(2-fluorobiphenyl-4-yl) propanoyl]-N-substituted hydrazinecarbothioamide (5ah) and 2-(2-fluorobiphenyl-4-yl)-N′-[(3-methyl-4-oxo-1,3-thiazolidin-2-ylidene]propanehydrazide (6ab, 6e and 6g) has been synthesized in this study. All synthesized compounds were screened for antimicrobial activity against various bacterial and fungal strains. Additionally, compounds were evaluated for the ability to inhibit Hepatitis C virus NS5B polymerase. The most active 4-thiazolidinone compound was 4k (SGK119) with 67.0 % and thiosemicarbazide compound was 5d (SGK123) with 69.50 % inhibition at 200 μM against hepatitis C virus NS5B RNA polymerase. Anticancer activity of the selected compounds (3i, 3j, 3h, 4d, 4i and 6b) was determined at a single dose towards the full panel of 60 human cancer cell lines by the National Cancer Institute (NCI). 2-(2-Fluoro-4-biphenylyl)-N-[2-[4-(trifluoromethyl)phenyl]-4-oxo-1,3-thiazolidine-3-yl]propanamide 4d, containing thiazolidinone ring, demonstrated the most marked effect with 20.80 % growth percent on leukaemia cancer cell line SR at 10?5 M. The results demonstrated that none of the compounds tested have anticandidal and antifungal activities, but two of them (4a and 4i) showed antibacterial inhibition against Micrococcus luteus, and Staphylococcus cohnii and Staphylococcus aureus, respectively.  相似文献   

15.
Reactions of chromone derivatives 14 with N-substituted hydrazines were described. Hydrazones (6, 7a, 8ac, 9be, 10e, 11e, 12) were evaluated for cytotoxicity (MTT test) against HL-60 and NALM-6 leukemia cells. Phosphorohydrazone of 3-formylchromone 8a and hydrazone of 2-amino-3-chromone derivative 11e showed appreciable cytotoxicity. The cytotoxicity indices of 8a, 11e, and 12 were higher on drug-resistant HL-60 ADR cells in comparison to HL-60. Compounds 8a and 11e were tested for their ability to induce cytochrome c translocation from mitochondria to cytosol.  相似文献   

16.
A series of asymmetric bis-1,2,4-triazoles (4al) were synthesized from respective 1,2,4-triazole-3-thiocarbohydrazides (2a, b) via base catalyzed dehydrative cyclization of thiosemicarbazide intermediates (3al). The synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, and Mass spectral studies. The asymmetric bis-1,2,4-triazole derivatives (4al) were evaluated for in vitro antioxidant activity by DPPH radical scavenging assay method. The compounds with significant antioxidant potential were evaluated for in vitro cytotoxicity by MTT assay method against HT29 (Human adenocarcinoma) and MDA-231 (Human breast cancer) cancer cell lines. All the synthesized compounds were evaluated for in vitro antibacterial activity against Bacillus subtilus (ATCC 6633), Staphylococcus aureus (ATCC-25923), Escherichia coli (ATCC-25922), and Pseudomonas aeruginosa (ATCC-27853).  相似文献   

17.
New indole analogues containing pyrido[2,3-d]pyrimidin-4-(3H)-ones (3ai), pyrazolo[3,4-b]pyridin-3-amines (4ai) and pyrido[2,3-d]pyrimidin-4-amines (5ai) were synthesized using appropriate synthetic routes. These newly synthesized compounds were screened for their antimicrobial and antioxidant activities. Compounds 3a, 3g, 4c, 4h, 4i, 5a, 5c and 5f exhibited good antibacterial and antifungal activities. The compounds 3b, 3c, 3g, 4a, 4h, 4i and 5a exhibited good radical scavenging activity. Compounds 3a and 4d exhibited good metal chelating activity compare with standards.  相似文献   

18.
In the present study, we report the synthesis, characterization of new series of thiazolo[3,2-a]pyrimidine-6-carboxylate derivatives 3af and 4af. The newly synthesized compounds were screened for in vitro antimicrobial and antiviral activities. The probable mode of action of these active compounds was determined through in silico docking study by docking the receptor methionyl-tRNA synthetase and human inosine-5′-monophosphate dehydrogenase (IMPDH) for antibacterial and antiviral activities, respectively. Among the compounds, 4c exhibited excellent in vitro antimicrobial activity against all tested strains with binding and docking energies ?35.6 and ?12.4 kcal/mol, respectively. The antiviral studies were carried out for the selected compounds in which 4a exhibited 73.69 and 54.42 % of inhibition of buffalopox and camelpox viruses, respectively. Furthermore, compound 4a showed minimum docking and binding energy along with the maximum hydrogen/hydrophobic interaction with IMPDH. The study contributes towards identification and screening of potential antimicrobial and antiviral agent’s against the pathogens.  相似文献   

19.
The synthesis of two novel series of quinol dimethyl ethers linked to either various functionalities or to some biologically active nitrogenous heterocycles is described. Nine of the newly synthesized quinol dimethyl ethers 5a, b, 9b, 10a, d, 12a, b, and 13a, b were selected by the NCI and were tested initially at a single high dose (10 μM) in the full NCI 60 cell panel. Four of the screened quinol dimethyl ethers bearing unsubstituted phenylhydrazone 5a, 4-chlorophenylhydrazone 5b, 4-chlorophenyl-3-sulfanyl-1,2,4-triazole 9b, as well as 4-chloroanilino-1,3,4-oxadiazole 12b moieties satisfied the threshold antitumor screen. 4-Chlorophenylhydrazone 5b showed very promising results and accordingly was chosen for in vivo antitumor screening. Thus, compound 5b of the series could be considered as the potential lead for development of novel anticancer agents. In addition, compounds 5a–c, 6a–c, 9a–c, 10a, b, d, e, g, h, 11a–c, 12a–c, and 13a–c were screened for their in vitro antimicrobial activity. Some of the tested compounds exhibited special high activity comparable to the reference ampicillin against Pseudomonas aeruginosa and Escherichia coli.  相似文献   

20.
Previously unknown biphenyl containing 5-phenyl-1-benzofuran-2-yl derivatives; methanones (2ai), tertiary alcohols (3al), and carbinols (4af) were synthesized and evaluated for their antimicrobial and antioxidant activities to study the effect of functionalization at the carbonyl carbon and substitution at biphenyl ring on these activities. The introduction of hydroxyl group at carbonyl carbon enhanced the antioxidant property (3a, 3g, 3h, 4a, and 4b), while antimicrobial activity decreased; the carbinol and tertiary alcohols corresponding to methanone 2a and 2b showed no antimicrobial activity. Biphenyl methanones 1, 2a, 2f, and 2g exhibited antimicrobial activity with minimal inhibitory concentration ranging between 0.001 and 0.500 mg/mL, tertiary alcohols 3a, 3g, and 3h and carbinols 4a and 4b exhibited the promising antioxidant property. The mode of action of these active compounds was carried out by docking of receptor GlcN6P synthase with newly synthesized candidate ligands 1, 2a, 2e, 2f, 2g, 2h, 3a, 3g, 3h, 4c, and 4d.  相似文献   

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