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Synthesis and biological activity of some triazole-bearing benzimidazole derivatives  [PDF]
K. F. ANSAR,C. LAL,R. K. KHITOLIYA
Journal of the Serbian Chemical Society , 2011,
Abstract: A number of N’-(arylmethylidene)-2-(2-methyl-1H-benzimidazol-1-yl)acetohydrazide and 4-aryl-5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-4H-1,2,4-triazole-3-thiol derivatives were synthesized by incorporating various aromatic and heterocyclic substituents on 2-methyl-1H-benzimidazole. The structures of all the synthesized compounds were elucidated based on their elemental analyses and spectral data. The in vitro activities of these compounds against bacteria and fungi were evaluated by the disc diffusion and the minimum inhibitory concentration (MIC) methods. Some of the synthesized derivatives were found to be as active as kanamycin (standard drug).
Synthesis of some pyrazolo[3,4-d]pyrimidines and their fused triazole and tetrazole derivatives
SAMIRA A. SWELAM,OSAMA I. ABD EL-SALAM,MAGDI E. A. ZAKI
Journal of the Serbian Chemical Society , 1999,
Abstract: Reaction of 2 with different reagents, namely formic acid, acetic anhydride and trichloroacetonitrile, yielded pyrazolo[3,4-d]pyrimidine derivatives 3, 5 and 6, respectively. Pyrazolo[3,4-d]pyrimidine m-thiazine(7) and 2,4-(1H,3H)dithione (8) derivatives were formed by the action of carbon disulfide on 2, depending on the reaction medium. Interaction of 7 with hydrazine hydrate yielded the aminoimino derivative 9 which reacted with acetic anhydride, triethyl orthoacetate and/or appropriate aldehydes to give 11, 12 and 13a,b, respectively. Methylation of compound 8 gave 14, which reacted with hydrazine hydrate to afford the monohydrazino derivative 15. Reaction of 15, with formic acid and nitrous acid afforded pyrazolo[4,3-e]triazolo[1,5-c]pyrimidine (16) and pyrazolo[4,3-e]tetrazolo-[1,5-c]pyrimidine (17) derivatives, respectively. The structures of products 3-17 were identified in light of their elemental analyses and spectra data.
Synthesis of New Derivatives of Heterocyclic Compounds Containing Pyridine, Pyrimidine and Triazole Ortho-Fused to Isoquinoline Moiety  [cached]
Hamdi M. Hassaneen,Nada M. Abunada,Huwaida M. E. Hassaneen,Omar A. Miqdad
International Journal of Chemistry , 2012, DOI: 10.5539/ijc.v4n3p86
Abstract: 4-Amino-9,10-dimethoxy-2-phenyl-6,7-dihydro-2(H)-pyrido[2,1-a]isoquinoline-1,3-dicarbonitrile derivatives 4a-c were obtained from the reaction of 6,7-dimethoxy-3,4-dihydroisoqinoline-1-acetonitrile 1 with arylidenemalononitrile 2a-c in boiling acetonitile in the presence of piperidine. The reaction of 4a-c with triethyl orthoformate in acetic anhydride at reflux give the ethoxymethyleneamino derivatives 5a-c. Compounds 5a-c were reacted with hydrazine hydrate and give the corresponding 4-amino-3-imino-2-aryl-3,4,8,9-tetrahydro-2(H)-pyrimido[5?,4?:5,6]pyrido[2,1-a]isoquinoline-1-carbonitrile derivatives 6a-c. Refluxing compound 6a in an excess of triethyl orthoformate give 7a. When compounds 6a-c were refluxed with acetic anhydride or benzoyl chloride in pyridine, they afford the corresponding 4-methyl and 4-phenyl derivatives 8a-c and 9a-c, respectively. Compound 6a was refluxed in diethyloxalate and give product 10. Also, the reaction of 6a with C-acylhydrazonoyl halides 13a,b in refluxing chloroform in the presence of triethylamine afford 14a,b. Correct elemental analyses and spectral data (IR, 1H NMR, 13C NMR and MS) confirm the structure of the synthesized compounds.
Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties  [PDF]
Bedia Kocyigit-Kaymakcioglu,Ahmet Ozgur Celen,Nurhayat Tabanca,Abbas Ali,Shabana I. Khan,Ikhlas A. Khan,David E. Wedge
Molecules , 2013, DOI: 10.3390/molecules18033562
Abstract: A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity. Triazole derivatives 3a– e and 4a– e were synthesized by reacting thiocarbohydrazide with thiourea and urea compounds 1a– e and 2a– e, respectively, in a 130–140 °C oil bath. The proposed structures of all the synthesized compounds were confirmed using elemental analysis, UV, IR, 1H-NMR and mass spectroscopy. All compounds were evaluated for antifungal activity against plant pathogens, larvicidal and biting deterrent activity against the mosquito Aedes aegypti L. and in vitro cytotoxicity and anti-inflammatory activity against some human cell lines. Phomopis species were the most sensitive fungi to these compounds. Compounds 1b, 1c, 3a and 4e demonstrated selectively good activity against Phomopis obscurans and only 1b and 4e showed a similar level of activity against P. viticola. Compound 3d, with a LD 50 value of 67.9 ppm, followed by 1c (LD 50 = 118.8 ppm) and 3e (LD 50 = 165.6 ppm), showed the highest toxicity against Aedes aegypti larvae. Four of these compounds showed biting deterrent activity greater than solvent control, with the highest activity being seen for 1c, with a proportion not biting (PNB) value of 0.75, followed by 1e, 2b and 1a. No cytotoxicity was observed against the tested human cancer cell lines. No anti-inflammatory activity was observed against NF-kB dependent transcription induced by phorbol myristate acetate (PMA) in human chondrosarcoma cells.
Synthesis and Biological Activity of Some Novel Derivatives of 4-Amino-3-(D-galactopentitol-1-yl)-5-mercapto-1,2,4-triazole  [PDF]
Jian-yu Jin,Li-xue Zhang,An-jiang Zhang,Xin-Xiang Lei,Jiang-Hai Zhu
Molecules , 2007, DOI: 10.3390/12081596
Abstract: To discover new 1,2,4-triazole derivatives which may possess significant biological activities, we synthesized a series of novel 6-aryl-3-(D-galactopentitol-1-yl)- 7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazines and 4-(arylmethylidene)amino-5-(D-galactopentitol- 1-yl)-3-mercapto-4H-1,2,4-triazoles from 4-amino-3-(D-galactopentitol-1-yl)-5- mercapto-1,2,4-triazole. All the title compounds were characterized by elemental analysis, IR, 1H- and 13C-NMR. Plant growth-regulating activity tests showed that these compounds have remarkable effects on the growth of radish and wheat.
Biological evaluation of some triazole and triazolothiadiazine derivatives
Usama Abu Mohsen
Marmara Pharmaceutical Journal , 2012,
Abstract: Triazole and triazoles fused with six-membered ring systems are found to possess diverse applications in the field of medicine, agriculture and industry. The 1,2,4-triazole and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazines derivatives were synthesized as cholinesterase inhibitors. The reaction of 1H-indol-3-acetic acid with thiocarbohydrazide gave the 4-amino- 3-mercapto-5-[(1H-indol-3-yl)methyl]-4H-1,2,4-triazole. The reaction of triazole with arylaldehydes in ethanol gave the 4-arylideneamino-3-mercapto-5-[(1H-indol-3-yl)methyl]-4H- 1,2,4-triazoles. The 3-[(1H-indol-3-yl)methyl]-6-aryl-7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazines were obtained by condensing triazole with phenacylbromides in absolute ethanol. The chemical structures of the compounds were elucidated by IR, 1H-NMR and FAB+-MS spectral data and elemental analysis. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman's spectrophotometric method. Compounds 1b and 1c can be identified as promising anticholinesterase agents due to their inhibitory effect on AChE with IC50 value of 96.45±8.14 and 76.24±6.42 μM respectively when compared with Donepezil (IC50 =0.056±0.001μM).
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF SOME NOVEL 1,2,4-TRIAZOLE [3,4-B][1,3,4] THIADIAZOLE DERIVATIVES  [cached]
Kratika Shrivastva,Vivek Daniel,Pramod S. Kunwar,Swapnil Goyal
Journal of Global Pharma Technology , 2010, DOI: 10.1234/jgpt.v2i1.85
Abstract: Several 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were prepared by condensation of 4-amino-5-(2-(4-isobutyl phenyl) propyl)-4H-1,2,4-triazole-3-thiol (4) with acetic acid, substituted aromatic acids, phenyl isothiocynate, pyridine and urea through a one-pot reaction. These compounds were investigated for their antibacterial, antifungal, analgesic and antihelmentic. Some compound showed analgesic activity as compared to ibuprofen. Some of the tested compounds also showed moderate antimicrobial activity against tested bacterial and fungal strains. These compound show better antihelmentic activity as compared to albendazole.
Synthesis and studies of the biological activity of novel pyrimido fused acridine derivatives
BHAVESH B. PATEL,RANJAN G. PATEL,MANISH P. PATEL
Journal of the Serbian Chemical Society , 2006,
Abstract: Anthranilic acid was reacted with various substituted 6-bromoquinazolinones in the presence of Cu-powder and anhydrous potassium carbonate in DMF to give acid intermediates (Ullmann Type-II condensation). All these acids were then cyclized in phosphorus oxychloride to give 11-chloropyrimido[4,5-b]acridin-4(3H)-ones. All the synthesized compounds were identified by conventional methods (1H-NMR, IR, elemental analysis) and were screened for their antimicrobial activity on some bacterial and fungal cultures. The results were compared with standard bactericides and fungicides. All the synthesized compounds exhibited moderate antibacterial and antifungal activity.
SYNTHESIS AND In vitro ANTIMICROBIAL ACTIVITY OF SOME TRIAZOLE DERIVATIVES
MISHRA,RAVINESH; KUMAR,RAJIV; KUMAR,SURESH; MAJEED,JASEELA; RASHID,MOHD; SHARMA,SAMEER;
Journal of the Chilean Chemical Society , 2010, DOI: 10.4067/S0717-97072010000300019
Abstract: some 4-[{1-(substituted)methylidine}-amino]-3-(4-pyridyl)-5-mercapto-4h-1,2,4-triazol (3a- 3f) and n-[5-(4-substituted)-1h-1,2,3-triazol-1-yl] isonicotinamide derivatives (5a- 5e) were synthesized by a sequence of reactions starting from isonicotinic acid hydrazide and is illustrated in scheme 1 and 2. the antibacterial and antifungal activities of newly synthesized compounds were tested by the disc diffusion method using nutrient agar medium against various microorganisms such as gram positive staphylococcus aureus and bacillus subtilis, gram negative escherichia coli and the fungi aspergillus niger and candida albicans. ciprofloxacin and fluconazole at 50 μg/ml were used as standard drugs for antibacterial and antifungal activities, respectively. all the synthesized compounds showed significant activity against various microorganisms.
SYNTHESIS AND In vitro ANTIMICROBIAL ACTIVITY OF SOME TRIAZOLE DERIVATIVES  [cached]
RAVINESH MISHRA,RAJIV KUMAR,SURESH KUMAR,JASEELA MAJEED
Journal of the Chilean Chemical Society , 2010,
Abstract: Some 4-[{1-(substituted)methylidine}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazol (3a- 3f) and N-[5-(4-substituted)-1H-1,2,3-triazol-1-yl] isonicotinamide derivatives (5a- 5e) were synthesized by a sequence of reactions starting from isonicotinic acid hydrazide and is illustrated in scheme 1 and 2. The antibacterial and antifungal activities of newly synthesized compounds were tested by the disc diffusion method using nutrient agar medium against various microorganisms such as gram positive Staphylococcus aureus and Bacillus subtilis, gram negative Escherichia coli and the fungi Aspergillus niger and Candida albicans. Ciprofloxacin and Fluconazole at 50 μg/mL were used as standard drugs for antibacterial and antifungal activities, respectively. All the synthesized compounds showed significant activity against various microorganisms.
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