51 research outputs found
Synthesis and anticancer activity of some 1,2,3-trisubstituted pyrazinobenzimidazole derivatives
No full textWOS: 000345518000007PubMed ID: 24456294The synthesis of some new pyrazino[1,2-a]benzimidazole derivatives and investigation of their anticancer activities were aimed in this work. Thus, 2-acetylbenzimidazole was reacted with appropriate alpha-bromoacetophenones and potassium carbonate in acetone to give 2-(2-acetyl-1H-benzimidazol-1-yl)-1-phenylethanone derivatives (3a-d). These diketone compounds were reacted with varied benzylamines in acetic acid to obtain 2-benzyl-1-methylidene-3-aryl-1,2-dihydropyrazino[1,2-a]benzimidazole derivatives (4a-t). The structures of the obtained compounds were elucidated by using IR, H-1-NMR, C-13-NMR, MS spectral data and elemental analyses results. Anticancer activities of the selected compounds were investigated in National Cancer Institute, Bethesda, MD. 3c and 4n showed remarkable anticancer activity comparing with standard drugs, melphalan and cisplatin
Synthesis and Antimicrobial Activity of Some New N-(1H-benzimidazol-2- yl)-2-mercaptoacetamide Derivatives
No full text
Background:
Due to multi-drug, extended-drug, and pandrug resistance phenotypes,
bacterial resistance to antibiotics and fungal infections are a general health issue. Particulary,
increase of fungal infections due to secondary cause of human diseases have been observed. An
extensive variety of benzimidazole derivatives have been characterized for their chemotherapeutic
significance. Benzimidazole derivatives have received important attention because of pharmacological
significance during current years, especially antimicrobial, anti-fungal, antitubercular, antioxidant,
anti-Alzheimer's disease and antihypertension activities.
Methods:
Some N-(1H-benzimidazol-2-yl)-2-mercaptoacetamide derivatives (2a-h) were
synthesised and evaluated for their antimicrobial activity. The title compounds were gained by
reacting N-(1H-benzimidazol-2-yl)-2-chloroacetamide with some substituted 2-mercapto heterocyclic
rings. The synthesised compounds were investigated for their antimicrobial activities against
C. albicans (ATCC 24433), C. krusei (ATCC 6258), C. glabrata (ATCC90030), C. parapsilosis
(ATCC 22019), E. coli (ATCC 25922), E. coli (ATCC 35218), E. feacalis (ATCC 51299),
E. feacalis (ATCC 29212), S. aureus (ATCC 25923), K. pneumoniae (ATCC 700603),
P. aeruginosa (ATCC 27853).
Results:
The compounds showed high antifungal activity when compared with standard drug
ketoconazole. In addition, all compounds (MIC 100 µg/mL) showed inhibitor activity against
P. aeruginosa at two fold concentration of chloramphenicol (MIC 50 µg/mL). Also, compounds 2a,
2c and 2e (MIC: 50 µg/mL) have equal effect against E. coli (ATCC 35218) and more effective
than other compounds (MIC of chloramphenicol: 100 µg/mL).
Conclusıon:
All compounds showed notable activity. Compounds have determined to possess higher
antifungal activity than antibacterial activity. Additionally, compounds 2a with 1-methyltetrazole,
2c with benzothiazole and 2e with 6-chlorobenzothiazole moieties were found as the most active
compounds.</jats:sec
Microwave supported synthesis of some novel 1,3-Diarylpyrazino[1,2-a] benzimidazole derivatives and investigation of their anticancer activities
No full textWOS: 000286905400048PubMed ID: 21122952The syntheses of 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and the investigation of their anticancer activities were studied. For this, 2-aryloylbenzimidazole derivatives were reacted with 2-bromoacetophenones in acetone to give 1-(2-aryl-2-oxoethyl)-2-aryloylbenzimidazoles. The resulting materials were reacted with ammonium acetate in acetic acid to obtain the aimed compound. In this reaction, microwave irradiation method was applied as the reaction conditions. Anticancer activities of the compounds obtained were investigated. It was observed that some of the compounds showed remarkable anticancer activities
New N’-Arylidene-2-[(4-Nitrophenyl)Piperazın-1-yl]Acetohydrazide Derivatives: Synthesis and Anticancer Activity Investigation
No full textWOS: 000405935700007Background: Compounds bearing ortho-hydroxy N-acyl hydrazone moiety have been reported with high anticancer activity acting by increasing the enzymatic activity of procaspase-3 in cancer cells and therefore inducing apoptosis in some tumour models. Methods: Considering this subunit's proclivity for anticancer activity we have synthesized novel N'-arylidene-2-[(4-nitrophenyl) piperazin-1-yl] acetohydrazide derivatives (3a-3n) including N-acyl hydrazone moiety with a well-known three step synthetic procedure. The antiproliferative activity of the compounds were investigated using MTT method and xCELLigence real time cell analysis system against NIH/3T3 (Mouse embryo fibroblast cell line) as healthy cell line and A549 (Human lung adenocarcinoma ephitelial cell line) as tumour cell line. Results and Conclusion: The IC50 values of final compounds were determined for 24h and 48h incubation periods. As a second stage, flow cytometric analysis was performed for selected highly active compounds (3g, 3i, 3j, 3n) on A549 cell line. Compound 3i bearing 3-chlorophenyl moiety was detected to cause apoptosis in a ratio of 54.7 %
New Cyclohexylamine-dithiocarbamate Derivatives as Potential Anti-microbial Agents
No full textWOS: 000412336400010Background: In this study, 2-(substituted-sulfanyl)-N, N-dicyclohexylacetamide derivatives (2a-2g) and 2-(dicyclohexylamino)-2-oxoethyl-1-substituted carbodithioate derivatives (2h-2m) were synthesized and screened for their antimicrobial activity. Methods: Newly synthesized compounds were screened against two gram negative bacteria (S. typhimurium and E. coli), three gram positive bacteria (S. aureus, B. cereus and L. monocytogenes), four Candida species, four Aspergillus spp. and three Penicillium spp. Among them (2a-2m), compounds 2i (2-(dicyclohexylamino)-2-oxoethyl-thiomorpholine-4-carbodithioate) and 2k (2( dicyclohexylamino)-2-oxoethyl-4-(4-methoxyphenyl) piperazine-1-carbodithioate) were detected to have higher inhibitory effect than other compounds. Results and Conclusion: Minumum inhibitor concentrations (MICs) of the compounds were determined between the range of 97.5-390 mu g/mL. Additionally, parameters determined that some physicochemical and toxic properties were predicted using computational methods
New formulae for Zagreb indices
No full textInternational Conference on Numerical Analysis and Applied Mathematics (ICNAAM) -- SEP 19-25, 2016 -- Rhodes, GREECEIn this paper, we study with some graph descriptors also called topological indices. These descriptors are useful in determination of some properties of chemical structures and preferred to some earlier descriptors as they are more practical. Especially the first and second Zagreb indices together with the first and second multiplicative Zagreb indices are considered and they are calculated in terms of the smallest and largest vertex degrees and vertex number for some well-known classes of graphs.Uludag UniversityUludag University [F-2015/17, F-2015/23]; Selcuk UniversitySelcuk UniversityThe first author was supported by the Research Fund of Uludag University project no: F-2015/17, F-2015/23. The last author is supported by Selcuk University Research Fund
Synthesis, Antibacterial, Antifungal, Antimycobacterial Activity Evaluation of Novel 1,2,4-triazole Derivatives Bearing 4-Aminophenyl Moiety
No full textWOS: 000405935700010Background: In this work, 2-[[5-(4-aminophenyl)-4-(4-substituted phenyl)-4H-1,2,4-triazol- 3-yl] thio]-1-(4-substituted phenyl) ethan-1-one derivatives (1-15) and 2-[[5-(4-aminophenyl)-4-( 4-substituted phenyl)-4H-1,2,4-triazol-3-yl] thio]-N-(4-substituted phenyl) acetamide derivatives (15-30) were synthesized using 4-aminobenzohydrazide as starting material. Methods: These compounds were screened to determine their antimicrobial activities against Gram-positive bacteria B. cereus, S. aureus, E. faecalis, L. monocytogenes; Gram-negative bacteria E. coli, P. aeruginosa, K. pneumoniae, S. typhimurium, yeasts C. parapsilosis, C. albicans, C. glabrata, C. krusei; molds A. niger, A. flavus, A. parasiticus, A. fumigatus, Rhizopus sp., A. alternate, S. rolfsii and a mycobacteria M. tuberculosis. Results and Conclusion: Compounds 2, 6, 7, 8 have displayed antituberculotic potential as much as standard drug, rifampicin. Also, compounds have exhibited moderate antibacterial and antifungal activities, contrary to expectations
Microwave supported synthesis of some novel 1,3-Diarylpyrazino[1,2-a]benzimidazole derivatives and investigation of their anticancer activities
No full texta b s t r a c t The syntheses of 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and the investigation of their anticancer activities were studied. For this, 2-aryloylbenzimidazole derivatives were reacted with 2-bromoacetophenones in acetone to give 1-(2-aryl-2-oxoethyl)-2-aryloylbenzimidazoles. The resulting materials were reacted with ammonium acetate in acetic acid to obtain the aimed compound. In this reaction, microwave irradiation method was applied as the reaction conditions. Anticancer activities of the compounds obtained were investigated. It was observed that some of the compounds showed remarkable anticancer activities
Synthesis and anticancer activity of some 1H-inden-1-one substituted (heteroaryl)acetamide derivatives
No full textWOS: 000459738100002Background: The synthesis of 2-[3/4-((6-substituted-1-oxo-2,3-dihydro-1H-inden-2ylidene) methyl)phenoxy]-N-(heteroaryl)acetamide derivatives and the investigation of their anticancer activity were studied. Methods: 2-(3/4-Hydroxybenzylidene)-6-substituted-2,3-dihydro-1H-inden-1-ones were reacted with suitable 2-chloroacetamides to give 2-[3/4-((6-substituted-1-oxo-2,3-dihydro-1H-inden-2-ylidene)methyl) phenoxy]-N-(heteroaryl) acetamide derivatives. Results: The structure elucidation of the newly synthesised 16 compounds was performed by IR, 1H-NMR, mass spectroscopic data and elemental analyses. The anticancer screening was carried out in National Cancer Institute (NCI), USA. Conclusion: Compound 3e (2-(3-((6-chloro-1-oxo-2,3-dihydro-1H-inden-2-ylidene) methyl)phenoxy)N-(thiazol-2-yl)acetamide), exhibited highest growth inhibition against the leukaemia (61.47%), non-small cell lung cancer (79.31%) and breast cancer (62.82%) cell lines.Anadolu University, Turkey (BAP) [050301]This work was supported by Anadolu University, Turkey (BAP Project No: 050301). NCI, USA is gratefully acknowledged for investigating the anticancer activity
ChemInform Abstract: Microwave Supported Synthesis of Some Novel 1,3-Diarylpyrazino[1,2-a]benzimidazole Derivatives and Investigation of Their Anticancer Activities.
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