scholarly journals Design, Synthesis, and In Vitro Antimicrobial Evaluation of Fused Pyrano[3,2-e]tetrazolo[1,5-c]pyrimidines and Diazepines

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Sankari Kanakaraju ◽  
P. Sagar Vijay Kumar ◽  
Bethanamudi Prasanna ◽  
G. V. P. Chandramouli
Keyword(s):  
Carbon Disulfide ◽  
Phenacyl Bromide ◽  
Mass Spectral Data ◽  
Design Synthesis ◽  
Mass Spectral ◽  
H Nmr ◽  
Elemental Analyses ◽  
Antimicrobial Evaluation ◽  
C Nmr

A series of novel pyranochromene-containing tetrazoles fused with pyrimidinethiones, pyrimidines, and diazepines 3a–f, 4a–f, and 5a–f were synthesized by condensation of the corresponding tetrazoles 2a–f with carbon disulfide, benzaldehyde, and 4-methoxy phenacyl bromide, respectively. The compound 2a–f was obtained by reaction of pyrano[3,2-c]chromenes 1a–f with sodium azide. The structures of the newly synthesized compounds 2a–f to 5a–f were established on the basis of their elemental analyses, IR, 1H NMR, 13C NMR, and mass spectral data. All of the title compounds were subjected to in vitro antibacterial testing against four pathogenic strains and antifungal screening against two fungi. Preliminary results indicate that some of them exhibited promising activities and that they deserve more consideration as potential antimicrobials.

The Synthesis and Anticancer Activities of Peptide 5-fluorouracil Derivatives

2009 ◽  
Vol 2009 (4) ◽  
pp. 261-264 ◽  
Author(s):  
Xiaowei Yan ◽  
Maolin Hu ◽  
Qian Miao ◽  
Shun Wang ◽  
Kejian Zhao
Keyword(s):  
Cell Lines ◽  
Mass Spectra ◽  
Anticancer Activities ◽  
H Nmr ◽  
Elemental Analyses ◽  
C Nmr

A new series of peptide 5-fluorouracil derivatives was designed and synthesised in order to test in vitro anticancer activities. The results indicated that peptide 5-fluorouracil derivatives possessed anticancer activities against human HL-60 and Bel-7402 cell lines. The structures of the compounds were determined by means of 1H NMR, 13C NMR, IR, mass spectra and elemental analyses.

Synthesis and characterization of N-glucosylated dithiadiazepine derivatives through carbon-sulfur bond formation

2015 ◽  
Vol 21 (5) ◽  
pp. 269-272 ◽  
Author(s):  
Snehal A. Chavan ◽  
Avinash G. Ulhe ◽  
Baliram N. Berad
Keyword(s):  
Bond Formation ◽  
Synthesis And Characterization ◽  
Mass Spectral ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
New Compounds ◽  
Sulfur Bond ◽  
C Nmr

AbstractNew 4,7-bis(arylamino)-2-tetra-O-acetyl-β-d-glucopyranosylimino-1,3,5,6-dithiadiazepines were synthesized via reaction of N-tetra-O-acetyl-β-d-glucopyranosyl isocyanodichloride with 1,6-diaryl-2,5-dithio-bis-ureas without using any catalyst. Thus, the synthesis of 7-membered heterocycles containing two sulfur and two nitrogen atoms through carbon-sulfur bond formation was explored. The chemical structures of these new compounds were elucidated by IR, 1H NMR, 13C NMR, mass spectral, and elemental analyses.

scholarly journals Approach for the Synthesis of Potent Antimicrobials Containing Pyrazole, Pyrimidine and Morpholine Analogues

2016 ◽  
Vol 69 ◽  
pp. 87-96 ◽  
Author(s):  
Nisheeth C. Desai ◽  
Bonny Y. Patel ◽  
Bharti P. Dave
Keyword(s):  
Antimicrobial Activity ◽  
Dilution Method ◽  
Mass Spectral ◽  
H Nmr ◽  
Sar Studies ◽  
Mueller Hinton ◽  
Morpholine Derivatives ◽  
Mueller Hinton Broth ◽  
C Nmr

The present study is in the interest of some synthesized novel derivatives containing 4-(1,3-diphenyl-1H-pyrazol-4-yl)-N-(morpholinomethyl)-6-arylpyrimidin-2-amines pooled with different bio-active heterocycles such as pyrazole, pyrimidine and morpholine derivatives. The structures of newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR and mass spectral data. The synthesized compounds were evaluated for their in vitro antimicrobial activity against different bacterial and fungal strains using Mueller-Hinton Broth dilution method. On the basis of SAR studies, it was observed that the presence of electron withdrawing groups remarkably enhanced the antimicrobial activity of synthesized compounds.

scholarly journals Synthesis of New Bicyclic Hydroxamic Acids with Cytotoxic Activity

2018 ◽  
Vol 61 (4) ◽  
Author(s):  
Iker S. Escalona-Torres ◽  
Francisco Yuste ◽  
Rubén Sánchez-Obregón
Keyword(s):  
Cytotoxic Activity ◽  
Nitro Group ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Hydroxamic Acids ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
C Nmr

Six new bicyclic hydroxamic acids were synthesized through an uncommon nitro group rearrangement between β-nitrostyrenes and dimedone. The structures of all the new synthesized compounds were confirmed using a combination of FTIR, <sup>1</sup>H NMR, <sup>13</sup>C NMR and mass spectral data. Likewise, the cytotoxic activity of the obtained products was evaluated in six different cancer cell lines. Two compounds showed significant potency on two cancer cell lines with IC50 between 9.31±0.1 and 23.38±0.9 μM.

scholarly journals 1H-Benzimidazole derivatives as mammalian DNA topoisomerase I inhibitors.

2007 ◽  
Vol 54 (3) ◽  
pp. 561-565 ◽  
Author(s):  
A Selcen Alpan ◽  
H Semih Gunes ◽  
Zeki Topcu
Keyword(s):  
Topoisomerase I ◽  
Biological Properties ◽  
Benzimidazole Derivatives ◽  
Type I ◽  
Mass Spectral Data ◽  
Dna Topoisomerase ◽  
Mass Spectral ◽  
Elemental Analyses ◽  
Supercoil Relaxation

Benzimidazole is one of the most important heterocyclic groups manifesting various biological properties, such as antibacterial, antifungal, antimicrobial, antiprotozoal and antihelmintic activities. Several benzimidazole derivatives are also active as inhibitors of type I DNA topoisomerases. In this study, three 1H-benzimidazole derivatives with different electronic characteristics at position 5-, namely 5-chloro-4-(1H-benzimidazole-2-yl)phenol (Cpd I), 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) and 4-(1H-benzimidazole-2-yl)phenol (Cpd III), were synthesized and evaluated for their effects on mammalian type I DNA topoisomerase activity using quantitative in vitro plasmid supercoil relaxation assays. For the structure elucidation of the compounds, melting points, UV, IR, 1H NMR, 13C NMR, mass spectral data and elemental analyses were interpreted. Among the compounds, 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) manifested relatively potent topoisomerase I inhibition.

scholarly journals A Novel and Efficient Synthesis of [1,2,3]-Triazolyl Substituted Benzo[c]Coumarins and Evaluation of their Antimicrobial Activity

2016 ◽  
Vol 70 ◽  
pp. 1-11
Author(s):  
Neha N. Gohil ◽  
Kaushik N. Kundaliya ◽  
Dinkar I. Brahmbhatt
Keyword(s):  
Antimicrobial Activity ◽  
Fungal Pathogens ◽  
Sodium Acetate ◽  
Efficient Synthesis ◽  
Mass Spectral Data ◽  
Pyridinium Bromide ◽  
Mass Spectral ◽  
H Nmr ◽  
Anti Fungal ◽  
C Nmr

A series of novel [1,2,3]-triazolyl substituted benzo [c] coumarins have been synthesized by reacting various 3-coumarinoyl methyl pyridinium bromide salts with 1-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl) ethanones in the presence of sodium acetate in refluxing acetic acid. The structures of the synthesized compounds have been elucidated by IR,1H-NMR,13C-NMR and Mass spectral data. All the synthesized compounds have been screened for theirinvitroanti-bacterial and anti-fungal activities. Some of the compounds have been found to be active against some bacterial and fungal pathogens compared to standard drugs.

scholarly journals Synthesis and In Vitro Antibacterial and Antifungal Evaluation of Quinoline Analogue Azetidin and Thiazolidin Derivatives

2014 ◽  
Vol 39 ◽  
pp. 195-210 ◽  
Author(s):  
Shraddha M. Prajapati ◽  
Rajesh H. Vekariya ◽  
Kinjal D. Patel ◽  
Shyamali N. Panchal ◽  
Hitesh D. Patel ◽  
...  
Keyword(s):  
Gram Negative Bacteria ◽  
Aspergillus Clavatus ◽  
Dilution Technique ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Antibacterial And Antifungal ◽  
Broth Dilution

A library of quinoline analog two novel series of azetidin (SH1-5) and thiazolidin (SHa-e) derivatives were designed and synthesized with simple and eco-friendly methodologies. The structures of the compounds were elucidated with the aid of elemental analysis, IR, 1H-NMR and mass spectral data. These novel synthesized compounds were evaluated for antibacterial activity against two gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus) and two gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also studied for their antifungal activity with Candida albicans, Aspergillus niger, Aspergillus clavatus using the broth dilution technique. Most of the compounds were the best bio-active desired antibacterial analog with less MIC value against different tested strains.

An Efficient Synthesis and Antimicrobial Evaluation of some New Pyrazoline, Pyrimidine and Benzodiazepine Derivatives Bearing 1,3,5-Triazine Core

2015 ◽  
Vol 57 ◽  
pp. 13-24 ◽  
Author(s):  
Anjani Solankee ◽  
Riki Tailor
Keyword(s):  
Guanidine Hydrochloride ◽  
Antibacterial Activities ◽  
Dilution Method ◽  
Mass Spectral ◽  
E Coli ◽  
H Nmr ◽  
Antimicrobial Evaluation ◽  
Benzodiazepine Derivatives ◽  
Amino Pyrimidine

In our present investigation a new class of diverse sets of acetyl pyrazolines (6a-e), amino pyrimidines (7a-e) and 1,5-benzodiazepines (8a-e) bearing 1,3,5-triazine core were synthesised from chalcones (5a-e). Treatment of chalcone with hydrazine hydrate, guanidine hydrochloride and o-phenylenediamine afforded the corresponding acetyl pyrazoline, amino pyrimidine and 1,5-benzodiazepine derivatives respectively. The structures of all the newly synthesised compounds were assigned on the basis of FTIR, 1H NMR, 13C NMR, mass spectral data as well as elemental analysis. In vitro antimicrobial proficiency of the title compounds were assessed against selected pathogens S. aureus MTCC 96, S. pyogeneus MTCC 442, E. coli MTCC 443 and P. aeruginosa MTCC 1688 bacteria for antibacterial activities as well as antifungal activities against C. albicans MTCC 227, A. niger MTCC 282 and A. clavatus MTCC 1323 were used. The minimum inhibitory concentration (MIC) was determined by broth dilution method and recorded at the lowest concentration inhibiting growth of the organism. Among the synthesised compounds 6b, 6c, 7b, 8b, 8d and 8e exhibited excellent antimicrobial activity and said to be the most proficient members of the series.

scholarly journals Synthesis and Biological Evaluation of Some Novel 1, 3, 5-Trisubstituted Pyrazolines

2010 ◽  
Vol 7 (1) ◽  
pp. 295-298 ◽  
Author(s):  
B. C. Revanasiddappa ◽  
R. Nagendra Rao ◽  
E. V. S. Subrahmanyam ◽  
D. Satyanarayana
Keyword(s):  
Antimicrobial Activity ◽  
Acetic Acid ◽  
Spectral Data ◽  
Glacial Acetic Acid ◽  
Biological Evaluation ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Synthesis And Biological Evaluation

A new series of chalcones (3a-j) were synthesized by condensation of simple aldehydes with substituted acetophenones in presence of alkali. The resulted chalcones upon cyclization in presence of glacial acetic acid with isoniazid (INH) will yields the title compounds (4a-j). The newly synthesized compounds were assigned on the basis of IR,1H NMR, and Mass spectral data. All the final compounds were evaluated for theirin vitroantimicrobial activity.

scholarly journals Synthesis, Characterization, and Biological Evaluation of Some New Functionalized Terphenyl Derivatives

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Seranthimata Samshuddin ◽  
Badiadka Narayana ◽  
Balladka Kunhanna Sarojini ◽  
Divya N. Shetty ◽  
Nalilu Suchetha Kumari
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Spectral Data ◽  
Antioxidant Properties ◽  
Biological Evaluation ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr

New functionalized terphenyl derivatives incorporating various heterocyclic rings are prepared by using 4,4′′-difluoro-5′-hydroxy-1,1′:3′,1′′-terphenyl-4′-carbohydrazide as a key intermediate derived from 4,4′-difluoro chalcone, a versatile synthone. All the derivatives are characterized by 1H NMR, IR, and mass spectral data. All the synthesized products are screened for their in vitro antimicrobial and antioxidant properties. The majority of the tested compounds exhibited significant antioxidant activity and some of them showed good antimicrobial activity.

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