scholarly journals Synthesis and Biological Evaluation of 7-O-Modified Formononetin Derivatives

2008 ◽  
Vol 2008 ◽  
pp. 1-4 ◽  
Author(s):  
Ying Yang ◽  
Wen-Jun Mao ◽  
Huan-Qiu Li ◽  
Tao-Tao Zhu ◽  
Lei Shi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cell Line ◽  
Jurkat Cell ◽  
Preliminary Investigation ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Chemical Structures ◽  
Structure Activity ◽  
Synthesis And Biological Evaluation ◽  
Antiproliferative Activities

Three series of novel formononetin derivatives were synthesized, in which formononetin and heterocyclic moieties were separated by 2-carbon, 3-carbon, and 4-carbon spacers. The chemical structures of these compounds were confirmed. All the derivatives were screened for antiproliferative activities against Jurkat cell line and HepG-2 cell line. In this paper, compounds prepared were also screened for their antibacterial activity of six bacterial strains. Compound 3b exihibited promising antibacterial activity against B. subtilis with minimal inhibitory concentration (MIC) value of 0.78 μg/mL, and compound 5e showed significant antiproliferative activities against Jurkat cell growth with IC50 of 1.35×10−4 μg/mL. The preliminary investigation of structure-activity relationships (SARs) was also discussed based on the obtained experimental data.

One-pot synthesis and biological evaluation of novel 3-(5-((aryl) methyl) isoxazol-3-yl)-4H-chromen-4-one derivatives as potent antibacterial and anticancer agents

2021 ◽  
Vol 25 (11) ◽  
pp. 80-85
Author(s):  
Rani Janapatla Uma ◽  
Babu H. Ramesh ◽  
M. Prashanthi
Keyword(s):  
Antibacterial Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Cell Line Hela ◽  
Aryl Methyl ◽  
Mcf 7

In search of better antibacterial and anticancer agents, a series of novel 3-(5-((aryl) methyl) isoxazol-3-yl)-4Hchromen- 4-one derivatives was synthesized (4a-4l) by using 4-oxo-4H-chromene-3-carbaldehyde and alkyne via in situ generated nitrile oxide and evaluated for their antibacterial and anticancer activity in vitro. Antibacterial activity was evaluated against three G+ bacterial strains and anticancer activity against breast cancer cell line (MCF-7) and cervical carcinoma cell line (HeLa). Among all the tested compounds, 4j and 4g exhibited potent antibacterial activity against tested grampositive bacterial strains. 4g, 4i and 4j exhibited potent cytotoxic activity against MCF-7 with IC50 values nearer to the standard drug doxorubicin.

scholarly journals Synthesis and biological evaluation of some new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as antimicrobial agents

2022 ◽  
Vol 11 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Vasyl Matiychuk
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Synthesis And Biological Evaluation

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.

scholarly journals Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents

2019 ◽  
Vol 15 ◽  
pp. 1468-1474
Author(s):  
Leticia Monjas ◽  
Peter Fodran ◽  
Johanna Kollback ◽  
Carlo Cassani ◽  
Thomas Olsson ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Natural Product ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Methicillin Resistant ◽  
Structure Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Novel Antibiotics

The synthesis and antibacterial activity of two new highly truncated derivatives of the natural product abyssomicin C are reported. This work outlines the limits of structural truncation of the natural product and consequently provides insights for further structure–activity relationship studies towards novel antibiotics targeting 4-amino-4-deoxychorismate (ADC) synthase. Specifically, it is demonstrated that the synthetically challenging bicyclic motif is essential for activity towards methicillin-resistant Staphylococcus aureus (MRSA).

Synthesis and Biological Evaluation of Benzothiazole-piperazinesulfonamide Conjugates and Their Antibacterial and Antiacetylcholinesterase Activity

2019 ◽  
Vol 16 (9) ◽  
pp. 723-734
Author(s):  
B. Ramalingeswara Rao ◽  
Mohana R. Katiki ◽  
Kommula Dileep ◽  
C. Ganesh Kumar ◽  
G. Narender Reddy ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Micrococcus Luteus ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Reference Drug ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation

Two series of N-2-benzothiazolyl-4-(arylsulfonyl)-1-piperazineacetamides/propanamides were synthesized from substituted 2-aminobenzothiazoles and were assayed for their in vitro antimicrobial activities against a panel of different pathogenic bacterial strains such as Micrococcus luteus, S. aureus, S. aureus MLS-16, B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella planticola and Candida albicans. Among the synthesized compounds 5e,f,g and 6g,h,i showed promising antifungal activity against C. albicans as compared to the reference drug, miconazole. Further, compounds 6g,h,i showed broad spectrum antibacterial activity against all the tested bacterial strains, while the compounds 6a-f,j-m showed significant antibacterial activity against all the tested bacterial strains as compared to the reference drug, ciprofloxacin. In addition, the target compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity, and, among the tested, compounds 5j,k,l and 6i showed promising AChE inhibitory activity.

SYNTHESIS AND BIOLOGICAL EVALUATION OF 2-SUBSTITUTED PHENYL-1-(SUBSTITUTED PIPERAZIN-1-YL) METHYL)-1H-BENZO[D]IMIDAZOLES

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (01) ◽  
pp. 50-58
Author(s):  
S. K Gupta ◽  
◽  
N. Kumar ◽  
D. Pathak
Keyword(s):  
Antibacterial Activity ◽  
Anthelmintic Activity ◽  
Mannich Bases ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Diffusion Method ◽  
Benzimidazole Derivatives ◽  
Bacterial Strains ◽  
Death Time ◽  
Synthesis And Biological Evaluation

A series of biologically active benzimidazole derivatives (2a-2n) was synthesized by the reaction of o-phenylenediamine with the derivatives of benzoic acid in presence of 4N-HCl followed by the reaction with piperazine and formaldehyde to undergo Mannich reaction. The structures of all the synthesized Mannich bases were characterized by UV, FTIR, 1H NMR, mass spectroscopy and elemental analysis. The compounds were evaluated for their anthelmintic activity by the identification of paralyzing and death time by using mebendazole as standard in the concentration of 2 mg/ml. The compounds 2a, 2b, 2e and 2h were found to be most potent for anthelmintic activity. All the compounds were also evaluated for antibacterial activity against gram-positive bacterial strains like Bacillus subtilis and Streptococcus aureus, and gram-negative bacterial strains like Escherichia coli and Pseudomonas aeruginosa. The study was performed through disc diffusion method by using Ciprofloxacin as standard in the concentration of 50µg/ml. The compounds 2e, 2h, 2k, 2l and 2m were found to possess significant antibacterial activity.

scholarly journals Synthesis and Biological Evaluation of Novel Pyrane Glycosides

2020 ◽  
Vol 67 (4) ◽  
pp. 1061-1071
Author(s):  
Avula Srinivas ◽  
Malladi Sunitha ◽  
Sriramoju Shamili
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Elemental Analysis ◽  
Hydroxylamine Hydrochloride ◽  
Biological Evaluation ◽  
Chalcone Derivatives ◽  
Chemical Structures ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel (5R)-5-((2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-3,6-dihydro-2H-pyran-2-yl)-3-(4-fluorophenyl)-2,6-diphenyl-3,3a,5,6-tetrahydro-2H-pyrazolo[3,4-d]thiazoles 11a–g and (5R)-5-((2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-3,6-dihydro-2H-pyran-2-yl)-3-(4-fluorophenyl)-6-phenyl-3,3a,5,6-tetrahydroisoxazolo[3,4-d]thiazoles 12a–g were synthesized by the reaction of chalcone derivatives of (R,Z)-2-((2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-3,6-dihydro-2H-pyran-2-yl)-5-(4-fluorobenzylidene)-3-phenylthiazolidin-4-ones 10a–g with phenylhydrazine and hydroxylamine hydrochloride. The chemical structures of newly synthesized compounds were elucidated by IR, NMR, MS and elemental analysis. The compounds 11a–g and 12a–g were evaluated for their antibacterial activity and antifungal activity.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

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