Design, synthesis and mode of action of some benzothiazole derivatives bearing an amide moiety as antibacterial agents

RSC Advances ◽  
2014 ◽  
Vol 4 (36) ◽  
pp. 19013-19023 ◽  
Author(s):  
Meenakshi Singh ◽  
Sudhir K. Singh ◽  
Mayank Gangwar ◽  
Gopal Nath ◽  
Sushil K. Singh
Keyword(s):  
Antibacterial Activity ◽  
Mode Of Action ◽  
Antibacterial Agents ◽  
Design Synthesis ◽  
Benzothiazole Derivatives

Schematic outline of the most potent compound, benzothiazole bearing amide moiety A07, showing antibacterial activity and its mode of action.

scholarly journals 1,4-Naphthoquinone Analogues: Potent Antibacterial Agents and Mode of Action Evaluation

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1437 ◽  
Author(s):  
Palanisamy Ravichandiran ◽  
Sunirmal Sheet ◽  
Dhanraj Premnath ◽  
Ae Rhan Kim ◽  
Dong Jin Yoo
Keyword(s):  
Antibacterial Activity ◽  
Mode Of Action ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Annexin V ◽  
Ros Generation ◽  
Redox Potentials ◽  
Bacterial Strains ◽  
E Coli ◽  
New Class

1,4-Naphthoquinones have antibacterial activity and are a promising new class of compound that can be used to treat bacterial infections. The goal was to improve effective antibacterial agents; therefore, we synthesized a new class of naphthoquinone hybrids, which contain phenylamino-phenylthio moieties as significant counterparts. Compound 4 was modified as a substituted aryl amide moiety, which enhanced the antibacterial activity of earlier compounds 3 and 4. In this study, five bacterial strains Staphylococcus aureus (S. aureus), Listeria monocytogenes (L. monocytogenes), Escherichia coli (E. coli), Pseudomonas aeruginosa (P. aeruginosa) and Klebsiella pneumoniae (K. pneumoniae) were used to evaluate the antibacterial potency of synthesized naphthoquinones using the minimal inhibitory concentration (MIC) method. Most of the studied naphthoquinones demonstrated major antibacterial activity with a MIC of 15.6 µg/mL–500 µg/mL. Selected compounds (5a, 5f and 5x) were studied for the mode of action, using intracellular ROS generation, determination of apoptosis by the Annexin V-FITC/PI assay, a bactericidal kinetic study and in silico molecular modelling. Additionally, the redox potentials of the specified compounds were confirmed by cyclic voltammetry (CV).

Design, Synthesis and Mode of Action of Some New 2-(4';-aminophenyl) benzothiazole Derivatives as Potent Antimicrobial Agents

2016 ◽  
Vol 13 (5) ◽  
pp. 429-437 ◽  
Author(s):  
Meenakshi Singh ◽  
Sudhir Kumar Singh ◽  
Mayank Gangwar ◽  
Satheeshkumar Sellamuthu ◽  
Gopal Nath ◽  
...  
Keyword(s):  
Mode Of Action ◽  
Antimicrobial Agents ◽  
Design Synthesis ◽  
Benzothiazole Derivatives

Design, synthesis and biological evaluation of 5′-C-piperidinyl-5′-O-aminoribosyluridines as potential antibacterial agents

2015 ◽  
Vol 13 (28) ◽  
pp. 7720-7735 ◽  
Author(s):  
Takeshi Nakaya ◽  
Akira Matsuda ◽  
Satoshi Ichikawa
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Human Cells ◽  
Ritter Reaction ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Caprazamycin analogues, which were designed and synthesized via an aza-Prins–Ritter reaction, exhibit a good MraY and antibacterial activity without cytotoxicity against human cells.

scholarly journals Design, synthesis and antibacterial activity of new phthalazinedione derivatives

2011 ◽  
Vol 76 (3) ◽  
pp. 329-339 ◽  
Author(s):  
El-Galil Khalil ◽  
Moged Berghot ◽  
Mostafa Gouda
Keyword(s):  
Antibacterial Activity ◽  
Sodium Hydroxide ◽  
Ring Opening ◽  
Antibacterial Agents ◽  
Acetyl Chloride ◽  
Triazole Derivative ◽  
Design Synthesis ◽  
Gewald Reaction ◽  
Triazine Derivatives ◽  
Thiophene Derivatives

Dibenzobarrelene (1) was utilized as the key intermediate for the synthesis of some new 2-substituted (1,4-dioxo-3,4,4e,5,10,10ahexahydro- 1H-5,10-benzeno-benzo[g]phthalazine: 2, 5a-d, 8a-c and 10. Condensation of 2 with benzaldehyde or anisaldehyde gave the corresponding acrylonitrile derivative 3a, b, respectively. Thiophene derivatives 4a, b were obtained via the Gewald reaction of 2 with cyclohexanone or pentanone, respectively. Treatment of 5d with acetyl chloride or p-toluenesulfonyl chloride afforded the corresponding esters 6, 7, respectively. Cyclization of 8a-c with formalin afforded the corresponding triazine derivatives 9a-c. Ring opening of 10 with sodium hydroxide gave the corresponding triazole derivative 11, which when alkylated with pentyl bromide afforded the pentylsulfanyl derivative 12. Representative compounds of the synthesized products were established and evaluated as antibacterial agents.

scholarly journals Design, synthesis and evaluation of anti-inflammatory, analgesic and antibacterial activity of 2, 4, 6-trisubstituted quinazoline derivatives

2018 ◽  
Vol 29 (2) ◽  
pp. 97-102
Author(s):  
Nivrati Jain ◽  
Harshita Jain ◽  
Ashish Jain ◽  
Veerasamy Ravichandran ◽  
Prateek Jain
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Spectroscopy Analysis ◽  
Design Synthesis ◽  
E Coli ◽  
Quinazoline Derivatives ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation ◽  
Mass Spectroscopy Analysis

Abstract We described here the synthesis and biological evaluation of a series of 2, 4, 6-trisubstituted quinazoline derivatives as potential anti-inflammatory, analgesic and antibacterial agents. The synthesized compounds were characterized by FTIR, 1H NMR and mass spectroscopy analysis. We found that the compounds 6b, 6e, 6g, 6h and 6j showed better anti-inflammatory activity than indomethacin. Compounds 6b, 6e, 6h, 6j and 6l were found to exhibit appreciable analgesic activity, and 6b, 6g and 6k showed good antibacterial activity against Gram (+) bacteria: B. subtilis, S. aureus, S. epidermis, and Gram (-) bacteria: E. coli, P. aeruginosa and K. pneumoniae. Compound 6b showed overall better anti-inflammatory, analgesic and antibacterial activity among the synthesized compounds. The results of the present study could be helpful for the designing of effective anti-inflammatory, analgesic and antibacterial agents.

Design, synthesis, antibacterial activity evaluation and molecular modeling studies of new sulfonamides containing sulfathiazole moiety

2021 ◽  
Author(s):  
Tuğba Meşeli ◽  
Şengül Dilem Doğan ◽  
Miyase Gözde Gündüz ◽  
Zulbiye Onal ◽  
Sanja Skaro Bogojevic ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Molecular Modeling ◽  
Antibacterial Agents ◽  
Central Position ◽  
Design Synthesis ◽  
Bacterial Diseases ◽  
Activity Evaluation ◽  
Modeling Studies ◽  
Molecular Modeling Studies

Sulfonamides represent the oldest synthetic antibacterial agents; however, their central position in controlling bacterial diseases has been seriously damaged by the development of widespread resistance. Hereby, we revisited sulfathiazole, a...

Discovery of Antibacterial Agents Inhibiting the Energy-Coupling Factor (ECF) Transporters by Structure-Based Virtual Screening

2020 ◽  
Author(s):  
Eleonora Diamanti ◽  
Inda Setyawati ◽  
Spyridon Bousis ◽  
leticia mojas ◽  
lotteke Swier ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Energy Coupling ◽  
Coupling Factor ◽  
Design Synthesis ◽  
Screening Design ◽  
Starting Point ◽  
Wide Range ◽  
Vitamin Uptake

Here, we report on the virtual screening, design, synthesis and structure–activity relationships (SARs) of the first class of selective, antibacterial agents against the energy-coupling factor (ECF) transporters. The ECF transporters are a family of transmembrane proteins involved in the uptake of vitamins in a wide range of bacteria. Inhibition of the activity of these proteins could reduce the viability of pathogens that depend on vitamin uptake. Because of their central role in the metabolism of bacteria and their absence in humans, ECF transporters are novel potential antimicrobial targets to tackle infection. The hit compound’s metabolic and plasma stability, the potency (20, MIC Streptococcus pneumoniae = 2 µg/mL), the absence of cytotoxicity and a lack of resistance development under the conditions tested here suggest that this scaffold may represent a promising starting point for the development of novel antimicrobial agents with an unprecedented mechanism of action.<br>

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