Synthesis and Characterization of Novel N-(Benzo[d]Thiazol-2-yl)-2-(2-(6-Chloroquinolin-4-yl)Hydrazinyl)Acetamide Derivatives Containing Quinoline Linkage as Potent Antibacterial Agents

Bhoi, Manoj N.; Borad, Mayuri A.; Parmar, Hitesh B.; Patel, Hitesh D.

doi:10.18052/www.scipress.com/ilcpa.53.114

Cited by 7 publications

(8 citation statements)

References 10 publications

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“…2.2.2. General synthetic procedure for 2-Chloro-N-(6-substituted-1,3-benzothiazol-2-yl) acetamide BTC (1)(2)(3)(4)(5) To 250 ml round bottom ask, a suspension of the substituted 2-amino benzothiazole BT (1-5) (0.005mol), anhydrous Potassium carbonate (2.5 gm) and 1ml of TEA in dry chloroform (65 ml) was taken. To above suspension, chloroacetylchloride (0.006mol) was added and the mixture was re uxed for 4-5 hrs.…”

Section: Methods B: Bt 2-5mentioning

confidence: 99%

“…Benzothiazoles are important class of heterocyclic compounds possessing signi cant biological activities and interesting chemical features. Various benzothiazole derivatives are reported to possess broad spectrum of biological activities such as antimicrobial [1][2][3][4][5][6], antitubercular [7][8], anticancer [9][10], anticonvulsant [11][12], antidiabetic [13][14], antiviral [15] and anti-in ammatory [16]. Benzothiazole also showed antimicrobial activity through inhibition of DNA gyrase [17][18].…”

Section: Introductionmentioning

confidence: 99%

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Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

Pawar¹,

Kale²,

Zori³

et al. 2021

Preprint

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The new series of 2-(substituted amino)-N-(6- substituted-1,3-benzothiazol-2yl) acetamide BTC(a-t) has been synthesized by appropriate synthetic route from substituted 2-amino benzothiazole. The synthesized compounds were screened experimentally for its antimicrobial property against gram positive, gram negative bacteria and fungi. Zone of inhibition and minimum inhibitory concentration of compounds was determined against selected bacterial and fungal strains. Compound BTC-j N-(6-methoxy-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide and compound BTC-r N-(6-nitro-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide found to have good antimicrobial potential. The compound BTC-j has shown good antibacterial activity against S. aureus at MIC of 12.5 µg/ml, B. subtilis at MIC of 6.25µg/ml, E. coli at MIC of 3.125µg/ml and P. aeruginosa at MIC of 6.25µg/ml. No statistical difference in antimicrobial activity of standard and test compounds was found indicating test compounds have comparable activity. Further docking study was carried out to check the probable interactions with the selected protein using V-life MDS 3.5 software. (DNA gyrase, PDB: 3G75). The dock score of compounds and antimicrobial activity found to be consistent.

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Section: Methods B: Bt 2-5mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

Pawar¹,

Kale²,

Zori³

et al. 2021

Preprint

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“…[154,155] Pyridine unit containing scaffolds and benzothiazole derivatives have been demonstrated to possess broad-spectrum medicinal properties. [156][157][158] Based on these, the moieties pyridine, benzothiazole and isoniazid are brought into a single molecular framework to design 4H-pyrimido[2,1-b]benzothiazoles derivatives. [159] The molecular design includes pyrimidine fused to benzothiazole at its 2,3-positions and pyridine-2yl ring at 4-position in addition to the linkage of the pyridine-4-carbonyl motif at pyrimidine 5-position thorough carbohydrazide fragment.…”

Section: Thiazole/benzothiazole Analogsmentioning

confidence: 99%

Pharmacology Profile of Recently Developed Multi‐Functional Azoles; SAR‐Based Predictive Structural Modification

Dorababu¹

2020

ChemistrySelect

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Fungal infections have become ubiquitous diseases and their persistent nature and development of drug resistance have led to a global threat. Thereby urgent need to develop efficient antifungal agents is a must. Menace of protozoal diseases cannot be ruled out as the vaccines are not available currently and available anti-protozoal drugs are of low efficacy. Multidrug-resistant tuberculosis is responsible for the inefficient treatment of tuberculosis. Regarding cancer control, the fivemembered heterocyclic compounds such as triazoles and tetrazoles are significant pharmacores that play prominent roles in drug design. In this regard, the research is being carried out in the field of drug design and synthesis considering azole-containing scaffolds as promising target molecules. In this review, the research on azoles having inhibitory properties against various disease causative factors such as fungi, protozoa, bacteria, mycobacteria, etc and various cancer cell lines is described. The whole research is classified on the basis of the type of the azole pharmacore on which the drug molecules are synthesized. The pharmacology of the designed molecules is expressed alongside emphasizing the moieties responsible for the potent activity. Besides, possible structural modification speculating higher biological properties is demonstrated based on SAR.

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“…3 Recently, a research group was interested in the in vitro antifungal activities of synthesized 2-amino-benzothiazole derivatives and showed their novel structure leads to potent antimicrobial activity. 4,5 Previous results proved that an SH moiety at the 2 position of the heterocyclic nucleus significantly increases the antibacterial activity. 4 In addition, 2-ABZT is the amino derivative of the benzothiazole nucleus.…”

Section: Introductionmentioning

confidence: 99%

“…This molecule has emerged as a promising active agent against the persistent increase of antimicrobial resistance. [4][5][6] Benzothiazole is recognized as multitalented scaffold in pharmaceutical chemistry. 7 Thus, benzothiazole derivatives cover a large spectrum of pharmacological activities, such as antimicrobial, 8,9 antidiabetic, 10 antitumor, 11 antitrypanosomal, 12 anticancer, 13 anti-inflammatory and antifungal activity.…”

Section: Introductionmentioning

confidence: 99%

In vitro release study of 2-aminobenzothiazole from microspheres as drug carriers

et al. 2020

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The aim of the present study was the preparation of 2-aminobenzothiazole-loaded microspheres based on cellulose derivatives for controlled and prolonged release. Micro-encapsulation by the simple emulsion (O/W) solvent evaporation method was performed to prepare these formulations using two cellulose derivatives as matrices: ethyl cellulose (EC) and cellulose acetate butyrate (CAB). Optimization of the experimental parameters, such as the polymer/solvent ratio, the matrix type, stirring speed and the number of blades, was performed to obtain a high encapsulation efficiency of the drug. The effect of the selected parameters on microsphere characteristics, as well as the release rate was investigated. SEM images show that the obtained microparticles were spherical in shape. The effective entrapment of 2-amino-benzothiazole (2-ABZT) in the microspheres was confirmed by FTIR spectroscopy and XRD diffraction analysis. The encapsulation efficiency was improved when the polymer concentration increased reaching 89 %. Microspheres in the size range of 61-278 µm with EC and close to 113 µm with CAB were obtained by varying the process conditions. The in vitro release kinetics of the cation of 2-ABZT were established at 37 °C in simulated gastric medium pH 1.2 and the obtained data were analyzed according to the Fick law. The results showed that the surface morphology and encapsulation efficiency of the microspheres depended strongly on the polymer/solvent ratio and the release rate could be controlled by adjusting the process conditions.

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Synthesis and Characterization of Novel N-(Benzo[d]Thiazol-2-yl)-2-(2-(6-Chloroquinolin-4-yl)Hydrazinyl)Acetamide Derivatives Containing Quinoline Linkage as Potent Antibacterial Agents

Cited by 7 publications

References 10 publications

Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

Pharmacology Profile of Recently Developed Multi‐Functional Azoles; SAR‐Based Predictive Structural Modification

In vitro release study of 2-aminobenzothiazole from microspheres as drug carriers

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