Synthesis and antibacterial activity of some new 1-aroyl-3-(substituted-2-benzothiazolyl)thioureas

Saeed, Aamer; Rafique, Hummera; Hameed, Abdul; Rasheed, Safia

doi:10.1007/s11094-008-0094-x

Cited by 38 publications

(38 citation statements)

References 26 publications

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“…Acyl thiourea derivatives have been increasingly important with a wide diversity of applications in heterocyclic chemistry, metal complexes, molecular electronics and exhibit an array of biological activities [5][6][7][8][9]. Some of them are employed as fungicidal, antiviral, antimicrobial [10], parasiticidal [11], antitumoral [12] and pesticidal agent [13][14][15]. Indeed cytotoxicity studies using HeLa cancer cell lines have demonstrated that some of these platinum acyl thioureas show cytotoxic behavior, with the antiproliferative effects being dependent on the nature/type of the substituent in the acyl thiourea ligand [16][17][18].…”

Section: Introductionmentioning

confidence: 99%

On the cytotoxic activity of Pd(II) complexes of N,N-disubstituted-N′-acyl thioureas

Plutı́n

Mocelo

Alvarez

et al. 2014

Journal of Inorganic Biochemistry

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Section: Introductionmentioning

confidence: 99%

On the cytotoxic activity of Pd(II) complexes of N,N-disubstituted-N′-acyl thioureas

Plutı́n

Mocelo

Alvarez

et al. 2014

Journal of Inorganic Biochemistry

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“…In the synthesis of thiourea, isothiocyanate is formed as a reactive intermediate and easily converted to other side product during isolation [2]. Many studies reported on the direct reaction of isothiocyanate intermediate with amines after isolation of KCl to produce thiourea in good purity [3].…”

Section: Introductionmentioning

confidence: 99%

One-Pot Multicomponent Synthesis of Thiourea Derivatives in Cyclotriphosphazenes Moieties

Ngaini

Zulkiplee

Halim

2017

Journal of Chemistry

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In this study, hexasubstituted thiourea was carried out via reaction of isothiocyanato cyclophosphazene intermediates with a series of aromatics amines and amino acids in a one-pot reaction system. The reaction was not as straightforward as typical thiourea synthesis. Six unexpected thiourea derivatives a-f were formed in the presence of cyclotriphosphazene moieties in good yields (53-82%). The structures of a-f were characterized by elemental analysis and FTIR, 1 H, 13 C, and 31 P NMR spectroscopies. The occurrence of reverse thioureas formation in a one-pot reaction system is discussed. The possible binding interaction of the synthesised thiourea a-b in comparison to the predicted phenyl thiourea a-b and the targeted a with enzyme enoyl ACP reductase (FabI) is also discussed. Molecular docking of the targeted hexasubstituted thiourea a is able to give higher binding affinity of −7.5 kcal/mol compared to a-b (−5.9 kcal/mol and −6.3 kcal/mol) and thiourea a-b (−4.5 kcal/mol and −4.7 Kcal/mol).

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“…Benzothiazoleand its derivatives such as esters have also been reported as active against Gram-positive and Gram-negative bacteria Benzothiazole derivatives have also found to possess anticancer, antifungal and antibacterial activities [5,6]. 2-Aminobenzothiazole and a number of other aminobenzothiazole derivatives have been reported as muscle relaxants [7,8]. A literature survey performed for the current study revealed that 6-substituted-2-aminobenzothiazole derivatives such as 6-methyl, 6-methoxy, 6-ethoxy and 6-isopropoxy show antibacterial, anti-inflammatory and analgesic properties [9].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

et al. 2016

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Abstract:A new series of N-(6-arylbenzo [d]thiazol-2-yl)acetamides were synthesized by C-C coupling methodology in the presence of Pd(0) using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolyl)benzo[d]thiazol-2-yl)acetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.

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Synthesis and antibacterial activity of some new 1-aroyl-3-(substituted-2-benzothiazolyl)thioureas

Cited by 38 publications

References 26 publications

On the cytotoxic activity of Pd(II) complexes of N,N-disubstituted-N′-acyl thioureas

On the cytotoxic activity of Pd(II) complexes of N,N-disubstituted-N′-acyl thioureas

One-Pot Multicomponent Synthesis of Thiourea Derivatives in Cyclotriphosphazenes Moieties

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

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