Synthesis, antitubercular and antimicrobial potential of some new thiazole substituted thiosemicarbazide derivatives

Abhale, Yogita K.; Shinde, Abhijit; Deshmukh, Keshav K.; Nawale, Laxman; Sarkar, Dhiman; Mhaske, Pravin C.

doi:10.1007/s00044-017-1955-1

Cited by 39 publications

(27 citation statements)

References 45 publications

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“…culture at 620 nm was used and added into each well of 96 well plates which contains the compounds to be tested. 24,25 Optical density for each plate was measured at 620 nm after 8 h for Gram-negative bacteria and after 12 h for Gram-positive bacteria.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Antibacterial Screening of Novel (E)-3-(3-(2-(4-Fluorophenyl)-4-Methylthiazol-5-Yl)-1-Phenyl-1h-Pyrazol-4-Yl)-1-(2-Hydroxyphenyl)prop-2-en-1-Ones

Akolkar¹,

Karale²,

Darekar³

2019

Int Res J Pharm

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A novel series of chalcone 3a-e was prepared by conventional Claisen-Schmidt condensation of 3-(2-(4-fluorophenyl)-4-methylthiazol-5-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde 1 with substituted 2-hydroxyacetophenones using 40 % aq. KOH in ethanol. The starting material 3-(2-(4-fluorophenyl)-4-methylthiazol-5-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde 1 was synthesized by reacting 1-[2-(4-fluorophenyl)-4-methyl-1,3-thiazol-5-yl]ethan-1one with phenyl hydrazine followed by reaction with DMF/ POCl3. The structures of all newly synthesized compounds were assigned on the basis of spectral data such as IR, 1 H-NMR and mass. These compounds3a-e were evaluated for their antibacterial activity against gram-negative Pseudomonas fluorescens and Escherichia coli and gram-positive bacteria, Bacillus subtilis and Staphylococcus aureus. Compounds 3a-e showed good activity against gram positive bacterial strain of Bacillus subtilis compared to the standard drug Ampicillin at a concentration of 100 μg/mL also compounds 3a, 3c, 3d and 3e showed good activity at a concentration of 30 μg/mL but none of them was as active as standard Ampicillin.

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Section: Resultsmentioning

confidence: 99%

Synthesis and Antibacterial Screening of Novel (E)-3-(3-(2-(4-Fluorophenyl)-4-Methylthiazol-5-Yl)-1-Phenyl-1h-Pyrazol-4-Yl)-1-(2-Hydroxyphenyl)prop-2-en-1-Ones

Akolkar¹,

Karale²,

Darekar³

2019

Int Res J Pharm

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“…Recently, ethylidenethiosemicarbazides have been used as effective pharmacophoric agents in medicinal chemistry such as; antitumor 1 , anti-tubercular 2 , anti-amoebic 3 , anti-fungal 4 , antiviral 5 , antimicrobial 6 , antioxidant 7 , anticonvulsant 8 , and anti-trypanosomal 9,10 . Also, these compounds were prescribed for treatment of hypertension as calcium channel blockers 11 .…”

Section: Fig 1 Representative Derivatives Of Ethylidenethiosemicarbmentioning

confidence: 99%

A Decade of Development of Ethylidenethiosemicarbazides as Building Blocks for Synthesis of Azoles and Azines (A Review)

Riyadh¹,

El-Motairi²,

Deawaly³

2018

Orient. J. Chem

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“…It constitutes a main scaffold of many pharmaceutically significant compounds including natural (large range of terrestrial and marine compounds, for example, Kanamycin, Tubulysin E, and Thiostrepton which exhibit cyclo‐static, antibiotic, and antifungal activity) and synthetic ones (Bacillamides, Piscibactin, Ritonavir, Nizatidin, and Abafungin). Thiazole derivatives are associated with a broad spectrum of biological properties, such as anticonvulsant, antimicrobial, antitubercular, antiviral, antimalarial, anticancer, antihypertensive, anti‐inflammatory, and anti‐allergic . Thiazole derivatives also find application in various fields, including photonucleases, polymers, liquid crystals, fluorescent dyes or intermediates for dyes, insecticides, plant protectants, antioxidants, vulcanising accelerators (mercaptobenzothiazole), and photosensitizers …”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Activity of Novel Thiazoles with Reactive Functional Groups

et al. 2019

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A series of substituted thiazoles bearing different functional groups, such as carboxyethylamino, carboxyl, chloromethyl, (phenylamino)methyl, ethoxyoxoethyl, methoxyoxoethylidene, ethoxycarbonyl, (methoxy or hydrazinyl)oxopropyl, carbohydrazinyl, formyl, and ((phenyl, carbamothioyl or isonicotinoyl)hydrazono)methyl, incorporated into their structure were synthesized. The synthesized compounds were tested for their antimicrobial activity against Escherichia coli, Staphylococcus aureus, and Mycobacterium luteum bacteria strains, and Candida tenuis and Aspergillus niger fungi. Compounds exhibiting exclusive antifungal activity against Aspergillus niger (MIC 0.9, 1.9 μg/mL) and Candida tenuis (MIC 7.8 μg/mL) have been identified among the novel thiazole derivatives.

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Synthesis, antitubercular and antimicrobial potential of some new thiazole substituted thiosemicarbazide derivatives

Cited by 39 publications

References 45 publications

Synthesis and Antibacterial Screening of Novel (E)-3-(3-(2-(4-Fluorophenyl)-4-Methylthiazol-5-Yl)-1-Phenyl-1h-Pyrazol-4-Yl)-1-(2-Hydroxyphenyl)prop-2-en-1-Ones

Synthesis and Antibacterial Screening of Novel (E)-3-(3-(2-(4-Fluorophenyl)-4-Methylthiazol-5-Yl)-1-Phenyl-1h-Pyrazol-4-Yl)-1-(2-Hydroxyphenyl)prop-2-en-1-Ones

A Decade of Development of Ethylidenethiosemicarbazides as Building Blocks for Synthesis of Azoles and Azines (A Review)

Synthesis and Antimicrobial Activity of Novel Thiazoles with Reactive Functional Groups

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