Syntheses of Novel Pyrazoline as Antibacterial Agents from Natural Product Vanillin

Setyawati, Amri; Wahyuningsih, Tutik Dwi; Purwono, Bambang

doi:10.14233/ajchem.2017.20247

Cited by 7 publications

(3 citation statements)

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“…1. [5][6][7] In particular, considerable interest has been focused on 1,3,5-trisubstituted pyrazoline derivatives due their potential pharmacological activities including (i) antitubercular activity against the H37Rv strain of Mycobacterium, 9 (ii) antiproliferative activity, 8,10 (iii) antibacterial activity, [11][12][13] (iv) antiobesity effect in an animal model of the potent cannabinoid CB1 receptor antagonist, 14 (v) pre-emergent herbicide activity against various kinds of weeds, 15 and (vi) ACE-inhibitory activity with 0.123 mM IC504. 16 Pyrazoline derivatives show enhanced biological activity compared with their corresponding pyrazoles.…”

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confidence: 99%

TfOH mediated intermolecular electrocyclization for the synthesis of pyrazolines and its application in alkaloid synthesis

Annes

Vairaprakash

2018

RSC Adv.

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confidence: 99%

TfOH mediated intermolecular electrocyclization for the synthesis of pyrazolines and its application in alkaloid synthesis

Annes

Vairaprakash

2018

RSC Adv.

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“…The bacteria used were Escherichia coli (Gram Negative) and Staphylococcus aureus (Gram Positive). The method to test the antibacterial activity referred to Setyawati, et al (2017).…”

Section: Methodsmentioning

confidence: 99%

ANTIBACTERIAL ASSAY OF 2â€™-Hydroxy-4â€™,6â€™,4-Trimethoxychalcone AND 4-Methoxychalcone AGAINST GRAM POSITIVE AND GRAM NEGATIVE BACTERIA

Sepvianti¹,

Kusumaningrum

2019

Jurnal Riset Kesehatan

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Blood transfusion is currently one of the most important health care treatments. Unfortunately, the prevalence of transfusion reactions caused by the use of blood products is still quite high although blood products have been tested in terms of infectious diseases using 4 parameters, namely hepatitis B, hepatitis C, HIV and syphilis. The results of the analysis of blood products produced by UTD (Blood Transfusion Unit) Surabaya showed bacterial contamination of blood products, starting from normal skin flora to pathogens. Bacterial contamination is also believed to be one of the causes of transfusion reactions. Therefore, it is necessary to make efforts to prevent bacterial contamination of blood products. One of the efforts is to find chemical compounds that have good antibacterial activity. In this study, the antibacterial activity of 2 ˈ -hydroxy-4 ˈ ,6 ˈ ,4-trimethoxychalcone and 4-methoxychalcone was tested against gram positive and gram negative bacteria. The test method was agar diffusion at various concentrations of chalcone, namely 0.625; 1.25; 2.5 and 5.0%. The results showed that both chalcones had good antibacterial activity against gram-positive and gram-negative bacteria.

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“…Synthesis of N1-hydrogen pyrazoline was carried out following the method by Setyawati et al (2017) with slight modification. The mixture of chalcone 1 (1 mmol) and hydrazine monohydrate (3 mmol) in methanol was dissolved and refluxed for 2 h. The mixture was poured into the crushed ice to give a precipitate; then, it was filtered, washed, and dried.…”

Section: Synthesis Of 1-hydrogen-3-(2-hydroxyphenyl)-5-(4-hydroxy-3me...mentioning

confidence: 99%

Synthesis, Molecular Docking, and ADMET Study of N1-Hydrogen and N1-Benzoyl Pyrazoline as Antibacterial Agents

Tjitda¹,

Jumina²,

Wahyuningsih³

2022

CMUJNS

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Syntheses of N1-hydrogen and N1-benzoyl pyrazoline derivatives and their antibacterial in vitro and in silico assays have been carried out. N1-Hydrogen pyrazoline derivatives were synthesized by cyclization of 2’-hydroxy chalcone, and the subsequent substitution reaction produced N1-benzoyl pyrazoline derivatives. The in vitro antibacterial assay was carried out by disc diffusion method. In silico evaluation was performed via molecular docking against ecKAS III enzyme (ID PDB: 1hnj) and ADMET prediction was carried out using pkCSM tool. The synthesis results showed that N1-hydrogen and N1-benzoyl pyrazoline derivatives were yielded in 50-83%. Antibacterial test results indicated that the presence of N1-benzoyl substituent decreased the antibacterial activity and was only active on Gram-positive bacteria. In comparison, the N1-hydrogen pyrazolines exhibited good antibacterial activity against both Gram-positive and negative bacteria. The ADMET result confirms that compound 2 has the potential to be evolved as a drug in the future. Keywords: Pyrazoline, Antibacterial, Molecular Docking, ADMET

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Syntheses of Novel Pyrazoline as Antibacterial Agents from Natural Product Vanillin

Cited by 7 publications

References 0 publications

TfOH mediated intermolecular electrocyclization for the synthesis of pyrazolines and its application in alkaloid synthesis

TfOH mediated intermolecular electrocyclization for the synthesis of pyrazolines and its application in alkaloid synthesis

ANTIBACTERIAL ASSAY OF 2â€™-Hydroxy-4â€™,6â€™,4-Trimethoxychalcone AND 4-Methoxychalcone AGAINST GRAM POSITIVE AND GRAM NEGATIVE BACTERIA

Synthesis, Molecular Docking, and ADMET Study of N1-Hydrogen and N1-Benzoyl Pyrazoline as Antibacterial Agents

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