scholarly journals Microwave-Assisted Synthesis of Schiff Bases of Isoniazid and Evaluation of Their Anti-Proliferative and Antibacterial Activities

Molbank ◽  
10.3390/m1189 ◽  
2021 ◽  
Vol 2021 (1) ◽  
pp. M1189
Author(s):  
Bayan Ahed Al-Hiyari ◽  
Ashok K. Shakya ◽  
Rajashri R. Naik ◽  
Sanaa Bardaweel
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Aromatic Aldehydes ◽  
Antibacterial Activities ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Ic50 Values ◽  
In Vitro Inhibition ◽  
Mcf 7

Three new Schiff bases of isoniazid were synthesized using microwave-assisted synthesis and conventional condensation with aromatic aldehydes. Synthesized compounds were characterized using elemental analysis, IR, NMR, and Mass spectroscopy. Synthesized compounds were evaluated for antiproliferative activity against MCF-7 cell line. The IC50 values were from 125 to 276 µM. The compounds were also evaluated for antibacterial activity against Staphylococcus aureus and Escherichia coli. Results showed that the synthesized compounds produce significant antibacterial activity in vitro. Inhibition of compounds ranged from 13 to 18 mm.

Microwave assisted synthesis of novel Pyrazole derivatives and their biological evaluation as anti-bacterial agents

2020 ◽  
Vol 23 ◽  
Author(s):  
Hadis Khodadad ◽  
Farhad Hatamjafari ◽  
Khalil Pourshamsian ◽  
Babak Sadeghi
Keyword(s):  
Antibacterial Activity ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Antibacterial Activities ◽  
Structural Features ◽  
Biological Evaluation ◽  
Aureus Strain ◽  
Microwave Assisted Synthesis ◽  
Pyrazole Derivatives ◽  
Microwave Assisted

Aim and Objective: Microwave-assisted condensation of acetophenone 1 and aromatic aldehydes 2 gave chalcone analogs 3, which were cyclized to pyrazole derivatives 6a-f via the reaction with hydrazine hydrate and oxalic acid in the presence of the catalytic amount of acetic acid in ethanol. Materials and Methods: The structural features of the synthesized compounds were characterized by melting point, FT-IR, 1H, 13C NMR and elemental analysis. Results: The antibacterial activities of the synthesized pyrazoles was evaluated against three gram-positive bacteria such as Enterococcus durans, Staphylococcus aureus, Bacillus subtilis and two gram-negative bacteria such as Escherichia coli and Salmonella typhimurium. Conclusion: All the synthesized pyrazoles showed relatively high antibacterial activity against S. aureus strain and none of them demonstrated antibacterial activity against E. coli.

scholarly journals Green Chemistry Approach for Efficient Synthesis of Schiff Bases of Isatin Derivatives and Evaluation of Their Antibacterial Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Jnyanaranjan Panda ◽  
V. Jagannath Patro ◽  
Biswa Mohan Sahoo ◽  
Jitendriya Mishra
Keyword(s):  
Green Chemistry ◽  
Schiff Bases ◽  
Reaction Times ◽  
Antibacterial Activities ◽  
Primary Amines ◽  
Microwave Assisted Synthesis ◽  
Azomethine Group ◽  
Microwave Assisted ◽  
Isatin Derivatives

Microwave-assisted organic synthesis, a green chemistry approach, is nowadays widely used in the drug synthesis. Microwave-assisted synthesis improves both throughput and turnaround time for medicinal chemists by offering the benefits of drastically reduced reaction times, increased yields, and pure products. Schiff bases are the important class of organic compounds due to their flexibility, and structural diversities due to the presence of azomethine group which is helpful for elucidating the mechanism of transformation and rasemination reaction in biological system. This novel compound could also act as valuable ligands for the development of new chemical entities. In the present work, some Schiff bases of Isatin derivatives was synthesized using microwave heating method. Schiff base of Isatin were synthesized by condensation of the keto group of Isatin with different aromatic primary amines. They were characterized by means of spectral data and subsequently subjected to the in vitro antibacterial activities against gram positive and gram negative strains of microbes. It was observed that the compound with electron withdrawing substituents exhibited good antibacterial activities against almost all the micro organisms.

scholarly journals Microwave-assisted synthesis of 1,2,3,4-tetrahydroisoquinoline sulfonamide derivatives and their biological evaluation

2020 ◽  
pp. 76-76
Author(s):  
Stanimir Manolov ◽  
Iliyan Ivanov ◽  
Dimitar Bojilov
Keyword(s):  
Antibacterial Activity ◽  
Thin Layer ◽  
In Silico ◽  
Biological Evaluation ◽  
Reversed Phase ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
In Vitro Inhibition ◽  
Layer Chromatography

Herein we report an alternative eco-friendly method for the synthesis of 1,2,3,4-tetrahydroisoquinoline sulfonamide derivatives. All obtained compounds were screened for their in vitro inhibition of albumin denaturation, antioxidant, antitryptic, and antibacterial activity and have shown significant results. The lipophilicity was established using both reversed-phase thin layer chromatography and in silico calculations.

scholarly journals Microwave-Assisted Synthesis of (Piperidin-1-yl)quinolin-3-yl)methylene)hydrazinecarbothioamides as Potent Inhibitors of Cholinesterases: A Biochemical and In Silico Approach

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 656
Author(s):  
Rubina Munir ◽  
Muhammad Zia-ur-Rehman ◽  
Shahzad Murtaza ◽  
Sumera Zaib ◽  
Noman Javid ◽  
...  
Keyword(s):  
Neurodegenerative Disorder ◽  
Critical Role ◽  
Public Health Problem ◽  
Microwave Assisted Synthesis ◽  
Major Public Health Problem ◽  
Spectroscopic Techniques ◽  
Dual Inhibitor ◽  
Microwave Assisted ◽  
Ic50 Values

Alzheimer’s disease (AD), a progressive neurodegenerative disorder, characterized by central cognitive dysfunction, memory loss, and intellectual decline poses a major public health problem affecting millions of people around the globe. Despite several clinically approved drugs and development of anti-Alzheimer’s heterocyclic structural leads, the treatment of AD requires safer hybrid therapeutics with characteristic structural and biochemical properties. In this endeavor, we herein report a microwave-assisted synthesis of a library of quinoline thiosemicarbazones endowed with a piperidine moiety, achieved via the condensation of 6/8-methyl-2-(piperidin-1-yl)quinoline-3-carbaldehydes and (un)substituted thiosemicarbazides. The target N-heterocyclic products were isolated in excellent yields. The structures of all the synthesized compounds were fully established using readily available spectroscopic techniques (FTIR, 1H- and 13C-NMR). Anti-Alzheimer potential of the synthesized heterocyclic compounds was evaluated using acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The in vitro biochemical assay results revealed several compounds as potent inhibitors of both enzymes. Among them, five compounds exhibited IC50 values less than 20 μM. N-(3-chlorophenyl)-2-((8-methyl-2-(piperidin-1-yl)quinolin-3-yl)methylene)hydrazine carbothioamide emerged as the most potent dual inhibitor of AChE and BChE with IC50 values of 9.68 and 11.59 μM, respectively. Various informative structure–activity relationship (SAR) analyses were also concluded indicating the critical role of substitution pattern on the inhibitory efficacy of the tested derivatives. In vitro results were further validated through molecular docking analysis where interactive behavior of the potent inhibitors within the active pocket of enzymes was established. Quinoline thiosemicarbazones were also tested for their cytotoxicity using MTT assay against HepG2 cells. Among the 26 novel compounds, there were five cytotoxical and 18 showed proliferative properties.

scholarly journals Microwave-Assisted Synthesis, Proton Dissociation Processes, and Anticancer Evaluation of Novel D-Ring-Fused Steroidal 5-Amino-1-Arylpyrazoles

2019 ◽  
Vol 10 (1) ◽  
pp. 229
Author(s):  
Gergő Mótyán ◽  
Ádám Baji ◽  
Małgorzata Anna Marć ◽  
Mohana Krishna Gopisetty ◽  
Dóra I. Adamecz ◽  
...  
Keyword(s):  
Human Cancer ◽  
Condensation Reaction ◽  
Microwave Assisted Synthesis ◽  
Antiproliferative Effects ◽  
Human Cancer Cells ◽  
Microwave Assisted ◽  
Proton Dissociation ◽  
Ic50 Values ◽  
Spectrophotometric Titrations

Taking into account the pharmacological relevance of heterocycle-fused natural steroids, the objective of the current study was to develop a multistep reaction sequence for the efficient synthesis of novel D-ring-condensed 5-amino-1-arylpyrazoles from dehydroepiandrosterone (DHEA). A condensation reaction of 16-formyl-DHEA with hydroxylamine afforded the corresponding oxime, which was demonstrated to be stable in one of its cyclic isoxazoline forms due to possible ring-chain tautomerism. The subsequent base-induced dehydration to a diastereomeric β-ketonitrile, followed by microwave-assisted heterocyclization with different arylhydrazines led to the desired pyrazoles. The generally good yields of the products depended slightly on the electronic character of the substituent present on the aromatic ring of the reagent. The proton dissociation processes of the DHEA-derived heterocycles were investigated in aqueous solution by UV-visible spectrophotometric titrations to reveal their actual chemical forms at physiological pH. The determined pKa values attributed to the pyrazole NH+ moiety were low (1.8–4.0) and varied by the different substituents of the benzene ring. The antiproliferative effects of the structurally similar compounds were screened in vitro on human cancer cells (namely on HeLa, U2Os, MCF-7, PC-3, and A549), along with a noncancerous cell line (MRC-5). The IC50 values of the most active derivative were determined on all cell lines.

scholarly journals Ultrasound-microwave assisted extraction of flavonoid compounds from Eucommia ulmoides leaves and an evaluation of their antioxidant and antibacterial activities

2020 ◽  
Vol 72 (2) ◽  
pp. 211-221
Author(s):  
Xiang Wang ◽  
Mi-Jun Peng ◽  
Zhi-Hong Wang ◽  
Qiu-Ling Yang ◽  
Sheng Peng
Keyword(s):  
Antibacterial Activities ◽  
Eucommia Ulmoides ◽  
Microwave Assisted Extraction ◽  
Ultrasound Extraction ◽  
Microwave Assisted ◽  
Flavonoid Compounds ◽  
Assisted Extraction ◽  
Ic50 Values ◽  
Burman Design

Ultrasound/microwave assisted extraction (UMAE) of flavonoid compounds from Eucommia ulmoides leaves was studied and the extraction conditions were optimized by the Plackett-Burman design (PBD) method combined with the Box-Behnken design (BBD). The antioxidant and antibacterial activities of the flavonoid extract were investigated. The results show that the optimal conditions were an ethanol concentration of 41%, microwave power of 178 W and an ultrasound extraction time of 26 min. Under these conditions, the yield of the flavonoid compounds was 2.454%?0.230%, which was higher than that after direct solvent extraction, ultrasound extraction and microwave extraction. The results of in vitro antioxidant assays showed that the flavonoid extract had scavenging capacity for DPPH, ABTS and hydroxyl radicals, with corresponding IC50 values of 30.76 mg/L, 21.09 mg/L, 248.4 mg/L, respectively. In addition, this extract exhibited strong antibacterial activity on Escherichia coli, Staphylococcus aureus and Salmonella typhimurium.

Antimycobacterial assessment and Microwave-assisted synthesis of 2-aryl-3-(4-methylphenylamino)thiazolidin-4-one derivatives

2021 ◽  
Vol 18 ◽  
Author(s):  
Saad Alghamdi ◽  
Mehnaz Kamal ◽  
Mohammad Asif
Keyword(s):  
Inhibitory Concentration ◽  
Aromatic Aldehydes ◽  
Microwave Assisted Synthesis ◽  
Alamar Blue ◽  
Mycobacterium Tuberculosis H37rv ◽  
Lead Compounds ◽  
Microwave Assisted ◽  
H37rv Strain ◽  
Antimycobacterial Agents

: This article reports the microwave-assisted synthesis, characterization, and evaluation of some -4-one derivatives (2a-2h) for their in-vitro antimycobacterial activities against Mycobacterium tuberculosis H37Rv strain by microplate Alamar blue assay (MABA) method. All these final compounds (2a-2h) were synthesized from Schiff’s bases, 1-arylidene-2-(4-methylphenyl)hydrazines (1a-1h), and thioglycolic acid by using zinc chloride as a catalyst. Compounds (1a-1h) were synthesized from the reaction of 4-methylhydrazine and appropriate aromatic aldehydes by Schiff’s reaction. Among the target compounds, 2-(4-ethoxyphenyl)-3-(4-methylarylamino)thiazolidin-4-one (2f) and 2-(4-ethylphenyl)-3-(4-methylarylamino)thiazolidin-4-one (2g) were promising with a minimum inhibitory concentration (MIC) of 12.5 μg/mL against M. tuberculosisH37Rv. Based on the preliminary results, compounds 2f and 2g were considered as lead compounds for the advanced design and development of antimycobacterial agents.

scholarly journals Microwave-assisted synthesis and biological evaluation of thiazole-substituted dibenzofurans

2018 ◽  
Vol 24 (3) ◽  
pp. 171-176
Author(s):  
N.H. Kumar Baba ◽  
D. Ashok ◽  
Boddu Ananda Rao ◽  
Sarasija Madderla ◽  
N.Y.S. Murthy
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Antimycobacterial Activity ◽  
Biological Evaluation ◽  
Microwave Assisted Synthesis ◽  
Good Activity ◽  
Gram Negative ◽  
Microwave Assisted ◽  
Synthesis And Biological Evaluation

AbstractNew thiazole-substituted dibenzofurans 7a–j were synthesized from dibenzofuran derivatives 5a–b and substituted thiosemicarbazones 6a–h under conventional and microwave irradiation conditions. The structures of all products were established on the basis of analytical and spectral data. The synthesized compounds were evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative strains. Compounds 7b, 7d and 7h are active against Bacillus subtilis (+ve), and compound 7i displays good activity against Pseudomonas aeruginosa (-ve) strain. Compounds 7a–j were also evaluated for their in vitro antimycobacterial activity, and compound 7b shows antimycobacterial activity against Mycobacterium bovis strain.

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