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 3,5-Disubstituted Thiazolidine-2,4-Diones: Design, Microwave-Assisted Synthesis, Antifungal Activity, and ADMET Screening

2018 ◽  
Vol 23 (8) ◽  
pp. 807-814 ◽  
Author(s):  
Gabriel Marc ◽  
Anca Stana ◽  
Adrian Pîrnău ◽  
Laurian Vlase ◽  
Dan C. Vodnar ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Docking Study ◽  
Docking Studies ◽  
Microwave Assisted Synthesis ◽  
Molecular Fragments ◽  
In Silico Screening ◽  
Minimum Fungicidal Concentration ◽  
Microwave Assisted

A series of 12 new thiazolidine-2,4-dione derivatives were obtained by microwave-assisted synthesis. All compounds were physicochemically characterized by quantitative elemental C, H, N, S analysis and spectral data (mass spectrometry [MS], infrared [IR], and nuclear magnetic resonance [NMR]), with the results being in agreement with the expected data. An in vitro screening performed on Candida albicans ATCC 10231 showed their moderate antifungal activity, which was further investigated by determining the minimum inhibitory concentration and minimum fungicidal concentration values for the most active compounds on four strains of Candida. The molecular docking studies, performed against a fungal lanosterol 14α-demethylase, emphasized the importance of different molecular fragments in the compounds’ structures for their antifungal activity. The synthesized compounds were subjected to in silico screening for the prediction of their absorption, distribution, metabolism, excretion, and toxicity (ADMET) and molecular properties. The results of the antifungal activity assays, docking study, and ADMET predictions revealed that the synthesized compounds are potential anti- Candida agents that might act by interacting with the fungal lanosterol 14α-demethylase and could be further optimized and developed as antifungal agents.

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.

scholarly journals Microwave assisted Synthesis and Antimicrobial Activity of Substituted Pyrrolidinone derivatives

2020 ◽  
Vol 13 (1) ◽  
pp. 227-231
Author(s):  
Marapala Kumara Swamy ◽  
N. Venkatesh ◽  
M. Swapna ◽  
P. Venkateswar Rao
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Aldehydes ◽  
Microwave Assisted Synthesis ◽  
Water Medium ◽  
One Pot ◽  
Standard Drug ◽  
Microwave Assisted ◽  
Three Component Reaction ◽  
Fungal Organisms

A microwave assisted green synthetic methodoloy was developed for the synthesis various substituted pyrrolidinones derivatives by the one-pot three component reaction of aromatic aldehydes, aniline with dialkylbut-2-ynedioate in the presence of p-TsOH in water medium. The compounds were screened for their in vitro antimicrobial activity against four bacterial organism and two fungal organisms, resulted moderate to good activity with compared to their standard drug.

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 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.

Discovery of new chiral sulfonamides bearing benzoxadiazole as HIF inhibitors for non-small cell lung cancer therapy: design, microwave-assisted synthesis, binding affinity, in vitro antitumoral activities and in silico studies

2022 ◽  
Author(s):  
Demet Taşdemir ◽  
Ayşegül Karaküçük-İyidoğan ◽  
Yasemin Saygideger ◽  
EMİNE Elçin Emre ◽  
Tuğba Taşkın-Tok ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Treatment Strategies ◽  
Microwave Assisted Synthesis ◽  
Hypoxia Inducible Factors ◽  
Small Cell Lung ◽  
Microwave Assisted ◽  
In Silico Studies ◽  
Lung Cancer Therapy ◽  
Therapy Design

Hypoxia-inducible factors (HIF), one of the targeted treatment strategies with a rising promise in lung cancer, are known to play a role in tumor growth and other oncogenic properties in...

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