Microwave Assisted Synthesis and in vitro Antimicrobial Activities of Fluorine Containing 4-Benzofuran-2-yl-6-phenyl-pyrimidin-2-ylamines

2014 ◽  
Vol 10 (4) ◽  
pp. 409-417 ◽  
Author(s):  
Tejpal Chundawat ◽  
Nutan Sharma ◽  
Sunita Bhagat
Keyword(s):  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted

scholarly journals Microwave assisted synthesis and antimicrobial activity of some novel pyrimidine derivatives

2007 ◽  
Vol 72 (2) ◽  
pp. 109-117 ◽  
Author(s):  
S.J. Vaghasia ◽  
V.H. Shah
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Mass Spectral Data ◽  
Pyrimidine Derivatives ◽  
Plate Method ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
New Compounds

The synthesis of thiazolo[5,4-d]pyrimidines can be achieved from different 5- thiazolidinones, 2-butyl-1H-imidazole-5-carbaldehyde and thiourea using microwave irradiation within 5 min. The structures of the products were supported by FTIR, PMR and mass spectral data. The in vitro antimicrobial activity of the synthesized thiazolo[5,4-d]pyrimidines 1a-j, having substituents at the 1- and 3-positions, were determined by the cup-plate method against several standard strains chosen to define the spectrum and potency of the new compounds. The antimicrobial activities of the thiazolo[5,4-d]pyrimidines 1a-j are compared with those of known chosen standard drugs, viz. ampicillin, chloramphenicol, ciprofloxacin, norfloxacin and griseofulvin. .

scholarly journals Comparative studies on conventional and microwave-assisted synthesis of a series of 2,4-di and 2,3,4-trisubstituted benzimidazo[1,2-a] pyrimidines and their antimicrobial activities

2009 ◽  
Vol 7 (3) ◽  
pp. 337-342 ◽  
Author(s):  
Oztekin Algul ◽  
Asiye Meric ◽  
Serpil Polat ◽  
N. Didem Yuksek ◽  
Mehmet Serin
Keyword(s):  
Reaction Time ◽  
Microwave Irradiation ◽  
Comparative Studies ◽  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Microwave Irradiation Method ◽  
Yield Increase ◽  
Microwave Assisted ◽  
Mic Value

AbstractComparative studies were performed on a series of 2,4-di and 2,3,4-trisubstituted benzimidazo[1,2-a]pyrimidines, which were synthesized with conventional and microwave heating methods. In microwave irradiation method, approximately, 95–97.5% of the reaction time was increased and 1–45% yield increase was obtained. All compounds were able to inhibit the growth of the screened microorganisms in vitro with MIC values between 3.9–250 μg mL−1. The highest activity was expressed by compound IIId (2,4-diphenyl-benzo[4,5]imidazo[1,2-a] pyrimidine), which has the MIC value of 3.9 μg mL−1 and 31.2 μg mL-1 for Penicillium natatum ATCC 24791 and E. faecalis ATCC 29212, respectively.

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 Conventional and Microwave Assisted Synthesis of New Triazole Derivatives and Evaluation of Their Antimicrobial Activities

2019 ◽  
pp. 277-286
Author(s):  
Zeynep Özdemir ◽  
İnci Selin Doğan ◽  
Mehmet Abdullah Alagöz ◽  
Hasan Erdinç Sellitepe ◽  
Didem Kart
Keyword(s):  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Triazole Derivatives ◽  
Microwave Assisted

scholarly journals Microwave Assisted Synthesis and Antimicrobial Activities of Some 2-Amino-4-aryl-3-cyano-6-(4’-hydroxy phenyl)-pyridines

2011 ◽  
Vol 8 (1) ◽  
pp. 119-122 ◽  
Author(s):  
Priya Gothwal ◽  
Gunwanti Malhotra ◽  
Y. K. Srivastava
Keyword(s):  
Antimicrobial Activity ◽  
Ammonium Acetate ◽  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted

4’-Hydroxy chalcones were treated with malononitrile in the presence of ammonium acetate under solventless microwave assisted condition to get 2-amino-4-aryl-3-cyano-6-(4’-hydroxy phenyl)-pyridines. The prepared compounds were screened for their antimicrobial activity; some of them have exhibited promising antimicrobial activity.

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...

Microwave-assisted synthesis and in vitro stability of N-benzylamide non-steroidal anti-inflammatory drug conjugates for CNS delivery

2019 ◽  
Vol 29 (12) ◽  
pp. 1487-1491 ◽  
Author(s):  
Brandon D. Eden ◽  
Andrew J. Rice ◽  
Troy D. Lovett ◽  
Olivia M. Toner ◽  
Evan P. Geissler ◽  
...  
Keyword(s):  
Microwave Assisted Synthesis ◽  
Inflammatory Drug ◽  
Microwave Assisted ◽  
Drug Conjugates ◽  
Anti Inflammatory ◽  
In Vitro Stability ◽  
Cns Delivery
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