scholarly journals Microwave-Assisted Synthesis of 2-(5-(5-(4-Substituted phenyl)-2-(5-methoxy- 2H-chromen-3-yl)-1H-imidazol-1-yl)alkyl)-1H-benzo[de]isoquinoline- 1,3(2H)-dione Derivatives and their Antimicrobial Activity

2020 ◽  
Vol 32 (4) ◽  
pp. 839-844
Author(s):  
D. Ashok ◽  
K. Ramakrishna ◽  
Nalaparaju. Nagaraju ◽  
Ravinder Dharavath ◽  
M. Ram Reddy ◽  
...  

A method for the synthesis of several imidazoles containing isoquinoline scaffolds under conventional and microwave irradiation methods. In the microwave irradiation method gives higher yields with in shorter reaction time as compared to conventional heating method, using green solvents and eco-friendly reaction conditions. All the synthesized derivatives were characterized by IR, NMR and Mass spectral analysis. Furthermore, the title compounds were screened for their in vitro antimicrobial activity against bacteria such as Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Klebsiella pneumonia as well as fungi such as Aspergillus niger, Aspergillus flavus and Fusarium oxysporum. The compounds 8a, 8d, 8e and 8h exhibited better antimicrobial activity against all organisms.

2016 ◽  
Vol 81 (8) ◽  
pp. 851-858 ◽  
Author(s):  
Dongamanti Ashok ◽  
Velagapuri Rao ◽  
Rangu Kavitha

A series of new benzodiazepines 4a-h have been synthesized by Michael addition of chalcones 3a-h with o-phenylenediamine (OPDA) in presence of sodium acetate under conventional heating and microwave irradiation. Structures of the newly synthesized benzodiazepines 4a-h have been established on the basis of IR, 1H & 13C NMR and mass spectral data and tested for antimicrobial activity.


2007 ◽  
Vol 72 (2) ◽  
pp. 109-117 ◽  
Author(s):  
S.J. Vaghasia ◽  
V.H. Shah

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. .


2015 ◽  
Vol 80 (3) ◽  
pp. 305-313 ◽  
Author(s):  
Dongamanti Ashok ◽  
Bommidi Lakshmi ◽  
Sidda Ravi ◽  
Arram Ganesh

A series of pyrazolines 4a-g have been synthesized by Michael addition of chalcones 3a-g with hydrazine hydrate in presence of sodium acetate under conventional heating and microwave irradiation. Structures of the newly synthesized chalcones 3a-g and pyrazolines 4a-g have been established on the basis of IR, 1H & 13C NMR and mass spectral data. All the synthesized compounds were screened for their antimicrobial activity. Some of the compounds shown very good activity compared to standard drugs against all pathogenic bacteria and fungi.


2009 ◽  
Vol 7 (3) ◽  
pp. 337-342 ◽  
Author(s):  
Oztekin Algul ◽  
Asiye Meric ◽  
Serpil Polat ◽  
N. Didem Yuksek ◽  
Mehmet Serin

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.


2018 ◽  
Vol 83 (12) ◽  
pp. 1305-1313
Author(s):  
Dongamanti Ashok ◽  
Nalaparaju Nagaraju ◽  
Madderla Sarasija ◽  
Vijaya Lakshmi

A series of novel tetrazole scaffolds containing chalcones 4a?e and aurones 5a?e were synthesized under conventional and microwave irradiation conditions. All the newly synthesized compounds were characterized by IR, NMR and mass spectral data. Furthermore, the title compounds were screened in vitro for their antimicrobial activity against bacteria, such as Staphylococus aureus, Bacillus subtilis, Klebsiella pneumoniae and Escherichia coli, as well as fungi, such as Aspergillus niger, A. flavus and Fusarium oxysporum. Some of the compounds showed very good activity compared to standard drugs against all the tested pathogenic bacteria and fungi.


2019 ◽  
Vol 84 (3) ◽  
pp. 237-244
Author(s):  
Dongamanti Ashok ◽  
Rangu Kavitha ◽  
Srinivas Gundu ◽  
Madderla Sarasija

A new series of 6-[3-aryl-1-phenyl-4?,5?-dihydro[4,5?-bi-1H-pyrazol]-3?-yl]-2H-chromen-5-ol derivatives was synthesized by Michael addition of chalcones 5a?j with hydrazine hydrate in presence of sodium acetate under conventional heating and microwave irradiation. Structural assignment of the products was confirmed based on IR, 1H-NMR, 13C-NMR, MS and analytical data. All the synthesized compounds 6a?j were screened for their antimicrobial activity against various bacterial and fungal strains. Most of the compounds exhibited variable range of antimicrobial activity and compounds 6c?f and 6i showed promising antimicrobial potency.


2019 ◽  
Vol 6 (1) ◽  
pp. 44-53 ◽  
Author(s):  
Meenu Beniwal ◽  
Neelam Jain

Background: This paper describes the synthesis of novel thiazolidin-4-one substituted pyrazole derivatives from the condensation reaction of hydrazide with acetophenone derivatives. Herein we describe the synthesis of fourteen compounds by microwave irradiation method. The synthesized compounds are in excellent yield by utilizing microwave irradiation heating. Objective: Compounds using different aromatic or heteroaromatic compounds should be synthesized and screened for their antibacterial activity to explore the possibility of pyrazole substituted thiazolidin- 4-ones as a novel series of antimicrobials. Method: Synthesis of thiazolidin-4-one substituted pyrazole derivatives was carried out under microwave radiation. Result: These compounds were identified on the basis of melting point range, Rf values, IR, 1HNMR and mass spectral analysis. These compounds were evaluated for their in vitro antimicrobial activity and their Minimum Inhibitory Concentration (MIC) was determined. Among them Comp. 4b and Comp. 4k possess appreciable antimicrobial and antifungal activities. Conclusion: A novel series of Thiazolidin-4-one substituted pyrazole were synthesized under microwave irradiation method and identified on the basis of melting point range, Rf values, IR, 1HNMR, mass spectral data and elemental analysis. The compounds were subjected to in vitro antimicrobial screening and their Minimum Inhibitory Concentrations (MIC) were determined. Among all the tested compounds, two compounds 4b and 4k exhibited moderate to significant activity against all the tested strains of bacteria and fungus were found to have appreciable antimicrobial activities. The results of antibacterial activity showed that compounds containing electron withdrawing groups were found to be more active than the compounds containing electron releasing groups.


Author(s):  
Devidas G. Anuse ◽  
Suraj N. Mali ◽  
Bapu R. Thorat ◽  
Ramesh S. Yamgar ◽  
Hemchandra K. Chaudhari

Background: Antimicrobial resistance is major global health problem, which is being rapidly deteriorating the quality of human health. Series of substituted N-(benzo[d]thiazol-2-yl)-2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)acetamide (3a-j) were synthesized from substituted N-(benzo[d]thiazol-2-yl)-2-chloroacetamide/bromopropanamide (2a-j) and 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole (2) and further evaluated for their docking properties and antimicrobial activity. Methods: All synthesized compounds were characterized by FT-IR, NMR and Mass spectral analysis. All compounds were allowed to dock against different antimicrobial targets having PDB ID: 1D7U and against common antifungal target having PDB ID: 1EA1. Results: The compounds 3d and 3h were showed good activity against Methicillin-resistant Staphylococcus aureus (MRSA, resistance Gram-positive bacteria). All synthesized compounds showed good to moderate activity against selected bacterial and fungal microbial strains. If we compared the actual in-vitro antimicrobial activity and in-silico molecular docking study, we found that molecules 3i and 3h were more potent than the others. Conclusion: Our current study would definitely pave the new way towards designing and synthesis of more potent 2-aminobenzothiazoles derivatives.


2020 ◽  
Vol 7 (3) ◽  
pp. 183-195
Author(s):  
Musa Özil ◽  
Emre Menteşe

Background: Benzoxazole, containing a 1,3-oxazole system fused with a benzene ring, has a profound effect on medicinal chemistry research owing to its important pharmacological activities. On the other hand, the benzoxazole derivative has exhibited important properties in material science. Especially in recent years, microwave-assisted synthesis is a technique that can be used to increase diversity and quick research in modern chemistry. The utilization of microwave irradiation is beneficial for the synthesis of benzoxazole in recent years. In this focused review, we provide a metaanalysis of studies on benzoxazole in different reaction conditions, catalysts, and starting materials by microwave technique so far, which is different from conventional heating. Methods: Synthesis of different kind of benzoxazole derivatives have been carried out by microwave irradiation. The most used method to obtain benzoxazoles is the condensation of 2-aminophenol or its derivatives with aldehydes, carboxylic acids, nitriles, isocyanates, and aliphatic amines. Results: Benzoxazole system and its derivatives have exhibited a broad range of pharmacological properties. Thus, many scientists have remarked on the importance of the synthesis of different benzoxazole derivatives. Conventional heating is a relatively inefficient and slow method to convey energy in orientation to the reaction medium. However, the microwave-assisted heating technique is a more effective interior heating by straight coupling of microwave energy with the molecules. Conclusion: In this review, different studies were presented on the recent details accessible in the microwave- assisted techniques on the synthesis of the benzoxazole ring. It presents all examples of such compounds that have been reported from 1996 to the present. Benzoxazoles showed an extensive class of chemical substances not only in pharmaceutical chemistry but also in dyestuff, polymer industries, agrochemical, and optical brighteners. Thus the development of fast and efficient achievement of benzoxazoles with a diversity of substituents in high yield is getting more noteworthy. As shown in this review, microwave-assisted synthesis of benzoxazoles is a very effective and useful technique.


2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna

We report here an easy, efficient and green synthetic protocol for the (E)-1-aryl-3-(2-morpholinoquinolin-3-yl)prop-2-en-1-ones by the Claisen-Schmidt condensation of 2-morpholinoquinoline-3-carbaldehyde and different substituted acetophenones by using 1-butyl-3-methylimidazolium tetrafluoroborate (Bmim)BF4. The compounds were characterized by using 1H NMR, 13C NMR and mass spectral data and screened there in vitro antimicrobial activity against different bacterial and fungal organisms.


Sign in / Sign up

Export Citation Format

Share Document