scholarly journals Microwave Assisted One Pot Synthesis of Tetrazole Based 3-hydroxy-4H-chromen-4-ones by modified Algar-Flynn-Oyamada reaction and their Antimicrobial activity

2019 ◽  
Vol 63 (4) ◽  
Author(s):  
ASHOK DONGAMANTI ◽  
Nagaraju Nalaparaju ◽  
Sarasija Madderla ◽  
Vijaya Lakshmi Bommidi

In the present work, we report the one pot synthesis of tetrazole based 3-hydroxy-4H-chromen-4-ones 3(a-g) from  4-(1H-tetrazol-5-yl)benzaldehyde and 2-hydroxy acetophenone using KOH and H2O2 by modified Algar-Flynn-Oyamada reaction under conventional and microwave irradiation conditions. In this technique, flavonols are synthesized without isolating chalcones, in good yields. All the synthesized compounds were characterized by IR, NMR, MS and elemental. All newly synthesized compounds were screened for their in-vitro antimicrobial activity against strains such as Staphylococcus aurous, Bacillus subtilis, Klebsiella pneumonia, Escherichia coli, Aspergillus Niger, Aspergillus flavus, and Fusarium oxysporum. The results of antimicrobial studies revealed that most of the compounds exhibit good activity.

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.


2021 ◽  
Vol 6 (3) ◽  
pp. 222-227
Author(s):  
Krishna A. Bhensdadia ◽  
Prakash L. Kalavadiya ◽  
Nilam H. Lalavani ◽  
Shipra H. Baluja

A novel series of dihydropyrido[2,3-d]pyrimidine derivatives were synthesized by multicomponent domino cyclization via the one-pot three component reaction of 6-amino uracil, substituted aryl aldehydes and N-methyl-1-(methylthio)-2-nitroethenamine in the presence of PTSA 10 mol% as a catalyst. The structures of these synthesized compounds were characterized by spectral analysis. Further the synthesized compounds screened for in vitro antimicrobial activity. Among all the compounds, compound 4b containing flouro substitution exhibited good inhibition against the tested species.


2009 ◽  
Vol 24 (5) ◽  
pp. 1095-1100 ◽  
Author(s):  
Kallappa Mahadevappa Hosamani ◽  
Harisha Reddy Seetharamareddy ◽  
Rangappa Sangappa Keri ◽  
Manohar Shirugumbi Hanamanthagouda ◽  
Mark G. Moloney

2020 ◽  
Vol 16 (4) ◽  
pp. 514-520
Author(s):  
Marwa A. Sh. Shehab ◽  
Mohamed El-Naggar ◽  
Rabab A. Ismail ◽  
Hala M. El Kafrawy ◽  
Amira Abood ◽  
...  

Background: Amongst the quinolone core structures, 8-hydroxyquinoline (8-HQ or quinolinol) stands out as the greatest frequently used therapeutic moietiy. This includes the most critical molecules in medicinal chemistry. Quinolinol remains a broad-spectrum ligand capable of chelating to a large number of metal ions. Methods: The synthesized quinolinols Mannich bases were screened for their in vitro antimicrobial activity against Staphylococcus aureus (ATTCC 6538), Escherichia coli (ATTCC 7839), Klebsiella pneumonia (ATCC10131). The antifungal activity of the prepared compounds was assessed against Candida albicans (10231), Aspergillus niger and Penicillium sp. The antioxidant activity of the established compounds was assessed by means of α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method. Results: The antimicrobial outcomes indicated that all the synthesized compounds excluding 5 and 9b displayed reasonable antibacterial activity against Staphylococcus aureus (ATTCC 6538) and Escherichia coli (ATTCC 7839) with an inhibition zones ranging from 13 to 23 mm. However, in the case of Klebsiella pneumonia (ATCC10131) only compound 6 did not show any activity. The results also indicated that compounds 2b and 3 were the most potent antibacterial compounds against the verified strains with minimum inhibitory concentration (MIC) values ranging from 0.05 to 0.5mg/ml. In the antifungal assay, all compounds showed good activity against Candida albicans (10231) except compounds 5 and 9b. However, in the case of Aspergillus niger and Penicillium sp. only compounds 2b and 3 showed good activity. In the antifungal assay, MIC values for compounds 2b and 3 ranged from 0.25 to 2.5 mg/ml against the specified fungal strains. The antioxidant activity was assessed using the DPPH scavenging activity method. The results indicated that 2b was the most active among all tested compounds, with almost double the antioxidant activity as compared with that of trolox (positive control). Conclusion: In this work, we describe the synthesis of new Mannich bases comprising 8-HQ (1) and its derivative (8). The resulted Mannich bases of type 2 were used in transamination reactions with hydrazine and hydrazine derivatives. The structures of the newly synthesized Mannich bases were confirmed based on the NMR spectroscopic data and elemental analysis. Antimicrobial and antioxidant activities were also assessed.


2016 ◽  
Vol 52 (3) ◽  
pp. 172-176 ◽  
Author(s):  
Dongamanti Ashok ◽  
Mohsin Ahmed Kifah ◽  
Bommidi Vijaya Lakshmi ◽  
Madderla Sarasija ◽  
Shaik Adam

Author(s):  
E. Ramya Sucharitha ◽  
Thupurani Murali Krishna ◽  
Ravinder Manchal ◽  
Gondru Ramesh ◽  
Sirassu Narsimha

2021 ◽  
Vol 14 (03) ◽  
pp. 249-253
Author(s):  
Nicholas Chinedu Ewelike ◽  
Joy Chinyere Okammadu ◽  
Vincent Ezechukwu Ogwudire ◽  
Raymond Ikechukwu Nnadozie

Methanolic and aqueous leaf extracts of Chrysophyllum albidum (African star apple) and Garcinia kola (bitter kola) were studied for in-vitro microbial activity using the disc diffusion technique. The aqueous and methanolic leaf extracts of Chrysophyllum albidum showed antimicrobial activity against Escherichia coli, Staphylococcus aureus and Candida albicans but showed no antibacterial activity against Klebsiella pneumonia. The methanolic leaf extract of Garcinia kola inhibited the growth of Escherichia coli, Staphylococcus aureus and Klebsiella pneumonia while the aqueous extract of the leaf inhibited the growth of Staphylococcus aureus and Escherichia coli. Both methanolic and aqueous leaf extracts of the plant showed no antifungal activity against Candida albicans. The minimum inhibitory concentrations of the leaf extracts of Chrysophyllum albidum ranged from 12.5 mgL-1 to 25 mgL-1 while those of Garcinia kola ranged from 25 mgL-1 to 50 mgL-1. The results obtained suggest that the leaves of these plants can be used in treating diseases caused by the test organisms. The further investigation on the crude extracts would characterize bioactive components of the leaves of Chrysophyllum albidum and Garcinia kola.


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