Synthesis of New Rhodanine, Thiazole, Quinazolin-4-One, Imidazolone and Pyranothiazole Derivatives Incorporating Antipyrine Moiety as Antimicrobial Agents
Issue:
Volume 3, Issue 2, April 2017
Pages:
8-18
Received:
15 April 2017
Accepted:
10 May 2017
Published:
5 June 2017
Abstract: A new series of heterocycles incorporating antipyrine moiety were synthesized via reactions of 4-aminoantipyrine 1 with carbon disulphide then alkylation and /or chloroacetic acid to produce dithiocarbamate and rhodanine 3, 4 and 9. Multi-component reaction (MCR) of 4-aminoantipyrine with carbon disulfide and DMAD afforded rhodanine 7. The interaction of 9 with diazonium salt, DMF-DMA, nitrous acid and aromatic aldehydes to give thiazolidinone derivatives 10, 11, 13 and 14, respectively. Pyranothiazole 16 was prepared from reaction of 9 with cinamonitrile 15. Thiazolidinone 18 and thiazole 19 derivatives were obtained from reactions of 9 with phenyl isothiocyanate in the presence of KOH then halogenated the pot salt with ethyl bromoacetate and chloroacetone, respectively. Thiourea derivative 20 was prepared from reaction of methyl dithiocarbamate 3 with 4-aminoantipyrine. pyrimidine derivatives 21 and 22 were obtained from cyclocondensation of 3 with dimer of ethyl cyanoacetate and malononitrile. Pyrazolotriazine 24 was prepared from interaction of 3 with hydrazine hydrate. copounds 26 and 28 were obtained via reaction of 3 with glycine and anthranilic acid. Compounds 30, 32 and 34 were prepared via reaction of thiourea 20 with EAA, ECA and DMAD. Reaction of diazonium chloride of 1 with NaN3 afforded azide 36 which rearranged to triazine 39. The structures of the newly synthesized compounds were elucidated via elemental analysis and spectral data. The synthesized products were evaluated for their antimicrobial and anti-fungal activity.
Abstract: A new series of heterocycles incorporating antipyrine moiety were synthesized via reactions of 4-aminoantipyrine 1 with carbon disulphide then alkylation and /or chloroacetic acid to produce dithiocarbamate and rhodanine 3, 4 and 9. Multi-component reaction (MCR) of 4-aminoantipyrine with carbon disulfide and DMAD afforded rhodanine 7. The interact...
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A Comparative Study on the Phytochemicals and Antimicrobial Activities of the Hexane Extracts of the Leaves of Tectona Grandis and Its Mistletoe
Uzama Danlami,
Okolo Simon
Issue:
Volume 3, Issue 2, April 2017
Pages:
19-22
Received:
17 May 2017
Accepted:
16 June 2017
Published:
25 July 2017
Abstract: A comparative study on the phytochemical constituents and antimicrobial activities of the hexane extracts of the leaves of Tectona grandis and its mistletoe was carried out. The phytochemical screening was carried out by adopting standard methods. Agar well diffusion method was employed for the antimicrobial screening of the extracts of the leaves of Tectona grandis and its mistletoe. The phytochemical screening results of hexane extract of Tectona grandis leaves revealed the presence of steroids, glycosides, saponins, terpenoids, flavonoids, cardiac glycosides and volatile oils, while the hexane extract of the mistletoe leaves revealed the presence of steroids, terpenoids, saponins, glycosides and cardiac glycosides. For the antimicrobial activities screening, the results revealed the hexane extract of the mistletoe leaves to have greater zone of inhibition in Staphylococcus aureus (24mm), Escherichia coli (26mm), Salmonella typhi (20mm) and Pseudomonas aeriginosa (12mm) than the hexane extract of the Tectona grandis leaves in Staphylococcus aureus (16mm), Escherichia coli (13mm), Salmonella typhi (18mm) and Pseudomonas aeriginosa (10mm). The hexane extracts of the leaves of Tectona grandis and its mistletoe were not active on the Klebsiella pneumonia. The result of the antimicrobial screening showed the extracts of the leaves of the mistletoe to be more active than the leaves of Tectona grandis. The leaf extracts of Tectona grandis and its mistletoe can serve as antibiotics in ethno medicine.
Abstract: A comparative study on the phytochemical constituents and antimicrobial activities of the hexane extracts of the leaves of Tectona grandis and its mistletoe was carried out. The phytochemical screening was carried out by adopting standard methods. Agar well diffusion method was employed for the antimicrobial screening of the extracts of the leaves ...
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