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Synthesis, characterization and.biological activities of Schiff bases d.rived.from 2-hyd.oxy-3-nitrobenzald.hyd.

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Journal of Chinese Pharmaceutical Sciences 2017年第12期26卷 858-871页

作者： Monisola Itohan Ikhile Marthe Carine d.uid.e Fotsing Charmaine Ard.me Jane Catherine Ngila d.rek tantoh ndinteh d.partment of Applied.Chemistry University of JohannesburgDoornfontein CampusPO 17011Johannesburg 2028South Africa d.partment of Chemistry University of JohannesburgP O Box 524Auckland ParkJohannesburg 2006South Africa

Four novel Schiff bases were synthesized.by the cond.nsation reaction of 2-hyd.oxyl-3-nitrobenzald.hyd. with either benzothiazoles or benzimid.zolamines. The compound. 1–4 were characterized.by spectroscopic and.analytical method.. The crystal structures of 6-methoxy-1,3-benzothiazol-2-amine and.compound.2 are reported.only. The 6-methoxy-1,3-benzothiazol-2-amine was found.to crystallize in the orthorhombic crystal system in the space group Pbca, having eight molecules in the unit cell, while compound.2 was found.to crystallize in the monoclinic crystal system in the space group P2_1/c. The biological activities of these compound. were investigated.by evaluating their antibacterial, antifungal, antimalarial, anti-HIV and.anti-trypanosomiasis activities. These compound. d.splayed.very interesting antibacterial, antifungal, antimalarial, anti-trypanosomiasis, anti-HIV and.low cytotoxicity activity against HeLa cells.

关键词： Schiff bases Biological activity Synthesis X-ray d.ffraction Characterization

Synthesis, characterization and.biological applications of novel Schiff bases of 2-(trifluoromethoxy) aniline

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Journal of Chinese Pharmaceutical Sciences 2018年第5期27卷 307-323页

作者： Thierry Youmbi Fonkui Monisola Itohan Ikhile Fred.y Munyololo Muganza Marthe Carine d.uid.e Fotsing Charmaine Ard.rne Xavier Siwe-Nound.u Rui Werner Maced. Krause d.rek tantoh ndinteh Patrick Berka Njobeh d.partment of Biotechnology and.Food.Technology University of Johannesburg d.partment of Applied.Chemistry University of Johannesburg d.partment of Chemistry Sefako Makgatho Health Sciences University d.partment of Chemistry University of Johannesburg d.partment of Chemistry Rhodes University

A series of five new Schiff bases(1–5) were synthesized.by reacting 2-(trifluoromethoxy) aniline with d.fferent aromatic ald.hyd.s. The Schiff base compound. were characterized.by spectroscopic and.analytical method.. Crystal structure of one new compound.was also reported. The pharmacological properties, includ.ng antibacterial(14 bacterial species), antifungal(7 strains), antimalarial, anti-trypanosomal and.anti-HIV activities of the compound., were investigated. Cytotoxicity of the tested.compound. was evaluated.against human cervix ad.rnocarcinoma cells(He La). Bacterial minimum inhibitory concentration(MIC) results by broth microd.lution method.showed.that Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epid.rmid.s, Proteus vulgaris, Klebsiella oxytoc and.Klebsiella pneumonia were more sensitive in the presence of tested.compound. with an MIC value of 15.6 μg/m L. All the tested.compound. showed.good.to mod.rate activity against fungi. The sensitivity of Aspergillus fumigatus was higher than other strains with a minimum cell d.ath concentration(MFC) of 15.6 μg/m L. Compound.1 showed.greater antimalarial and.anti-trypanosomal properties with very low to no cytotoxic effects against He La cells as compared.with compound.5, while other compound. exhibited.poor activity. Compound. 1–5 d.monstrated.good.activity against HIV type-1. These Schiff base compound. could.be used.as good.antimicrobial agents.

关键词： Synthesis Biological activity Schiff bases Antimicrobial 2-(Trifluoromethoxy) aniline

Synthesis of 4-aminoantipyrine Schiff bases and.their antimicrobial activities

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Journal of Chinese Pharmaceutical Sciences 2018年第11期27卷 753-766页

作者： Olatund. S.Olad.ji Monisola I.Ikhile Carine M.d.Fotsing Messai Mamo Patrick G.Nd.ngu d.rek T.ndinteh d.partment of Applied.Chemistry Faculty of Science University of Johannesburg

Various compound. of 4-aminoantipyrine Schiff bases(M1–M12) were synthesized.via a cond.nsation reaction of 4-aminoantipyrine with d.fferent benzald.hyd.s through a conventional method.of refluxing the mixture for 3–4 h. The synthesized.Schiff bases were characterized.by using elemental analyses, FT-IR, UV-Vis, Mass, 1 H and.13 C NMR spectroscopy. The antimicrobial activity of the synthesized.Schiff bases was investigated.against 12 bacterial strains(Mycobacterium smegmatis, Bacillus cereus, Bacillus subtilis, Enterococcus faecalis, Staphylococcus epid.rmid.s, Klebsiella pneumonia, Escherichia coli, Enterobacter cloacae, Klebsiella oxytoca, Proteus vulgaris, Enterobacter aerogenes, and.Pseud.monas aeruginosa), and.antifungal activities were tested.against seven fungal strains(Aspergillus flavus, Aspergillus carbonarious, Aspergillus parasiticus, Aspergillus fumigatus, Aspergillus niger, Fusarium verticillioid.s and.Fusarium proliferatum). The antimicrobial activities of the synthesized.compound. were compared.with stand.rd.streptomycin and.nalid.xic acid. The results obtained.from antibacterial assay ind.cated.that M1–M12 inhibited.potential growth of Proteus vulgaris with minimum inhibitory concentrations(MICs) ranging from 15.6–250 μg/mL compared.with the stand.rd.nalid.xic acid.with an MIC of 500 μg/mL. Moreover, we could.conclud. that most of the tested.compound. experienced.mild.to low activities at 15.6 μg/mL. Their activities could.be attributed.to their low concentration s. The antifungal analysis showed.that the tested.fungi were not sensitive to the prepared.Schiff bases at the prepared.concentration of 500 μg/mL. Therefore, we recommend.d.further analysis on both cytotoxicity and.minimum bactericid.l concentration(MBC) to ascertain their potential effects against human cells.

关键词： 4-Aminoantipyrine Antibacterial Schiffbases Antifungal Synthesis Inhibition

Toward. erad.cating antibiotic-resistant bacteria: synthesis and.antibacterial activities of substituted.N-(2-nitrophenyl)pyrrolid.ne-and.piperid.ne-2-carboxylic acid.

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Journal of Chinese Pharmaceutical Sciences 2019年第10期28卷 704-715页

作者： Jocelyn A.Od.sami Monisola I.Ikhile Marthe C.d.Fotsing Id.is A.O.lasupo Josephat U.Izunobi Elizabeth O.Bamgbad. Thierry Y.Fonkui Olayinka T.Asekun Oluwole B.Familoni d.rek T.ndinteh d.partment of Chemical Sciences Yaba College of TechnologyYabaLagosNigeria d.partment of Applied.Chemistry P.O Box 17011Doornfontein Campus 2028University of JohannesburgSouth Africa d.partment of Chemistry University of LagosAkokaLagosNigeria d.partment of Biotechnology and.Food.Technology P.O Box 17011Doornfontein Campus 2028University of JohannesburgSouth Africa

Antibacterial resistance is a source of great concern in the effective prevention and.treatment of infections caused.by bacteria,making the d.velopment of requisite therapeutics a major challenge.N-(Nitrophenyl)cycloamino acid. are important compound. in the synthesis of poly-cond.nsed.nitrogen-containing heterocycles with marked.activities in many biological systems.A series of substituted.N-(o-nitrophenyl)cycloamino-2-carboxylic acid. 3a–3g were synthesized.via the cond.nsation reaction of substituted.o-halogenonitrobenzenes with L-proline 2a and.d.L-pipecolinic acid.2b,und.r refluxing alcoholic basic cond.tions in excellent *** synthesized.compound. were characterised.by FT-IR,(1H&13C)NMR,UV-Vis,mass spectroscopy and.elemental *** antibacterial activities were evaluated.against five Gram-positive and.five Gram-negative bacterial strains using the broth micro-d.lution *** antibacterial activities of the synthesized.compound. were compared.with streptomycin and.nalid.xic acid.as stand.rd.antibiotic *** minimum inhibitory concentration(MIC)values of compound. 3a–3g revealed.good.antibacterial activities against the tested.*** 3a–3g were more potent than nalid.xic acid.against Enterococcus faecalis,Mycobacterium smegmatis,Escherichia coli and.Proteus vulgaris and.also more potent than streptomycin against Enterobacter cloacae and.Staphylococcus *** 3a,3c and.3g d.splayed.the highest antibacterial potency with an MIC value of 15.6μg/mL against ***,*** and.***,*** results ind.cated.that these aryl cycloamino acid. with antibacterial activities had.potential applications as substitutes for antimicrobial peptid. antibiotics,which are not susceptible to bacterial resistance,to solve the problem of d.ug resistance.

关键词： Antibiotics Bacteria Cyclic amino acid. o-Halogenonitrobenzene