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a.ti-onchocerca.Meta.olites from Cyperus a.ticula.us:Isola.ion,In Vitro a.tivity a.d In Silico‘Drug-Likeness’

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Na.ura. Products a.d Bioprospecting 2014年第4期4卷 243-249页

作者： Jona.ha. a.unge Metuge Smith B.Ba.ia.a.Ja.es a.Mba. Fidele Ntie-Ka.g godf.ed a.ayimele Fidelis Cho-Ngwa a.DI Centre of Excellence Department of Biochemistry and Molecular BiologyFaculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon Depa.tment of Chemistry Faculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon Chemica. a.d Bioa.tivity Informa.ion Centre Chemistry DepartmentFaculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon

The a.ms of this investiga.ion were to isola.e a.tive ingredients from the roots/rhizomes of Cyperus a.ticula.us used a. herba. medicine in Ca.eroon for the trea.ment of huma. onchocercia.is a.d to a.sess the effica.y of the meta.olites on the Onchocerca.*** a.tifila.ia. a.tivity wa. eva.ua.ed in vitro on microfila.ia.(Mfs)a.d a.ult worms of the bovine derived Onchocerca.ochengi,a.close rela.ive of Onchocerca.*** wa. a.sessed in vitro on monkey kidney epithelia. *** structures of the a.tive compounds were determined using spectroscopic methods a.d their drug-likeness eva.ua.ed using Lipinski *** seconda.y meta.olites,a.J1[conta.ning musta.one(1)a. the ma.or component]a.d linoleic a.id or(9Z,12Z)-octa.eca.9,12-dienoic a.id(2)were *** compounds were found to kill both the microfila.ia. a.d a.ult worms of *** in a.dose dependent *** IC50s for a.J1 were 15.7 lg/mL for Mfs,17.4 lg/mL for a.ult ma.es a.d 21.9 lg/mL for a.ult fema.e worms while for linoleic a.id the va.ues were,15.7 lg/mL for Mfs,31.0 lg/mL for a.ult ma.es a.d 44.2 lg/mL for a.ult *** present report provides the first ever evidence of the a.ti-Onchocerca.effica.y of a.J1 a.d linoleic ***,these seconda.y meta.olites ma. provide a.lea. for design a.d development of new a.tifila.ia. a.ents.

关键词： Cyperus a.ticula.es Linoleic a.id Microfila.ia. Musta.one Onchocerca.ochengi Onchocerca.volvulus

Synthesis, Molecula. Structure a.d a.tiba.teria. a.tivity of 1-(4-Methoxybenza.dehyde)-4-Methylthiosemica.ba.one

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Interna.iona. Journa. of Orga.ic Chemistry 2017年第3期7卷 229-239页

作者： Ja.es a.eck Mba. godf.ed a.onglen ayimele Norbert Kodjio Joseph Ngwa.n Yong Emma.uel Ngwa.g Nfor Dona.ien Ga.sing Depa.tment of Chemistry University of Buea Buea Cameroon Depa.tment of Biochemistry Faculty of Science University of Dschang Dschang Cameroon

a.novel liga.d, 1-(4-methoxybenzylidene)-4-methylthiosemica.ba.one (MBT) derived from 4-methoxybenza.dehyde wa. synthesized a.d cha.a.terized by spectroscopic methods (IR, 1H NMR, 13C NMR), single crysta. X-ra. diffra.tion technique a.d physica. mea.s. MBT showed a.tiba.teria. a.tivity in vitro with MICs of 64 μg/mL (a.stra.n of Sa.monella.typhi (a.CC 6539)), 128 μg/mL (Sa.monella.typhi), 64 μg/mL (Sa.monella.pa.a.yphi a., 128 μg/mL (Sa.monella.pa.a.yphi B) a.d 64 μg/mL (Sa.monella.typhimurium). The results showed tha. MBT demonstra.ed modera.e in vitro a.tiba.teria. a.tivity a.a.nst a.stra.n of Sa.monella.typhi (a.CC 6539), Sa.monella.pa.a.yphi a. a.d Sa.monella.typhimurium, indica.ing its promise a. a.possible lea. for the discovery of a.tiba.teria. drugs.

关键词： Novel Schiff Ba.e a.tiba.teria. a.tivity Crysta. Structure

Synthesis, Molecula. Structure, a.ti-Pla.modia., a.timicrobia. a.d a.ti-Oxida.t Screening of (E)-1-(Phtha.a.in-1-yl)-1-[(Pyridin-2-yl)Ethylidene]Hydra.a.ine a.d 1-[2-(1-(pyridine-3- yl)ethylidene)hydra.inyl]phtha.a.ine

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Interna.iona. Journa. of Orga.ic Chemistry 2021年第3期11卷 91-105页

作者： a.gelbert F. a.a.tu godf.ed a. ayimele Jea. Jules K. Ba.keu edoua.d a. Na.tia.Pa.rick V. T. Fokou Fa.rice F. Boyom Emma.uel N. Nfor Bruno N. Lenta.Silvère a. Ngouela Depa.tment of Chemistry The University of Bamenda Bambili Cameroon Depa.tment of Chemistry University of Buea Buea Cameroon Depa.tment of Biochemistry The University of Bamenda Bambili Cameroon Depa.tment of Biochemistry University of Yaoundé I Yaoundé Cameroon Depa.tment of Chemistry Higher Teachers’ Training College University of Yaoundé I Yaoundé Cameroon Depa.tment of Orga.ic Chemistry Faculty of Science University of Yaoundé I Yaoundé Cameroon

Two new hydra.a.ine hydrochloride-derived Schiff ba.es: (E)-1-(Phtha.a.in- 1-yl)-1-[(Pyridin-2-yl)Ethylidene]Hydra.a.ine (PPEH), a.d 1-[2-(1-(pyridine- 3-yl)ethylidene)hydra.inyl]phtha.a.ine (PEHP), were synthesized a...

Two new hydra.a.ine hydrochloride-derived Schiff ba.esa.>:a.> (E)-1-(Phthalazin- 1-yl)-1-[(Pyridin-2-yl)Ethylidene]Hydralazine (PPEH), and 1-[2-(1-(pyridine- 3-yl)ethylidene)hydrazinyl]phthalazine (PEHP), were synthesized and partially characterized by spectroscopic and crystallographic methods including IR and X-ray. The single-crystal X-ray diffraction (SCXRD) analysis of PEHP indicatesa.> that the hydralazine moiety of both ligands possessesa.> the exocyclic C=N bond. Both, PPEH and PEHP were tested as antimicrobials and antiparasites. Just PEHP could be considered as slightly antiplasmodial and antibacterial agent. In effect, PPEH showed low antimicrobial activity against one bacterial strain with Minimum Inhibitory Concentration (MIC) value of 250 μg/ml while PEHP showed very interesting activity against 18 out of 19 bacterial strains with MIC of 31.25 -a.> 250 μg/ml compared to the standard drug, amoxicillin. PPEH and PEHP showed higher reducing activity on ferric ions compared to Vitamin C. On the other hand, both hidrazaline synthetized derivatives showeda.>a. style="font-fa.ily:Verda.a."> a. better reducing a.ents tha. Vita.in C on ferric io

关键词： Schiff Ba.e Hydra.a.ine Hydrochloride a.ti-Pla.modia. a.tivity a.timicrobia. a.tivity a.ti-Oxida.t a.tivity

Novel Hydra.a.ine Schiff Ba.e Deriva.ives a.d Their a.timicrobia., a.tioxida.t a.d a.tipla.modia. Properties

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Interna.iona. Journa. of Orga.ic Chemistry 2020年第1期10卷 1-16页

作者： a.gelbert F. a.a.tu Ya.nick Stepha.e F. Fonga.g godf.ed a. ayimele edoua.d a. Na.tia.Pa.rick V. T. Fokou Fa.rice F. Boyom Celine K. Ngwa.g Bruno N. Lenta.Silvère a. Ngouela Depa.tment of Chemistry The University of Bamenda Bambili Cameroon Depa.tment of Chemistry University of Maroua Maroua Cameroon Depa.tment of Chemistry University of Buea Buea Cameroon Depa.tment of Biochemistry The University of Bamenda Bambili Cameroon Depa.tment of Biochemistry University of Yaoundé I Yaoundé Cameroon Depa.tment of Chemistry Higher Teachers’ Training College University of Yaoundé I Yaoundé Cameroon Depa.tment of Orga.ic Chemistry Faculty of Science University of Yaoundé I Yaoundé Cameroon

Two novel Schiff ba.es, 3-[1-(2-(phtha.a.in-1-yl)hydra.ono)ethyl)-1,3-oxa. zina.e (PHEO) a.d 2-[(2-(phtha.a.in-1-yl)hydra.ono)methyl]phenol (PHMP), derived from hydra.a.ine hydrochloride, a. effective drug a.a.nst hypertension, were synthesized a.d cha.a.terized by spectroscopic methods, Infra.ed (IR), Proton Nuclea. Ma.netic Resona.ce (1H NMR) a.d Ca.bon-13 Nuclea. Ma.netic Resona.ce (13C NMR). PHEO showed low a.timicrobia. a.tivity a.a.nst one ba.teria. stra.n with MIC va.ue of 250 μg/ml while PHMP showed interesting a.tivity a.a.nst 4 ba.teria. stra.ns with MIC of 31.25 - 250 μg/ml compa.ed to the sta.da.d drug, a.oxicillin. PHEO a.d PHMP showed higher reducing a.tivity on ferric ions compa.ed to Vita.in C. On lipid peroxida.ion, PHEO showed higher inhibition while PHMP showed lower inhibition compa.ed to Vita.in C. Both compounds presented lower stimula.ing effect a.d lower ca.a.a.e a.tivity compa.ed to the sta.da.d Vita.in C. PHEO a.d PHMP showed less tha. 80% inhibition in the prelimina.y a.tipla.modia. a.sa. a.d so were not considered for the dose-response studies.

关键词： Hydra.a.ine Hydrochloride Schiff Ba.es a.timicrobia. a.ti-Oxida.t a.ti-Pla.modia. a.tivities