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Utiliza.ion of a.Propenone Deriva.ive in the Synthesis of Some New Cytotoxic Heterocyclic Compounds

RUSSIa. JOURNa. OF ORGa.IC CHEMISTRY 2020年第3期56卷 465-475页

作者： Ma.sour, S. Y. Sa.ed, G. H. a.-Ha.im, S. a. marzouk, M. I. Sha.a., S. S. Ain Shams Univ Dept Chem Fac Sci Cairo 11566 Egypt Ain Shams Univ Dept Math & Phys Fac Engn Cairo 11566 Egypt Ain Shams Univ Chem Subdept Fac Engn Cairo 11566 Egypt

New dia.yl-substituted pyridine, pyrimidine, pyra.ole, a.d isoxa.ole deriva.ives bea.ing biphenyl-4-yl a.d 4-(dimethyla.ino)phenyl substituents ha.e been prepa.ed by the rea.tion of 1-(1,1 '-biphenyl-4-yl)-3-[4-(dimethyla.ino)phenyl]prop-2-en-1-one with different nitrogen nucleophiles such a. urea. thiourea. gua.idine hydrochloride, semica.ba.ide hydrochloride, thiosemica.ba.ide, a.d hydroxyla.ine hydrochloride. Nicotinonitrile deriva.ive ha. been synthesized by one-pot rea.tion of 4-a.etylbiphenyl, 4-(dimethyla.ino)benza.dehyde, a.d ma.ononitrile in the presence of a.monium a.eta.e under microwa.e irra.ia.ion, a.d subsequent trea.ment with hydra.ine hydra.e ga.e 4,6-dia.yl-1H-pyra.olo[3,4-b]pyridin-3-a.ine. The beha.ior of 4,6-dia.ylpyrimidin-2-a.ine towa.d ca.bon electrophiles ha. been investiga.ed by rea.ting it with p-toluenesulfonyl chloride, a.etyl chloride, ethyl a.etoa.eta.e, ethyl cya.oa.eta.e, a.d nitrous a.id to a.ford the corresponding N-substituted deriva.ives. 3,5-Dia.yl-4,5-dihydro-1H-pyra.ole-1-ca.boxa.ide rea.ted with p-toluenesulfonyl chloride a.d phenylhydra.ine to produceN-tosyl ca.boxa.ide a.d ca.bohydra.ona.ide deriva.ives, respectively. Trea.ment of a.a.ogous pyra.ole-1-ca.bothioa.ide with phenyl isothiocya.a.e, p-toluenesulfonyl chloride, a.d chloroa.etyl chloride a.fordedN-(phenylca.ba.othioyl), N-tosyl, a.d a.inoa.eta.ide deriva.ives, respectively. a.l the synthesized compounds were cha.a.terized by(1)H NMR, IR, a.d ma.s spectra.a.d elementa. a.a.yses. Some of the newly synthesized compounds were eva.ua.ed for theirin vitro cytotoxic a.tivity a.a.nst HePG-2 a.d MCF-7 cell lines. 4-(1,1 '-Biphenyl-4-yl)-6-[4-(dimethyla.ino)phenyl]-5,6-dihydropyrimidine-2(1H)-thione a.d 4-[5-(1,1 '-biphenyl-4-yl)-4,5-dihydro-1,2-oxa.ol-3-yl]-N,N-dimethyla.iline displa.ed a.promising growth inhibitory effect towa.d the two cell lines in compa.ison with the sta.da.d drug doxorubicin.

关键词： pyrimidine pyra.ole isoxa.ole cya.opyridine

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Experimenta. a.d Numerica. Investiga.ion of a.Novel Fra.ta. Tube Configura.ion in Helica.ly Tube Hea. Excha.ger

SSRN

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SSRN 2022年

作者： marzouk, Seif a. a.ou, M.M. a.-Sood El-Sa.d, Ema. M.S. Younes, M.M. El-Fa.ha.a.y, Ma.da.K. Mechanical Engineering Dept. Faculty of Engineering Kafrelsheikh University Kafrelsheikh Egypt Mechanical Power Engineering Dept Faculty of Engineering Damietta University Damietta Egypt

The effects of innova.ive fra.ta. configura.ion in helica.ly tubula. hea. excha.gers on therma. a.d hydra.lic performa.ce a.e investiga.ed using numerica. a.d experimenta. methods in this work. With Reynolds (Re) numbers ra.ging from 12025 to 21220, the overa.l hea. tra.sfer coefficient (U), pressure drop (∆P), a.d coefficient of performa.ce (COP)a.e investiga.ed. The fluid flow within a.d outside the tubes is studied using tempera.ure, velocity, a.d pressure distributions. The numerica. model wa. va.ida.ed by compa.ing the simula.ion results to the experimenta. da.a. a.d the difference between the results wa. found to be a.cepta.le a.d trustworthy. In compa.ison to the sta.da.d helica.ly tube hea. excha.ger (HTHE), the results showed tha. the fra.ta. tube hea. excha.ger (FTHE) is more fa.ora.le to hea. tra.smission. The entire hea. tra.sfer coefficient enha.cement ra.io is a.ound 289%. The exergy efficiency increa.es with the increa.e of the Re number a.d fra.ta. tube configura.ion ha. the highest exergy efficiency. The fra.ta. tree-like structure is more beneficia. in decrea.ing pumping powers tha. typica. HTHE, with a.reduction ra.io of ∆P of roughly 57%. a. the sa.e Re number ra.ge, the FTHE ha. a.grea.er COP tha. the HTHE, indica.ing tha. fra.ta. tree-like hea.excha.gers a.e prefera.le to sta.da.d HTHEs. The fra.ta.-like tree form is grea.er tha. the helica. sha.e for velocity, a.cording to velocity contours a.d strea.lines. © 2022, The a.thors. a.l rights reserved.

关键词： Hea. excha.gers

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In silico study a.d biologica. screening of benzoquina.olines a. potentia. a.timicrobia. a.ents a.a.nst methicillin-resista.t Sta.hylococcus a.reus, ca.ba.enem-resista.t Klebsiella.pneumonia., a.d flucona.ole-resista.t Ca.dida.a.bica.s

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MICROBIa. Pa.HOGENESIS 2021年第0期160卷 105157-105157页

作者： a.uelizz, Ha.em a. marzouk, Moha.ed Ba.hiet, a.med a.del-a.iz, Ma.wa.M. Ezzeldin, Essa. Ra.hid, Ha.unor a.-Sa.a.i, Ra.ha. King Saud Univ Coll Pharm Dept Pharmaceut Chem POB 2457 Riyadh 11451 Saudi Arabia Natl Res Ctr Chem Tanning Mat & Leather Technol Dept Organ Chem Ind Div 33 El Bohouth StEl Tahrir St Cairo 12622 Egypt Al Azhar Univ Reg Ctr Mycol & Biotechnol Med Microbiol Cairo Egypt Univ Sydney Childrens Hosp Fac Med & Hlth Natl Ctr Immunisat Res & Surveillance NCIRSKids Westmead NSW 2145 Australia

Globa.ly, a.tibiotic-resista.t pa.hogens ha.e become a.serious threa. to public hea.th. The use of drugs ha.ing structures different from those a.plied in the clinica. trea.ments of ba.teria. infections is a.well-known potentia. solution to the a.tibiotic resista.ce crisis. Benzo-[g]-quina.olines were identified by our resea.ch group a. a.new cla.s of a.timicrobia. a.ents. Herein, to follow-up the resea.ch on such compounds, three benzo-[g]-quina.olines (1-3) were studied, a. in vitro a.tiba.teria. ca.dida.es a.a.nst methicillin-resista.t Sta.hylococcus a.reus (MRSa., ca.ba.enem-resista.t Klebsiella.pneumonia., a.d flucona.ole-resista.t Ca.dida.a.bica.s, a. well. The minimum inhibitory concentra.ion (MIC) a.sa. for benzoquina.olines wa. ca.ried out via.the ca.orimetric broth microdilution method using the XTT a.sa. in compa.ison with va.comycin, ciprofloxa.in, a.d ketocona.ole a. reference drugs. The ta.get compounds 1-3 revea.ed high va.ia.ion in their a.tivity a.a.nst the exa.ined resista.t microbia. stra.ns. Benzoquina.oline 3 exhibited a.more potent effect a.a.nst the resista.t stra.ns compa.ed with the reference drugs. a.docking study wa. performed to identify the intera.tions between the benzoquina.olines 1-3 a.d liga.d proteins (OXa.48 ca.ba.enema.e, beta.la.ta.a.e, a.d sterol 14-a.pha.demethyla.e (CYP51)) a. the a.tive sites. Benzoquina.olines 1-3 showed very wea. cytotoxicity a.a.nst huma. lung fibrobla.t norma. cells (WI-38). The ta.gets showed promising a.timicrobia. effects a.a.nst the three resista.t stra.ns. These findings ma. inform future inhibitor discoveries ta.geting penicillin-binding proteins.

关键词： Klebsiella.pneumonia. Benzoquina.olines Sta.hylococcus a.reus Ca.dida.a.bica.s Docking study

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Thermo-hydra.lic study in a.shell a.d tube hea. excha.ger using rod inserts consisting of wire-na.ls with a.r injection: Experimenta. study

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INTERNa.IONa. JOURNa. OF THERMa. SCIENCES 2021年 161卷 106742-106742页

作者： marzouk, S. a. a.ou a.-Sood, M. M. El-Fa.ha.a.y, Ma.da.K. El-Sa.d, Ema. M. S. Kafr El Sheikh Univ Fac Engn Mech Engn Dept Kafr Al Sheikh Egypt Fayoum Univ Fac Engn Mech Engn Dept Al Fayyum Egypt

Recently, a.r bubbles injection with utilizing insets inside the tubes for enha.cing hea. tra.sfer performa.ce in shell a.d tube hea. excha.ger STHEs ha. a.hieved a.grea. interest. In this study, a.r wa. injected by the simple method in tube sides where wired na.ls-circula. rod inserts (WNCR) a.e presented with wa.er tube side flow ra.e TSFR cha.ged from 14 LPM to 18 LPM a.d wa.er shell side flow ra.e is kept consta.t a. a.typica. va.ue of 18 LPM. Two configura.ions of inserts with different dista.ce between the na.ls (10 cm a.d 5 cm) a.e employed with three different a.r volumetric flow ra.es a.FR of 1, 2, a.d 3 LPM. Effects of inserts only, inserts in conjunction with a.r injection, a.d a.r injection only on therma. pa.a.eters (i.e. number of tra.sfer units NTU, effectiveness epsilon, a.d overa.l hea. tra.sfer coefficient U) a.d hydra.lic performa.ce (indica.ed in pressure drop Delta.p) a.e studied a.d discussed. Moreover, exergy efficiency a.d therma. hydra.lic pa.a.eter a.e a.so presented a.d studied. Results indica.ed tha. inserts a.e more pronounced tha. a.r injection for a.l performa.ce pa.a.eters. Moreover, the second type (insert B) of inserts ha. more influence tha. the first one (insert a.. Percenta.e enha.cements in performa.ce pa.a.eters a.e within the ra.ges of 31%-131% for insert a. 43%-177% for insert B, 33%-143% for injection with insert a. 44%-184% for injection with insert B, 2%-19% for a.r injection only with insert a. a.d 1%-23% for insert B. Fina.ly, a.r injection only gives a.sma.l effect on hea. excha.ger performa.ce pa.a.eters (less tha. 5%) for performa.ce pa.a.eters such a. NTU, Delta.p, a.d therma. hydra.lic pa.a.eter.

关键词： Shell a.d tube hea. excha.ger Enha.cement Circula. rod Inserts a.r injection Performa.ce pa.a.eter

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a.tioxida.t a.tivities a.d molecula. docking of 2-thioxobenzo[g]quina.oline deriva.ives

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PHa.Ma.OLOGICa. REPORTS 2019年第4期71卷 695-700页

作者： a.-Sa.a.i, Ra.ha. Ta.e, Ha.a. a. a. Ba.heit, a.med H. marzouk, Moha.ed a.mehizia. a.dulra.ma. a. Herqa.h, Ra.hed a.uelizz, Ha.em a. King Saud Univ Coll Pharm Dept Pharmaceut Chem Riyadh Saudi Arabia Natl Res Ctr Div Agr & Biol Res Plant Biochem Dept Giza Egypt El Neelain Univ Fac Sci & Technol Dept Chem Khartoum Sudan Natl Res Ctr Ctr Excellence Adv Sci Chem Nat Prod Grp Cairo Egypt

Ba.kground: Oxida.ive stress a.d rela.ed disea.es resulting from the overproduction of free ra.ica.s ca. be countera.ted by designing a.d developing novel a.tioxida.ive a.ents tha. ca. protect the huma. body a.a.nst the da.a.e ca.sed by free ra.ica.s. Methods: The present study eva.ua.ed the a.tioxida.t a.tivities of 15 deriva.ives of 2-thioxobenzo[g]quina.oline using three different a.sa.s: 1,1-diphenyl-2-picryl hydra.yl (DPPH) ra.ica. sca.enging, reducing power ca.a.ility, a.d ferric reduction a.tioxida.t power. Results: Some benzoquina.olines ha. good a.tivity a.d ha. the ca.a.ity to deplete DPPH a.d free ra.ica.s compa.ed to a.positive control butyla.ed hydroxyl toluene (BHT). a.docking study identified the possible intera.tions between binding models a.d the a.tioxida.t a.tivities of the ta.get compounds. Conclusions: The a.tive compounds ca. be used a. templa.es for further development of more potent a.tioxida.ive a.ents. (C) 2019 The a.thors. Published by Elsevier B.V. on beha.f of Ma. Institute of Pha.ma.ology, Polish a.a.emy of Sciences.

关键词： Benzoquina.olines a.tioxida.t ca.a.ity DPPH Reducing power BHT Molecula. docking

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a.sessing ototoxicity a.d pa.ients' sa.isfa.tion of topica. loca. a.a.sthesia.in myringotomy a.d ventila.ion tube insertion

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JOURNa. OF La.YNGOLOGY a.D OTOLOGY 2019年第4期133卷 285-288页

作者： marzouk, S. a.-la.i, a. Sykes, R. Neuma.n, C. Nixon, I. J. East Kent Hosp Univ NHS Fdn Trust William Harvey Hosp Dept ENT Ashford TN24 0LZ Kent England

Objectivesa.ima. studies ha.e suggested tha. exposure of the middle ea. to topica. loca. a.a.sthesia.ma. be ototoxic. This study a.med to report sensorineura. hea.ing outcomes a.d pa.ients' sa.isfa.tion in those who underwent myringotomy a.d ventila.ion tube insertion using topica. loca. ***-nine pa.ients (32 ea.s) were opera.ed on. Pre- a.d post-opera.ive a.diology findings were compa.ed. a.Likert-type questionna.re on trea.ment sa.isfa.tion wa. completed a. the end of the *** pa.ient a.e wa. 55 yea.s (ra.ge, 27-88 yea.s). Pre- a.d post-opera.ive bone conduction pure tone a.era.es were 26.76 dB a.d 25.26 dB respectively (mea. reduction of -1.22 dB, 95 per cent confidence interva. of -5.91 to 8.13 dB;p = 0.7538). One ea. (3 per cent) ha. a.reduction in pure tone a.era.e of 10 *** results suggest tha. sensorineura. hea.ing loss is not a.complica.ion of ea. exposure to topica. loca. a.a.sthesia.during myringotomy a.d ventila.ion tube insertion. The procedure wa. well perceived.

关键词： Otitis Media.With Effusion a.esthesia Loca. Hea.ing Loss Pa.ient Sa.isfa.tion

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Synthesis a.d biologica. eva.ua.ion of 4-(1H-1,2,4-tria.ol-1-yl)benzoic a.id hybrids a. a.tica.cer a.ents

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RSC a.Va.CES 2019年第33期9卷 19065-19074页

作者： a.uelizz, Ha.em a. a.a., Ha.em M. marzouk, Moha.ed Na.r, Fa.d a. a.qa.ta.i, a.i S. Ba.heit, a.med H. Na.la., a.med M. a.-Sa.a.i, Ra.ha. King Saud Univ Coll Pharm Dept Pharmaceut Chem POB 2457 Riyadh 11451 Saudi Arabia Natl Res Ctr Dept Tanning Mat & Leather Technol 33 El Bohouth St Cairo 12622 Egypt Natl Res Ctr Ctr Excellence Adv Sci Chem Nat Prod Grp 33 El Bohouth St Cairo 12622 Egypt King Saud Univ Coll Pharm Med Aromat & Poisonous Plants Res Ctr POB 2457 Riyadh 11451 Saudi Arabia King Saud Univ Pharmacognosy Dept Coll Pharm POB 2457 Riyadh 11451 Saudi Arabia El Neelain Univ Fac Sci & Technol Dept Chem POB 12702 Khartoum 11121 Sudan King Saud Univ Coll Pharm Dept Pharmaceut Chem DEDC Riyadh 11451 Saudi Arabia Natl Res Ctr Chem Ind Res Div Peptide Chem Dept 33 El Bohouth St Cairo 12622 Egypt

a.series of 4-(1H-1,2,4-tria.ol-1-yl)benzoic a.id hybrids (1-17) wa. successfully synthesized a.d their structures were esta.lished by NMR a.d MS a.a.ysis. In vitro cytotoxic eva.ua.ion indica.ed tha. some of the hybrids exhibited potent inhibitory a.tivities a.a.nst MCF-7 a.d HCT-116 ca.cer cell lines, with IC50 va.ues ra.ging from 15.6 to 23.9 mu M, compa.ed with reference drug doxorubicin (19.7 a.d 22.6 mu M, respectively). Nota.ly, the most potent compounds, 2, 5, 14, a.d 15, not only exhibited a. obvious improvement in IC50 va.ues, but demonstra.ed very wea. cytotoxic effects towa.d norma. cells (RPE-1) compa.ed with doxorubicin. a.further investiga.ion showed tha. compounds 2 a.d 14 clea.ly inhibited the prolifera.ion of MCF-7 ca.cer cells by inducing a.optosis. In a.dition, these hybrids showed a.cepta.le correla.ion with bioa.sa. results in regression plots genera.ed by 2D QSa. models. Our results indica.ed tha. 1,2,4-tria.ole benzoic a.id hybrids could be used a. a.structura. optimiza.ion pla.form for the design a.d development of more selective a.d potent a.tica.cer molecules.

关键词： Benzoic a.id

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In vitro eva.ua.ion of new 2-phenoxy-benzo [g]tria.olo[1,5-a./i>] quina.oline deriva.ives a. a.timicrobia. a.ents: 收藏
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引用; MICROBIa. Pa.HOGENESIS 2018年第0期117卷 60-67页; 作者： a.uelizz, Ha.em a. El-Dib, Ra.a. a. marzouk, Moha.ed a.-Sa.a.i, Ra.ha. King Saud Univ Coll Pharm Dept Pharmaceut Chem POB 2457 Riyadh 11451 Saudi Arabia King Saud Univ Coll Pharm Dept Pharmocognosy POB 2452 Riyadh 11495 Saudi Arabia Helwan Univ Fac Pharm Dept Pharmacognosy Cairo 11795 Egypt Prince Sattam bin Abdulaziz Univ Coll Sci & Humanities Dept Chem Alkharj 83 Saudi Arabia Natl Res Ctr Ctr Excellence Adv Sci Chem Nat Prod Grp Cairo 12622 Egypt; Previously, seventeen 2-phenoxy-benzo[g][1,2,4]tria.olo[1,5-a.quina.oline deriva.ives were prepa.ed a.d cha.a.terized by physicochemica. a.d spectra. mea.s. This study wa. conducted to eva.ua.e their a.tivities in vit... 详细信息; Previously, seventeen 2-phenoxy-benzo[g][1,2,4]tria.olo[1,5-a.quina.oline deriva.ives were prepa.ed a.d cha.a.terized by physicochemica. a.d spectra. mea.s. This study wa. conducted to eva.ua.e their a.tivities in vitro a.a.nst five Gra.-nega.ive a.d five Gra.-positive of clinica.ly pa.hogenic ba.teria. stra.ns a.d ten funga. stra.ns. The a.timicrobia. a.tivity wa. a.sessed, a.d the minimum inhibitory concentra.ion va.ues of the tested compounds were determined in mu g ml(-1), using the diffusion a.a. technique. The ba.teria. stra.ns used were Escherichia.coil (a.CC 25922), Proteus mira.ilis (a.CC 7002), Klebsiella.oxytoca.(a.CC 700324), Pseudomona. a.ruginosa.(a.CC 10145), Enteroba.ter cloa.a. (a.CC 13047D-5), Ba.illus subtilis (NRRL B-543), Enterococcus fa.ca.is (RCMB 0100154-2), Sta.hylococcus a.reus (a.CC 29213), Sta.hylococcus epidermidis (a.CC 12228), a.d Streptococcus pyogenes (RCMB 0100174-2). a.pergillus fumiga.us (RCMB 02568), Syncepha.a.trum ra.emosum (IMI 21178), Geotricum ca.didum (IMI 329542), Ca.dida.a.bica.s (a.CC 10231), a.pergillus niger (IMI 130783), Cryptococcus neoforma.s (NRRL Y-1518), Ca.dida.tropica.is (RCMB 05239), Penicillium expa.sum (IMI 146655), Microsporum ca.is (RCMB 0834), a.d Trichophyton menta.rophytes (RCMB 0925) were used a. the funga. stra.ns. a.picillin a.d genta.icin were used a. reference a.tiba.teria. drugs a.d a.photericin B wa. used a. the reference a.tifunga. drug. The a.timicrobia. studies revea.ed tha. the tested compounds 6-8, 11, 12, a.d 14-16 showed the highest a.tivities a.a.nst the ba.teria. a.d funga. stra.ns. The current study showed tha. some benzo [g]tra.zoloquina.olines displa.ed rema.ka.le a.timicrobia. a.tivity a.d could be used a. templa.e for further design of potent a.timicrobia. a.ent.; 关键词： a.tiba.teria. a.tivity a.tifunga. a.tivity Minimum inhibitory concentra.ion Benzotria.oloquina.oline; 来源：评论; 学校读者我要写书评

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Exploiting the 4-hydra.inobenzoic a.id moiety for the development of a.tica.cer a.ents: Synthesis a.d biologica. profile

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BIOORGa.IC CHEMISTRY 2020年 102卷 104098-104098页

作者： a.uelizz, Ha.em a. a.a., Ha.em M. marzouk, Moha.ed Na.r, Fa.d a. Ba.heit, a.med H. Na.la., a.med M. a.-sha.lia., Na.ser S. a.-Sa.a.i, Ra.ha. King Saud Univ Dept Pharmaceut Chem Coll Pharm POB 2457 Riyadh 11451 Saudi Arabia Natl Res Ctr Dept Tanning Mat & Leather Technol 33 El Bohouth St Cairo 12622 Egypt King Saud Univ Coll Pharm Med Aromat & Poisonous Plants Res Ctr POB 2457 Riyadh 11451 Saudi Arabia El Neelain Univ Fac Sci & Technol Dept Chem POB 12702 Khartoum 11121 Sudan King Saud Univ Dept Pharmaceut Chem Coll Pharm Drug Explorat & Dev Chair DEDC Riyadh 11451 Saudi Arabia Natl Res Ctr Chem Ind Res Div Peptide Chem Dept 33 El Bohouth St Cairo 12622 Egypt

Thirteen 4-hydra.inobenzoic a.id deriva.ives were ela.ora.ed a.d cha.a.terized by spectra. a.a.yses (NMR a.d MS). Eva.ua.ion of their in vitro cytotoxic a.tivity showed tha. some of the ta.gets demonstra.ed potent inh... 详细信息

Thirteen 4-hydra.inobenzoic a.id deriva.ives were ela.ora.ed a.d cha.a.terized by spectra. a.a.yses (NMR a.d MS). Eva.ua.ion of their in vitro cytotoxic a.tivity showed tha. some of the ta.gets demonstra.ed potent inhibitory effects a.a.nst HCT-116 a.d MCF-7 ca.cer cells. The IC50 va.ues ra.ged between 21.3 +/- 4.1 a.d 28.3 +/- 5.1 mu M, respectively, wherea. those of doxorubicin (reference drug) ra.ged between 22.6 +/- 3.9 a.d 19.7 +/- 3.1 mu M, respectively. The a.tive ta.gets 6, 7 a.d 9 exhibited very wea. cytotoxicity on norma. cells (RPE-1) a.d showed higher IC50 va.ues a.a.nst HCT-116 a.d MCF-7 cells in compa.ison to doxorubicin. Furthermore, compounds 7, 9 a.d 10 inhibited the prolifera.ion of MCF-7 by the induction of a.optosis. The bioa.sa. results in the regression plots genera.ed in 3D QSa. models were in a.reement a.d correla.ed with the a.tica.cer results of the ta.get molecules. The 4-hyda.inobenzoic a.id deriva.ives ca. be used a. cornerstones for further structura. modifica.ions a. future a.tica.cer a.ents.

关键词： 4-Hydra.inobenzoic a.id MTT a.sa. a.tica.cer a.optosis 3D QSa.

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Screening a.d eva.ua.ion of a.tioxida.t a.tivity of some 1,2,4-tria.olo[1,5-a./i>] quina.oline deriva.ives

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FUTURE MEDICINa. CHEMISTRY 2018年第4期10卷 379-390页

作者： a.-Sa.a.i, Ra.ha. a.oua., El-Ha.sa.e marzouk, Moha.ed Ta.e, Ha.a. a. a. a.uelizz, Ha.em a. King Saud Univ Dept Pharmaceut Chem Coll Pharm POB 2457 Riyadh 11451 Saudi Arabia Prince Sattam bin Abdulaziz Univ Dept Chem Coll Sci & Humanities Alkharj 83 Saudi Arabia Natl Res Ctr Chem Nat Prod Grp Ctr Excellence Adv Sci Cairo 12622 Egypt Natl Res Ctr Dept Plant Biochem Div Agr & Biol Res 33 El Bohouth St Giza 12622 Egypt

a.m: The present study wa. ca.ried out to a.sess a.new series of tria.oloquina.olines 1-40 for their a.tioxida.t a.tivities using 1,1-diphenyl-2-picryl hydra.yl ra.ica. sca.enging, ferric reduction a.tioxida.t power a...

a.m: The present study wa. ca.ried out to a.sess a.new series of tria.oloquina.olines 1-40 for their a.tioxida.t a.tivities using 1,1-diphenyl-2-picryl hydra.yl ra.ica. sca.enging, ferric reduction a.tioxida.t power a.d reducing power ca.a.ility a.sa.s. Results: a.l tria.oloquina.olines 1-40 exhibited a.tioxida.t a.tivity ra.ged from wea. to modera.e a.d high. The obta.ned findings revea.ed tha. the tria.oloquina.olines 30, 36 a.d 38-40 ha.e superiority a.ong a.l compounds, demonstra.ing the highest ca.a.ity to deplete 1,1-diphenyl-2-picryl hydra.yl a.d free ra.ica.s, in rela.ion to butyla.ed hydroxyl toluene, a. a.synthetic a.tioxida.t a.ent. Conclusion: Chemica. modifica.ions together with density functiona. theory study on the ta.gets supplied us with some va.ua.le cla.ifica.ions a.out the required properties needed for the ta.get compounds to be more a.tive a.a.nst free ra.ica.s.

关键词： a.tioxida.t a.tivity BHT DFT DPPH FRa. in vitro eva.ua.ion tria.oloquina.olines

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