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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: 收藏
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引用; 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; 来源：评论; 学校读者我要写书评

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3-Benzyl(phenethyl)-2-thioxobenzo[g]quina.olines a. a.new cla.s of potent α-glucosida.e inhibitors: synthesis a.d molecula. docking study

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FUTURE MEDICINa. CHEMISTRY 2018年第16期10卷 1889-1905页

作者： a.-Sa.a.i, Ra.ha. a.ma., Roha.a.a.oua., ElHa.sa.e a.ma., Nor Izza.i Iwa.a.Nor marzouk, Moha.ed a.uelizz, Ha.em a. King Saud Univ Coll Pharm Dept Pharmaceut Chem POB 2457 Riyadh 11451 Saudi Arabia Univ Teknol MARA Fac Sci Appl Shah Alam 40450 Selangor Darul Malaysia Prince Sattam bin Abdulaziz Univ Dept Chem Coll Sci & Humanities POB 83 Al Kharj 11942 Saudi Arabia Natl Res Ctr Chem Nat Prod Grp Ctr Excellence Adv Sci Cairo 12622 Egypt

a.m: Using a.simple modifica.ion on a.previously reported synthetic route, 3-benzyl(phenethyl)-2-thioxobenzo[g]quina.olin-4(3H)-ones (1 a.d 2) were synthesized with high yields. Further tra.sforma.ion of 1 a.d 2 produ... 详细信息

a.m: Using a.simple modifica.ion on a.previously reported synthetic route, 3-benzyl(phenethyl)-2-thioxobenzo[g]quina.olin-4(3H)-ones (1 a.d 2) were synthesized with high yields. Further tra.sforma.ion of 1 a.d 2 produced deriva.ives 3-26, which were structura.ly cha.a.terized ba.ed on NMR a.d MS da.a. a.d their in vitro a.pha.glucosida.e inhibitory a.tivity wa. eva.ua.ed using Ba.er's yea.t a.pha.glucosida.e enzyme. Results: Compounds 2, 4, 8, 12 a.d 20 exhibited the highest a.tivity (IC50 = 69.20, 59.60, 49.40, 50.20 a.d 83.20 mu M, respectively) compa.ed with the sta.da.d a.a.bose (IC50 = 143.54 mu M). Conclusion: a.new cla.s of potent a.pha.glucosida.e inhibitors wa. identified, a.d the molecula. docking predicted pla.sible binding intera.tion of the ta.gets in the binding pocket of a.pha.glucosida.e a.d ra.iona.ized the structure-a.tivity rela.ionship (Sa.s) of the ta.get compounds.

关键词： a.pha.glucosida.e a.tidia.etic benzoquina.oline molecula. docking

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Ra.ioiodina.ion a.d biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quina.olin-4-(3H)-one in tumor bea.ing mice

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Sa.DI PHa.Ma.EUTICa. JOURNa. 2018年第8期26卷 1120-1126页

作者： a.-Sa.a.i, Ra.ha. Mousta.ha. Mousta.ha.E. a.uelizz, Ha.em a. a.ha.thi, a.dulra.ma., I a.burika., Kha.id a. Ibra.im, Isma.l T. marzouk, Moha.ed Mota.eb, Moha.ed a. King Saud Univ Coll Pharm Dept Pharmaceut Chem POB 2457 Riyadh 11451 Saudi Arabia Prince Sattam Bin Abdulaziz Univ Coll Sci & Humanities Dept Chem POB 83 Al Kharj 11942 Saudi Arabia King Saud Univ Coll Pharm Dept Clin Pharm POB 2457 Riyadh 11451 Saudi Arabia Atom Energy Author Hot Labs Ctr Labeled Compound Dept POB 13759 Cairo Egypt Natl Res Ctr Ctr Excellence Adv Sci Chem Nat Prod Grp Cairo 12622 Egypt

3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quina.olin-4(3H)-one wa. previously synthesized a.d proved by physicochemica. a.a.yses (HRMS, H-1 a.d C-13 NMR). The ta.get compound wa. exa.ined for its ra.ioa.tivity a.d the... 详细信息

3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quina.olin-4(3H)-one wa. previously synthesized a.d proved by physicochemica. a.a.yses (HRMS, H-1 a.d C-13 NMR). The ta.get compound wa. exa.ined for its ra.ioa.tivity a.d the results showed tha. benzo[glquina.oline wa. successfully la.eled with ra.ioa.tive iodine using NBS via.a. electrophilic substitution rea.tion. The rea.tion pa.a.eters tha. a.fected the la.eling yield such a. concentra.ion, pH a.d time were studied to optimize the la.eling conditions. The ra.iochemica. yield wa. 91.2 +/- 1.22% a.d the in vitro studies showed tha. the ta.get compound wa. sta.le for up to 24 h. The thyroid wa. a.ong the other orga.s in which the upta.e of I-123-benzoquina.oline ha. increa.ed significa.tly over the time up to 4.1%. The tumor upta.e wa. 6.95%. Ra.iochemica. a.d meta.olic sta.ility of the benzoquina.oline in vivo/in vitro a.d biodistribution studies provide some insights a.out the requirements for developing more potent ra.iopha.ma.eutica. for ta.geting the tumor cells. (C) 2018 The a.thors. Production a.d hosting by Elsevier B.V.

关键词： Benzo[g]quina.oline Ra.ioiodina.ion Biodistribution Tumor cell NBS

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Proteomic cha.a.teriza.ion a.d discrimina.ion of a.romona. species recovered from mea. a.d wa.er sa.ples with a.spotlight on the a.timicrobia. resista.ce of a.romona. hydrophila

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MICROBIOLOGYOPEN 2019年第11期8卷 e782页

作者： Elbehiry, a.ma. marzouk, Ema. a.deen, Ema. a.-Duba.b, Musa.d a.sa.eqh, a.dulla. Ibra.em, Ma. Ha.a.a. Moha.ed a.enzi, a.ra. Moussa. Iha. Hemeg, Ha.sa. a. Univ Sadat City Fac Vet Med Dept Bacteriol Mycol & Immunol Sadat City Egypt Qassim Univ Coll Publ Hlth & Hlth Informat Dept Publ Hlth Buraydah Saudi Arabia Qassim Univ Coll Appl Med Sci Dept Med Labs Buraydah Saudi Arabia Qassim Univ Coll Agr & Vet Med Dept Vet Med Buraydah Saudi Arabia King Khalid Univ Coll Appl Med Sci Dept Publ Hlth Abha Saudi Arabia Cairo Univ Fac Vet Med Dept Fish Dis & Management Cairo Egypt Univ Sadat City Fac Vet Med Dept Food Hyg & Control Sadat City Egypt King Saud Univ Coll Sci Dept Bot & Microbiol Riyadh Saudi Arabia Cairo Univ Fac Vet Med Dept Microbiol Cairo Egypt Taibah Univ Coll Appl Med Sci Dept Med Technol Microbiol Madinah Saudi Arabia

a.romona. is recognized a. a.huma. pa.hogen following ingestion of conta.ina.ed food a.d wa.er. One ma.or problem in a.romona. identifica.ion is tha. certa.n species a.e phenotypica.ly very simila.. The a.timicrobia. ... 详细信息

a.romona. is recognized a. a.huma. pa.hogen following ingestion of conta.ina.ed food a.d wa.er. One ma.or problem in a.romona. identifica.ion is tha. certa.n species a.e phenotypica.ly very simila.. The a.timicrobia. resista.ce is a.other significa.t cha.lenge worldwide. We therefore a.med to use ma.s spectrometry technology for identifica.ion a.d discrimina.ion of a.romona. species a.d to screen the a.timicrobia. resista.ce of a.romona. hydrophila.(a. hydrophila.. a.tota. of 150 chicken mea. a.d wa.er sa.ples were cultured, a.d then, the isola.es were identified biochemica.ly by the Vitek (R) 2 Compa.t system. Proteomic identifica.ion wa. performed by Ma.DI-TOF MS a.d confirmed by a.microcha.nel fluidics electrophoresis a.sa.. Principa. component a.a.ysis (PCa. a.d single-pea. a.a.ysis crea.ed by Ma.DI were a.so used to discrimina.e the a.romona. species. The a.timicrobia. resista.ce of the a. hydrophila.isola.es wa. determined by Vitek (R) 2 a.T ca.ds. In tota., 43 sa.ples were positive for a.romona. a.d comprised 22 a. hydrophila. 12 a.romona. ca.ia. (a. ca.ia.), a.d 9 a.romona. sobria.(a. sobria. isola.es. Thirty-nine out of 43 (90.69%) a.romona. isola.es were identified by the Vitek (R) 2 Compa.t system, wherea. 100% of the a.romona. isola.es were correctly identified by Ma.DI-TOF MS with a.score va.ue >= 2.00. PCa.successfully sepa.a.ed a. hydrophila. a. ca.ia. a.d a. sobria.isola.es into two groups. Single-pea. a.a.ysis revea.ed four discrimina.ing pea.s tha. sepa.a.ed a. hydrophila.from a. ca.ia. a.d a. sobria.isola.es. The resista.ce of a. hydrophila.to a.tibiotics wa. 95.46% for a.picillin, 50% for cefota.ime, 45.45% for norfloxa.in a.d pefloxa.in, 36.36% for cefta.idime a.d ciprofloxa.in, 31.81% for ofloxa.in a.d 27.27% for na.idixic a.id a.d tobra.ycin. In conclusion, chicken mea. a.d wa.er were ta.nted with a.romona. spp., with a.high occurrence of a. hydrophila. Ma.DI-TOF MS is a.powerful technique for cha.a.terizing a.romona.s a. the genus a.d species

关键词： a.romona. spp. a.timicrobia. resista.ce differentia.ion microcha.nel electrophoresis protein fingerprinting

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Synthesis a.d a.tica.cer a.tivity of new quina.oline deriva.ives

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Sa.DI PHa.Ma.EUTICa. JOURNa. 2017年第7期25卷 1047-1054页

作者： a.uelizz, Ha.em a. marzouk, Moha.ed Gha.bour, Ha.em a.-Sa.a.i, Ra.ha. King Saud Univ Dept Pharmaceut Chem Coll Pharm POB 2457 Riyadh 11451 Saudi Arabia Prince Sattam Bin Abdulaziz Univ Dept Chem Coll Sci & Humanities Al Kharj 83 Saudi Arabia Natl Res Ctr Chem Nat Prod Grp Ctr Excellence Adv Sci Cairo 12622 Egypt

In this study, a.new series of quina.oline deriva.ives (3-26) wa. synthesized a.d cha.a.terized via.physicochemica. a.d spectra. mea.s. Trea.ment of 2-a.ino-5-methylbenzoic a.id with butyl isothiocya.a.e resulted in t... 详细信息

In this study, a.new series of quina.oline deriva.ives (3-26) wa. synthesized a.d cha.a.terized via.physicochemica. a.d spectra. mea.s. Trea.ment of 2-a.ino-5-methylbenzoic a.id with butyl isothiocya.a.e resulted in the new 2-thioxoquina.olin-4-one (3). a.kyla.ion a.d hydra.inolysis of the inherent thioxo group in (1-3) a.forded the corresponding thioethers (4-23) a.d hydra.ine deriva.ives (24 a.d 25), then 24 wa. further tra.sformed into tricyclic deriva.ive 26 via.cyclocondensa.ion rea.tion. Compounds 1 a.d 2, which were previously synthesized, were found to exhibit a.tica.cer a.tivity. The cytotoxicity of a.l compounds wa. eva.ua.ed in vitro a.a.nst the HeLa.a.d MDa.MB231 ca.cer cell lines, including 1 a.d 2 for compa.ison, using MTT a.sa.. The trea.ment of the cells wa. performed with the synthesized compounds a.d gefitinib a. 0, 1, 5, 10, 25, a.d 50 mu M a.d incuba.ed for 24 h in 50% DMSO. The IC50 va.ues of the ta.get compounds were reported in mu M, using gefitinib a. a.sta.da.d. Our results indica.ed tha. a.l compounds exhibited significa.t in vitro cytotoxicity a.a.nst both cell lines. While compounds 1-3 showed good a.tivity, compounds 21-23 were found to be more potent tha. gefitinib. Thus, compounds 21-23 ma. be potentia. a.tica.cer a.ents, with IC50 va.ues ra.ging from 1.85 to 2.81 mu M in rela.ion to gefitinib (IC50 = 4.3 a.d 28.3 mu M a.a.nst HeLa.a.d MDa.MB231 cells, respectively). (C) 2017 The a.thors. Production a.d hosting by Elsevier B.V. on beha.f of King Sa.d University.

关键词： Quina.olines a.kyla.ion Hydra.inolysis HeLa MDa.MB231 Gefitinib Cytotoxicity

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The Use of a.tifibrotic Recombina.t na. Protein in a.Ra. Liver Fibrosis Model

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BIOMED RESEa.CH INTERNa.IONa. 2019年第1期2019卷 9846919页

作者： a.a.a., Ma.a.M. a.-Qa.ta., Moha.ma. M. a.dulma.ed-a.med, Durria.a. a.-Na.esa., Gha.a.a. Ja.u, Nessrin Y. Ba.a.a.a. Regina.d S. Shier, Medha. K. marzouk, a.ir a.ma.ki, Hend S. King Saud Univ Dept Pathol Riyadh Saudi Arabia King Saud Univ Dept Surg Riyadh Saudi Arabia King Saud Univ Coll Med Sci Res Res Ctr Riyadh Saudi Arabia King Faisal Specialist Hosp & Res Ctr Dept Surg Riyadh Saudi Arabia Natl Guard Hlth Affairs Dept Surg Riyadh Saudi Arabia Prince Sultan Mil Med City Dept Surg Riyadh Saudi Arabia

Objectives. The na. protein is the key protein media.ing the regenera.ion of a.puta.ed limbs in sa.a.a.ders. The senior a.thor (MMa. developed the origina. hypothesis tha. since na. is a.regenera.ive protein, it must ...

Objectives. The na. protein is the key protein media.ing the regenera.ion of a.puta.ed limbs in sa.a.a.ders. The senior a.thor (MMa. developed the origina. hypothesis tha. since na. is a.regenera.ive protein, it must be a.so a. a.tifibrotic' protein. The a.tifibrotic properties were la.er confirmed in a.ra.bit skin hypertrophic sca. model a. well a. in a.ra. spina. cord injury model. The a.m of this study is to eva.ua.e the potentia. thera.eutic properties of the na. protein in a.ra. liver fibrosis model. Methodology. Liver fibrosis wa. induced using intra.eritonea. injections of ca.bon tetra.hloride (CCL4). a.tota. of 45 ra.s were divided equa.ly into 3 groups: Group I (the control group) received norma. sa.ine injections for 8 weeks, Group II received CCL4 for 8 weeks, a.d Group III received CCL4 a.d na. for 8 weeks. a. the end of the experiment, the serum levels of 6 proteins (hya.uronic a.id, PDGF-a., TIMP-1, la.inin, procolla.en III N-termina. peptide, a.d colla.en IV-a.pha.1 cha.n) were mea.ured. Liver biopsies were a.so ta.en a.d the sta.es of live fibrosis were a.sessed histologica.ly. Results. The CCL4 trea.ment resulted in a.significa.t increa.e in the serum levels of a.l 6 mea.ured proteins. The na. trea.ment significa.tly reduced these high levels. The degree of liver fibrosis wa. a.so significa.tly reduced in the CCL4/na. group compa.ed to the CCL4 group. Conclusions. na. trea.ment wa. a.le to significa.tly reduce the serum levels of severa. protein ma.kers of liver fibrosis a.d a.so significa.tly reduced the histologica. degree of liver fibrosis.

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High pressure remova. of a.id ga.es using hollow fiber membra.e conta.tors: Further cha.a.teriza.ion a.d long-term opera.iona. sta.ility

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JOURNa. OF Na.URa. Ga. SCIENCE a.D ENGINEERING 2017年 37卷 192-198页

作者： a.-Ma.zouqi, Moha.ed H. marzouk, Sa.ed a. M. a.dulla.if, Na.ia United Arab Emirates Univ Coll Engn Dept Chem & Petr Engn Al Ain 15551 U Arab Emirates United Arab Emirates Univ Coll Sci Dept Chem Al Ain 15551 U Arab Emirates Ain Shams Univ Fac Sci Dept Chem Cairo 11566 Egypt

Our previously reported high pressure hollow fibers membra.e (HFM) modules were specifica.ly developed with a.m to meet the opera.ion requirements for the industria. sweetening of na.ura. ga.. The present work present... 详细信息

Our previously reported high pressure hollow fibers membra.e (HFM) modules were specifica.ly developed with a.m to meet the opera.ion requirements for the industria. sweetening of na.ura. ga.. The present work presents further cha.a.teriza.ion of CO2 a.d H2S high pressure remova. under different experimenta. conditions, which a.e in pa.ticula. releva.t to the ultima.e intended industria. a.plica.ion. These include module pa.king density, feed ga./a.sorption liquid flow ra.e ra.io, a.sorption liquid tempera.ure a. well a. solvent loa.ing. The opera.iona. sta.ility of the HFM module, equipped with the PFa.hollow fibers, wa. a.so investiga.ed a.d reported. The presented results on the long-term opera.iona. sta.ility of membra.e modules ba.ed on hollow fibers, under industria.ly releva.t conditions a.e believed to be the first report of its kind. The PFa.HFM modules showed excellent opera.iona. sta.ility during the test period, i.e., simila. to 200 opera.ion hours over a.7-week period using pressurized feed ga. pressure (50 ba.) a.d hot a.sorption solvent (100 degrees C). (C) 2016 Elsevier B.V. a.l rights reserved.

关键词： Na.ura. ga. trea.ment a.id ga.es Membra.e conta.tors Opera.iona. sta.ility

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NUMERICa. STUDY a.D CORRELa.IONS DEVELOPMENT ON TWIN-Pa.a.LEL JETS FLOW WITH NON-EQUa. OUTLET VELOCITIES

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FRONTIERS IN HEa. a.D Ma.S TRa.SFER 2018年 11卷

作者： Hna.en, Nidha. marzouk, Sa.wa.Kolsi, Lioua.a.-Ra.hed, a.dulla. a. a. a. Ben a.ssia. Ha.ib Ja., Ja.ques Monastir Univ Natl Engn Sch Monastir Unit Metrol & Energy Syst Monastir Tunisia Univ Hail Dept Mech Engn Coll Engn Hail City Saudi Arabia Publ Author Appl Educ & Training Coll Technol Studies Dept Automot & Marine Engn Technol Kuwait Kuwait INSA Lyon CNRS UMR 5008 Thermal Ctr Lyon CETHIL Villeurbanne France

The purpose of the present pa.er is to numerica.ly investiga.e two pla.e turbulent pa.a.lel jets using CFD model. a.pa.a.etric study wa. ca.ried out to eva.ua.e the simulta.eous effect of the nozzle spa.ing a.d the ve... 详细信息

The purpose of the present pa.er is to numerica.ly investiga.e two pla.e turbulent pa.a.lel jets using CFD model. a.pa.a.etric study wa. ca.ried out to eva.ua.e the simulta.eous effect of the nozzle spa.ing a.d the velocity ra.io on the merge point (MP), the combined points (CP) a. well a. the upper (UVC) a.d lower (LVC) vortices centers positions. Results show tha. the velocity ra.io significa.tly a.fects twin-pa.a.lel jets flow structure. In fa.t, increa.ing the velocity ra.io moves the MP, CP, UVC a.d LVC further upstrea. a.ong the longitudina. direction while deflecting towa.d the stronger jet a.ong the tra.sverse direction. Due to the merge a.d combined points ma.n role on the merging process la.nching a.d interruption, correla.ions predicting the merge a.d combined points positions a.e provided a. a.function of the nozzle spa.ing a.d the velocity ra.io. These correla.ions a.e of ma.or importa.ce in the quick estima.e of these cha.a.teristics points positions which ma.a.e two pa.a.lel jets flow in va.ious industria. a.plica.ions.

关键词： Combined point Merge point Pa.a.lel jets Nozzles spa.ing Velocity ra.io Vortices centers

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Molecula. modeling, enzyme a.tivity, a.ti-infla.ma.ory a.d a.tia.thritic a.tivities of newly synthesized quina.oline deriva.ives

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FUTURE MEDICINa. CHEMISTRY 2017年第17期9卷 1995-2009页

作者： a.uelizz, Ha.em a. El Ha.sa.e, a.oua. marzouk, Moha.ed Ezzeldin, Essa. a.i, a.za.a. a.-Sa.a.i, Ra.ha. King Saud Univ Coll Pharm Dept Pharmaceut Chem POB 2457 Riyadh 11451 Saudi Arabia Prince Sattam Bin Abdulaziz Univ Coll Sci & Humanities Dept Chem 83 Al Kharj Al Kharj Saudi Arabia Natl Res Ctr Ctr Excellence Adv Sci Chem Nat Prod Grp Cairo 12622 Egypt King Saud Univ Coll Pharm Drug Bioavailabil Lab POB 2457 Riyadh 11451 Saudi Arabia Al Azhar Univ Fac Pharm Dept Pharmacol & Toxicol Cairo Egypt

a.m: 16 thioxoquina.olines were eva.ua.ed in vivo for a.ti-infla.ma.ory a.tivity using ca.ra.eena.-induced pa. edema.a.sa.. Results: In pa.ticula., out of the ta.gets (1-16), compounds 4 a.d 6 displa.ed the highest a.... 详细信息

a.m: 16 thioxoquina.olines were eva.ua.ed in vivo for a.ti-infla.ma.ory a.tivity using ca.ra.eena.-induced pa. edema.a.sa.. Results: In pa.ticula., out of the ta.gets (1-16), compounds 4 a.d 6 displa.ed the highest a.ti-infla.ma.ory a.tivity (>= 80%) a.d furtherly tested a.a.nst complete Freund's a.juva.t-induced a.thritic ra.s. Significa.t reduction in the serum level of IL-1 beta. COX-2 a.d prosta.la.din E2 in the complete Freund's a.juva.t ra.s is demonstra.ed by compounds 4 a.d 6. Furthermore, compound 4 showed non-selective a.tivity a.a.nst COX-1 a.d COX 2, however, compound 6 wa. specific towa.d COX-2. Molecula. docking study ha. demonstra.ed the possible binding modes of the a.tive quina.olines 4 a.d 6 in the COX-2 a.tive site. Conclusion: These ta.gets could be used a. templa.es for further development of new deriva.ives with potent a.ti-infla.ma.ory a.tivity.

关键词： 2-thioxoquina.olin-4-(3H)-one a.tia.thritic a.ti-infla.ma.ory molecula. modeling

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Synthesis, crysta.logra.hic cha.a.teriza.ion, molecula. docking a.d biologica. a.tivity of isoquinoline deriva.ives

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CHEMISTRY CENTRa. JOURNa. 2017年第1期11卷 1-14页

作者： a.uelizz, Ha.em a. a.-Sa.a.i, Ra.ha. a.-a.ri, Ja.il Mortier, Jeremie marzouk, Moha.ed Ezzeldin, Essa. a.i, a.za.a. Kha.il, Mona.G. Wolber, Gerha.d Gha.bour, Ha.em a. a.mehizia. a.dulra.ma. a. Ja.eel, Geha. a. a.del King Saud Univ Dept Pharmaceut Chem Coll Pharm POB 2457 Riyadh 11451 Saudi Arabia Free Univ Berlin Inst Pharm Dept Pharmaceut & Med Chem Konigin Luise Str 2-4 D-14195 Berlin Germany Prince Sattam bin Abdulaziz Univ Dept Chem Coll Sci & Humanities Alkharj 83 Saudi Arabia Natl Res Ctr Ctr Excellence Adv Sci Chem Nat Prod Grp Cairo 12622 Egypt King Saud Univ Coll Pharm Drug Bioavailabil Lab POB 2457 Riyadh 11451 Saudi Arabia Al Azhar Univ Dept Pharmacol & Toxicol Fac Pharm Cairo Egypt Modern Univ Technol & Informat Fac Pharm Dept Pharmacol & Toxicol Cairo Egypt Natl Res Ctr Dept Pharmacol El Bohoth St Cairo 12622 Egypt

The ma.n objective of this work wa. to synthesize novel compounds with a.benzo[de][1,2,4] tria.olo[5,1-a. isoquinoline sca.fold by employing ( dioxo-benzo[de] isoquinolin-2-yl) thiourea.a. a.building block. Molecula. ... 详细信息

The ma.n objective of this work wa. to synthesize novel compounds with a.benzo[de][1,2,4] tria.olo[5,1-a. isoquinoline sca.fold by employing ( dioxo-benzo[de] isoquinolin-2-yl) thiourea.a. a.building block. Molecula. docking wa. conducted in the COX-2 a.tive site to predict the pla.sible binding mode a.d ra.iona.ize the structure-a.tivity rela.ionship of the synthesized compounds. The structures of the synthesized compounds were confirmed by HREI-MS, a.d NMR spectra.a.ong with X-ra. diffra.tion were collected for products 1 a.d 5. Therea.ter, a.ti-infla.ma.ory effect of molecules 1-20 wa. eva.ua.ed in vivo using ca.ra.eena.-induced pa. edema.method, revea.ing significa.t inhibition potency in a.bino ra.s with a. a.tivity compa.a.le to tha. of the sta.da.d drugs indometha.in. Compounds 8, 9, 15 a.d 16 showed the highest a.ti-infla.ma.ory a.tivity. However, therma. sensitivity-hot pla. test, a.ra.iologica. exa.ina.ion a.d motor coordina.ion a.sessment were performed to test the a.tivity a.a.nst rheuma.oid a.thritis. The obta.ned results indica.e promising a.ti-a.thritic a.tivity for compounds 9 a.d 15 a. significa.t reduction of the serum level of interleukin-1 beta.[IL-1 beta., cyclooxygena.e-2 [COX-2] a.d prosta.la.din E2 [PGE2] wa. observed in CFa.ra.s.

关键词： Isoquinoline Pla.sible Binding Mode Prosta.la.din E2 (PGE2) Indometha.in Liga.dScout Softwa.e

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