Browsing by Author "Refaey R.H."

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Metabolomic profiling and biological investigation of Tabebuia Aurea (Silva Manso) leaves, family Bignoniaceae
(Taylor and Francis Ltd., 2019) Mahmoud B.K.; Hamed A.N.E.; Samy M.N.; Abdelmohsen U.R.; Attia E.Z.; Fawzy M.A.; Refaey R.H.; Salem M.A.; Pimentel-Elardo S.M.; Nodwell J.R.; Desoukey S.Y.; Kamel M.S.; Department of Pharmacognosy; Faculty of Pharmacy; Minia University; Minia; Egypt; Department of Pharmacognosy; Faculty of Pharmacy; Deraya University; New Minia City; Egypt; Departmentof Biochemistry; Faculty of Pharmacy; Minia University; Minia; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Department of Biochemistry; University of Toronto; Toronto; ON; Canada
Both ethyl acetate and aqueous fractions of Tabebuia aurea leaves exhibited noteworthy antioxidant and nephroprotective activities against carbon tetrachloride (CCl4)-induced nephrotoxicity in rats, as evidenced by the remarkable improvements of renal serum biomarkers and histopathological features. Additionally, the ethyl acetate fraction displayed a prominent in vitro antitrypanosomal activity against Trypanosoma brucei; consequently, the leaves were subjected to LC-HR-ESI-MS metabolomic profiling to discover the constituents that possibly underlie their bioactivities. Therefore, ten metabolites were characterized, mostly dominated by flavonoids. Interestingly, two identified constituents viz., 3,9,12,15-octadecatetraenoic acid (9) and 9,11,13-octadecatrienoic acid (10) are reported firstly herein from the genus Tabebuia. Furthermore, among the dereplicated constituents, rutin (5) and kaempferol 3-O-rutinoside (6) exhibited the highest docking scores as effective antitrypanosomal compounds. � 2019, � 2019 Informa UK Limited, trading as Taylor & Francis Group.
Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives
(Elsevier Masson SAS, 2019) Mahmoud W.R.; Nissan Y.M.; Elsawah M.M.; Refaey R.H.; Ragab M.F.; Amin K.M.; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; Drug Research Center; Cairo; Egypt; Pharmacology and Toxicology Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt
Twenty four 6-aminocoumarin based derivatives were synthesized according to two schemes. All the compounds were screened for their acetylcholinesterase inhibitory activity where compound 5b proved to be the most potent AChE inhibitor with (IC50 = 37 nM) compared to tacrine and donepezil (IC50 = 55.0 and 59.0 nM, respectively). Six compounds 2f, 2g, 4b, 5b, 8b and 9b revealed superior activity over donepezil and a conclusive structure activity relationship study was conducted explaining the obtained results. Furthermore, compounds 2f, 4b and 5b were investigated for their neurobehavioral effect in vivo. All the tested compounds showed improvement of neurobehavioral experiments using donepezil as reference drug. In addition, compounds 2f, 4b and 5b were able to reduce extracellular deposition of amyloid beta 42 in a comparable manner to donepezil. The binding modes of the synthesized compounds were evaluated in silico via molecular docking in the active site of AChE, as well as molecular dynamics simulation study. A pharmacophore model was generated for the newly synthesized compounds. � 2019 Elsevier Masson SAS
New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES
(Elsevier Masson SAS, 2019) Hassan G.S.; Abdel Rahman D.E.; Abdelmajeed E.A.; Refaey R.H.; Alaraby Salem M.; Nissan Y.M.; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Badr University in Cairo; Badr City; Cairo; 11829; Egypt; National Cancer Institute; Cairo University; FomElkhalig; Kasr Elaini St.; Cairo; 11796; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt
New pyrazole derivatives 2�5 were synthesized and evaluated for their COX-1 and COX-2 inhibitory activity in vitro. All compounds showed good inhibitory activity at a nanomolar level and most compounds exhibited selectivity towards COX-2 inhibition. Compounds 2a, 3b, 4a, 5b and 5e exhibited IC50 towards COX-2 enzyme of 19.87, 39.43, 61.24, 38.73 and 39.14 nM, respectively. Furthermore, compounds 3b, 4a, 5b and 5e exhibited a selectivity index of 22.21, 14.35, 17.47 and 13.10, respectively. The most active compounds were further subjected to in vivo anti-inflammatory assay. The tested compounds showed better or comparable activity to celecoxib as positive control. In order to explore their binding mode and selectivity behaviour, molecular docking in the active site of COX-2 was carried out for these derivatives. Analysis of the docked poses of the compounds showed that they adopt similar conformations to the highly selective COX-2 inhibitor, SC-558. The docking pose of compound 3b was confirmed by molecular dynamics. All the tested compounds exhibited potent inhibitory effect on the production of PGE2, in addition to their inhibition of COX-2 enzyme. � 2019 Elsevier Masson SAS
Triazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular docking
(Academic Press Inc., 2019) Ahmed E.M.; Khalil N.A.; Taher A.T.; Refaey R.H.; Nissan Y.M.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October 6 University; Giza; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt
Novel series of some triazolo[4,3-b]pyridazine derivatives were designed and synthesized. All the newly synthesized compounds were evaluated for their cytotoxic activity at 10?5 M concentration towards 60 cancer cell lines according to USA NCI protocol. Most of the synthesized compounds showed good activity against SR (leukemia) cell panel. The most active compounds, 2f and 4a were subjected for further evaluation at a five dose level screening and their efficacy for c-Met kinase inhibition was determined in vitro. Binding mode of these derivatives was explored via molecular docking. 2019 Elsevier Inc.