Saco Pharm. Co.

Madīnat Sittah Uktūbar, Egypt

Saco Pharm. Co.

Madīnat Sittah Uktūbar, Egypt
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Dawood D.H.,National Research Center of Egypt | Batran R.Z.,National Research Center of Egypt | Farghaly T.A.,Cairo University | Farghaly T.A.,University of Umm Al - Qura | And 2 more authors.
Archiv der Pharmazie | Year: 2015

Two new series of coumarin derivatives incorporating thiazoline and thiazolidinone moieties were designed, synthesized, and investigated in vivo for their anti-inflammatory activities using the carrageenan-induced rat paw edema model and in vitro for their inhibitory activities against the human cyclooxygenase (COX)-1 and COX-2 isoforms. Most of the synthesized compounds demonstrated exceptionally high in vivo anti-inflammatory activity and displayed superior GI safety profiles (0-7% ulceration) as compared to indomethacin. All the bioactive compounds showed in vitro high affinity and selectivity toward the COX-2 isoenzyme, compared to the reference celecoxib with IC50 values ranging from 0.31 to 0.78 μM. The ethyl thiosemicarbazone 2b, thiazoline derivatives 3a, 3b, 5b, 6a, and 7f, and the thiazolidinone compounds 8b and 9a showed the highest in vivo and in vitro anti-inflammatory activities with remarkable COX-2 selectivity. Quantitative structure-activity relationship study (QSAR) was done and resulted in a highly predictive power R2 (0.908). A molecular docking study revealed a relationship between the docking affinity and the biological results. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Amr A.E.E.,King Saud University | Amr A.E.E.,National Research Center of Egypt | Abu Ghalia M.H.,National Research Center of Egypt | Al-Omar M.A.,King Saud University | Abdalla M.M.,Saco Pharm. Co.
Latin American Journal of Pharmacy | Year: 2016

A series of macrocyclic dipicolinic acid acylated peptides based on upper rim bridged peptidocalix[4]arene and peptidopyridine derivatives 1-10 were synthesized before as antimicrobial agents. In continuation of our previous work, herein we used these compounds 1-10 for evaluated as anticancer agents. All the tested compounds showed potent anticancer activities against many cancer cell lines on nano molar levels. © 2016, Colegio de Farmaceuticos de la Provincia de Buenos Aires. All rights reserved.


Amr A.E.E.,King Saud University | Amr A.E.E.,National Research Center of Egypt | Al-Omar M.A.,King Saud University | Abdalla M.M.,Saco Pharm. Co.
International Journal of Pharmacology | Year: 2016

A series of chiral linear and macrocyclic bridged pyridines (1-8) has been prepared starting from pyridine-2,6-dicarbonyl dichloride andthey screened as antimicrobial agents before. Screening of the compounds for their Inhibition of type A and type B monoamine oxidaseactivities in mitochondria preparation revealed that the tested compounds showed selective inhibition of type A monoamine oxidaseactivities in the following order 4a, 6, 5a, 3, 4b, 5b, 1, 4c, 7, 8 and 2, this confirmed by the in vivo tryptamine seizure potentiation modelin rats. The tested compounds showed in vivo good pharmacokinetic and pharmacodynamic profiles. © 2016 Abd El-Galil E Amr et al.


Amr A.E.E.,King Saud University | Amr A.E.E.,National Research Center of Egypt | Al-Omar M.A.,King Saud University | Abdalla M.M.,Saco Pharm. Co.
International Journal of Pharmacology | Year: 2016

Ten pyridine and pyrimidine and thiazolopyrimidine derivatives (1-10) were synthesized and screened as analgesic, anticonvulsant and antiparkinsonian agent before. Herein, all the target compounds showed anti-inflammatory activity. The active compounds showed selective inhibitory activity towards COX-2 enzyme as revealed by the in vitro enzymatic assay. All the tested compounds proved to have superior gastrointestinal (GI) safety profiles as compared to indomethacin, when tested for their ulcerogenic effects. © 2016 Abd El-Galil E. Amr et al.


Eldebss T.M.A.,Cairo University | Farag A.M.,Cairo University | Abdulla M.M.,Saco Pharm. Co | Arafa R.K.,Cairo University
Mini-Reviews in Medicinal Chemistry | Year: 2016

The design and synthesis of a novel series of benzo[d]imidazole-based heterocycles and their biological evaluation as antiviral agents are reported herein. 1-(1-Methyl-1H-benzo[d]imidazol- 2-yl)-2-thiocyanatoethanone 2 was used as a key intermediate for the synthesis of the thiazolylhydrazine 4, the thiazolylamine 5 and the methylthiazole 7. Coupling of compounds 5 or 7 with the appropriate diazotized aromatic amines gave the diazenyl derivatives 6a-c and 8a-c, respectively. The quinazoline derivative 12 was also synthesized. On the other hand, the phenylthio 20 and the phenylsulphonyl 22 bioisosteresand their respective diazenyl derivatives 21a-c and 23a-c were prepared. The synthesized compounds were evaluated for their HIV-1, HCV, SSPE and H1N1 inhibitory activities and were found to display very promising results. Furthermore, to investigate the underlying possible mechanism of action, in vitro and in silico screening of this series of benzo[d]imidazoles was performed against the viral enzymes HIV-1 RT, HCV NS3/4A serine protease and H1N1 NA 1. Overall findings of the executed investigations highlight these novel compounds as very promising potent, broad spectrum antiviral agents. © 2016 Bentham Science Publishers.


Abdalla M.M.,Saco Pharm. Co. | Al-Omar M.A.,King Saud University | Al-Salahi R.A.,King Saud University | Amr A.G.E.,King Saud University | And 2 more authors.
International Journal of Biological Macromolecules | Year: 2012

We herein report the anti-Alzheimer activity of some synthesized heterocyclic pyrimidine and thiopyrimidine derivatives fused with steroidal structure. Twenty-one of these compounds were synthesized and conveniently screened for their anti-Alzheimer activities using of Flurbiprofen as the reference drug. Some of these compounds were demonstrated to exhibit remarkable activity and their β-amyloid (Aβ) lowering results as IC50 values reported. © 2012 Elsevier B.V.


Gomha S.M.,Cairo University | Eldebss T.M.A.,Cairo University | Abdulla M.M.,Saco Pharm. Co. | Mayhoub A.S.,Al - Azhar University of Egypt
European Journal of Medicinal Chemistry | Year: 2014

Cellular tumor antigen p53 is crucial for cancer prevention via different mechanisms. E3 ubiquitin-protein ligase HDM2 binds to p53, blocks its ability to activate transcription, and therefore acts as a negative regulator. Blocking p53 binding site on HDM2 was believed to generate efficient antitumor agents. So far, limited scaffolds were reported with HDM2 antagonist activity. Herein, diphenylpyrroles were introduced and evaluated as a novel scaffold in the field of p53 activators. An efficient synthesis of novel 3-heteroaryl-pyrroles is described via reactions of E-3-(dimethylamino)-1-(2-methyl-4,5-diphenyl-1H- pyrrol-3-yl)prop-2-en-1-one or E-1-(2-methyl-4,5-diphenyl-1H-pyrrol-3-yl)-3- morpholinoprop-2-en-1-one with hydrazine hydrate, phenyl hydrazine, hydroxylamine, various heterocyclic amines and active methylene compounds. © 2014 Elsevier Masson SAS. All rights reserved.


Abdalla M.M.,Saco Pharm. Co. | Al-Omar M.A.,King Saud University | Bhat M.A.,King Saud University | Amr A.G.E.,King Saud University | And 2 more authors.
International Journal of Biological Macromolecules | Year: 2012

The aromatase and quinone reductase-2 inhibition of synthesized heterocyclic pyrazole derivatives fused with steroidal structure for chemoprevention of cancer is reported herein. All compounds were interestingly less toxic than the reference drug (Cyproterone ®). The aromatase inhibitory activities of these compounds were much more potent than the lead compound resveratrol, which has an IC 50 of 80μM. In addition, all the compounds displayed potent quinone reductase-2 inhibition. Initially the acute toxicity of the compounds was assayed via the determination of their LD 50. The aromatase and quinone reductase-2 inhibitors resulting from this study have potential value in the treatment and prevention of cancer. © 2012.


Alanazi A.M.,King Saud University | Al-Omar M.A.,King Saud University | Abdulla M.M.,Saco Pharm. Co. | Amr A.E.G.E.,King Saud University | Amr A.E.G.E.,National Research Center of Egypt
International Journal of Biological Macromolecules | Year: 2013

We herein report the anti-arthritic and immunosuppressive activities of some synthesized substituted terpenoidal structure. Forty-four triterpenoid derivatives 1-21 containing a carboxylic, ester, amide and ketone groups attached to a triterpene moiety were conveniently synthesized and screened for their anti-arthritic and immunosuppressive activities. Synthetic triterpenoidal structures linked to a different function groups seem to be a promising approach in the search for novel leads for potent anti-arthritic and immunosuppressive agents. The detailed synthetic pathways of obtained compounds and anti-arthritic and immunosuppressive activities were reported. © 2013 Elsevier B.V.


Shawali A.S.,Cairo University | Farghaly T.A.,Cairo University | Hussein S.M.,Cairo University | Abdalla M.M.,Saco Pharm. Co
Archives of Pharmacal Research | Year: 2013

Reactions of hydrazonoyl halides with cyanoacetic hydrazide and its N-arylidene derivatives proceeded site-selectively and afforded the respective pyrazolo[3,4-d]pyridazine and aldehyde N-(1-aryl-3-acetyl-4-cyanopyrazol-5-yl) hydrazone derivatives. The structures of the products were elucidated on the basis of their spectral and elemental analyses. The anti-aggressive activity of the compounds prepared was screened. © 2013 The Pharmaceutical Society of Korea.

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