- Novel Benzofuran Derivatives: Synthesis and Antitumor Agents
Heterocyclic Communications, سبتمبر 2012
D.I. Ali
Abdelal A. M.
Serry A. A. El Bialy
- Pirfenidone structural isosteres: design, synthesis and spectral study
Heterocyclic Communications Volume 18 Issue 4, الصفحات 193-197, Sept 2012
كاويليا فتحى عبد القادر - طالبة دراسات عليا
Serry A. A. El Bialy
El-Ashmawy M. B.
ديفيد بويكن - جامعة ولاية جورجيا
المرفقات
- Synthesis and in Vitro Activity of Novel Non-Nucleoside Derivatives as Anti-HCV Agents
Mansoura J.of Pharmaceutical sciences, 27 (2) 2011, يناير 2011
Amany S. M.
Serry A. A. El Bialy
Waleed A. Bayoumi
Abdelal A. M.
- [1,2,4]Triazolo[4,3-a]quinoxaline: synthesis, antiviral, and antimicrobial activities
MEDICINAL CHEMISTRY RESEARCH, August 2011
M.A.HENEN
Serry A. A. El Bialy
Fatma Goda
Magda N. A. Nasr
H. M. Eisa
الملخص الملخص [1,2,4]Triazolo[4,3-a]quinoxaline: synthesis, antiviral, and antimicrobial activities A series of novel [1,2,4]triazolo[4,3-a]quinoxa-line derivatives and their isosteres,pyrimido-quinoxaline, were synthesized as potential antiviral and antimicrobial agents. The new compounds were synthesized via aromatic nucleophilic substitution of 4-chloro-8-menthyI[1,2,4]triazolo[4,3-a]quinoxaline-1-amine with different amines and triazole-2-thiol. Some of the synthesized compounds were subjected to antiviral and cytoxtoxicity screening using plaque-erduction assay . Most of the tested compounds exhibited cytotoxicity at concentration 160 mg/mI and compound 8b showed promising antivitral activity. In virto antimicrobial screening against different pathogenic organisms using agardiffusion method demonstrated that compounds 4d,6c,7b and 8a exhibit antibacterial and/or antifungal activities
- Cyanoacetamide in heterocyclic chemistry: Synthesis, antitumor and antioxidant activities of some new benzothiophenes
Journal of Heterocyclic Chemistry, الصفحات 48و 1280–1286, أغسطس 2011
Gouda M. A.
Serry A. A. El Bialy
الملخص الملخص Cyanoacetamide in heterocyclic chemistry: Synthesis, antitumor and antioxidant activities of some new benzothiophenes Cyanoacylation of 2-amino-tetrahydrobenzothiophene-3-carboxylate ethyl ester with 3-(3,5-dimethyl-1H-pyrazol-1-yl)-3-oxopropanenitrile afforded cyanoacetamide 2. The later was utilized as key intermediate for the synthesis of 3-substituted 2-iminocoumarins 3–6 and acrylamides 7a, bvia Knoevenagel condensation with 2-hydroxy-1-naphthaldehyde; 2-hydroxybenzaldehyde; 1-nitrosonaphthalen-2-ol; 7-hydroxy-5-methoxy-2-methyl-4-oxo-4H-chromene-6-carbaldehyde; 4-dimethylamino-benzaldehyde; and 4-piperidin-1-yl-benzaldehyde in EtOH/piperidine. The derivatives 7a, b did not afford the pyrazoles 8a, b upon treating with phenyl hydrazine. Furthermore, coupling of 2 with 4-amino-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one and 4,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-3-amine afforded the hydrazone derivatives 9 and 10, respectively. The later derivative 10 was cyclized in acetic acid to afford the pyridopyrazolotriazine 11. Finally, 2 was treated with dimethylformamide-dimethylacetal (DMF-DMA) to afford the dimethylaminoacrylamide 12 which underwent transamination with 4,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-3-amine to afford the pyrazole 13. Cyclization of compound 13 in acetic acid or pyridine was unsuccessful. The antitumor and antioxidant activities of the synthesized products were evaluated; several were found to exhibit promising antioxidant activities. J. Heterocyclic Chem., (2011).
- Current progress in antifibrotics
Current Medicinal Chemistry. volume 18 , الصفحات 3082-3092, June 2011
Serry A. A. El Bialy
كاميليا فتحى عبد القادر - طالبة ماجستير
El-Ashmawy M. B.
المرفقات
- Efficient Regioselective Three-Component Domino Synthesis
of 3-(1,2,4-Triazol-5-yl)-1,3-thiazolidin-4-ones as Potent
Antifungal and Antituberculosis Agents
Arch. Pharm. Chem. Life Sci. , الصفحات 2011, 344, 821–829, 2/2011
Serry A. A. El Bialy
Maria M. Nagy - Department of Applied and Environmental Microbiology, Georgia State University
حمدى محمد عبد الرحمن - جامعة أسيوط
الملخص الملخص Efficient Regioselective Three-Component Domino Synthesis
of 3-(1,2,4-Triazol-5-yl)-1,3-thiazolidin-4-ones as Potent
Antifungal and Antituberculosis Agents In research for promising antibacterial and antifungal compounds, a series of 2-aryl 3-[1,2,4]triazol-5-
yl 4-thiazolidinones 1 were synthesized by a domino reaction of 5-amino-1H-[1,2,4]triazoles 3, aromatic
aldehydes, and a-mercaptoacids in boiling toluene in the presence of molecular sieves 4 A°
. Of the
twenty novel 3-[1,2,4]triazol-5-yl 4-thiazolidinone derivatives, four compounds 2-benzo[d][1,3]dioxol-6-
yl-3-[(3-morpholin-4-yl)-1H-1,2,4-triazol-5-yl)]-1,3-thiazolidin-4-one (1i), 2-(4-chlorophenyl)-5-methyl-3-[3-
(4-methylpiperazin-1-yl)-1H-1,2,4-triazol-5-yl]-1,3-thiazolidin-4-one (1p), 2-benzo[d][1,3]dioxol-6-yl-3-[3-
(4-methylpiperazin-1-yl)-1H-1,2,4-triazol-5-yl]-1,3-thiazolidin-4-one (1s), 2-benzo[d][1,3]dioxol-6-yl-5-
methyl-3-[3-(4-methylpiperazin-1-yl)-1H-1,2,4-triazol-5-yl]-1,3-thiazolidin-4-one (1t) exhibited MICs of
4 mg/mL or less versus Mycobacterium tuberculosis. Moreover, these compounds were screened
against Candida albicans. Compounds 1p, 1s gave MICs of 1 mg/mL or less, and were fungicidal.
Finally, compound 1s was evaluated against an expanded fungal panel and showed good activity
against Cryptococcus neoformans. In addition, compound 1s also appeared to be fungicidal against
Aspergillus arrhizus, with MIC <1 mg/mL.
- Synthesis of benzyloxycyanophenylboronic esters
Heterocyclic Communication , الصفحات 11–16, 2/2012
Serry A. A. El Bialy
كاميليا فتحى عبد القادر - جامعة المنصورة
David W. Boykin - Georgia State University
الملخص الملخص Synthesis of benzyloxycyanophenylboronic esters The synthesis of six new benzyloxycyanoboronic esters
2-benzyloxy-6-cyanophenyl-4,4,5,5-tetramethyl-[1,3,2]-
dioxaborolane ( 4a ), 4-benzyloxy-2-cyanophenyl-4,4,5,
5-tetramethyl-[1,3,2]dioxaborolane ( 4b ), 4-benzyloxy-3-
cyanophenyl-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane ( 8a ),
2-benzyloxy-5-cyanophenyl-4,4,5,5-tetramethyl-[1,3,2]-
dioxaborolane ( 8b ), 3-benzyloxy-4-cyanophenyl-4,4,5,5-
tetramethyl-[1,3,2]dioxaborolane ( 12a) , and 2-benzyloxy-5-
cyanophenyl-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane ( 12b )
is reported.
المرفقات
- Dicationic phenyl-2,20-bichalcophenes and analogues as antiprotozoal agents
Bioorganic & Medicinal Chemistry , الصفحات 978–984, يناير 2011
Serry A. A. El Bialy
Reto Brun - Swiss Tropical and Public Health Institute
Tanja Wenzler - Swiss Tropical and Public
Rupesh Nanjunda - Georgia State University
W. David Wilson - Georgia State University
David W. Boykin - Georgia State University
الملخص الملخص Dicationic phenyl-2,20-bichalcophenes and analogues as antiprotozoal agents A series of phenyl-2,2’-bichalcophene diamidines 1a–h were synthesized from the corresponding dinitriles
either via a direct reaction with LiN(TMS)2, followed by deprotection with ethanolic HCl or through
the bis-O-acetoxyamidoxime followed by hydrogenation in acetic acid and EtOH over Pd–C. These diamidines
show a wide range of DNA affinities as judged from their DTm values which are remarkably sensitive
to replacement of a furan unit with a thiophene one. These differences are explained in terms of the
effect of subtle changes in geometry of the diamidines on binding efficacy. Five of the eight compounds
were highly active (below 6 nM IC50) in vitro against Trypanosoma brucei rhodesiense (T. b. r.) and four
gave IC50values less than 7 nM against Plasmodium falciparum (P. f.). Only one of the compounds was
as effective as reference compounds in the T. b. r. mouse model for the acute phase of African
trypanosomiasis
المرفقات
- A Total Synthesis of(-)-g-Lycorine
Natural Product Research , الصفحات 1176-1188, 2008
Serry A. A. El Bialy
- Efficient Synthesis ofCephalotaxine- and Deoxyharringtonine Analogues by a Trimethylaluminium Mediated Domino-Reaction.
Tetrahedron, الصفحات 6437–6445, 2007
Serry A. A. El Bialy
Lutz F. Tietze, Holger Braun, Peter L.Steck, Serry A.A. El Bialy, Nina T?lle, Alexander Düfert
- Perchlorate mixed–ligand copper(II)complexes of b-diketone and ethylene Diamine derivatives: Thermal, spectroscopic and biochemical studies
Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy, الصفحات 1278-1286, 2007
Serry A. A. El Bialy
Usama El-Ayaan, Nashwa M. El-Metwally, Magdy M. Youssef, Serry A.A. El Bialy
- Generation of b-Keto Radicals from Cyclopropanols Catalyzed by AgNO3.
Chemistry Letters, الصفحات 35, 18, , 2006
Serry A. A. El Bialy
Shunsuke Chiba, Zhengyan Cao, Serry A. A.El Bialy, Koichi Narasaka
- 2,3-Bis (5-alkyl-2-thiono-1,3,5-thiadiazin-3-yl) propionic acid: One-Pot Domino Synthesis and Antimicrobial activity
Arch. Pharm. Chem. Life Sci, الصفحات 338, 38-43 , 2005
Serry A. A. El Bialy
Abdelal A. M.
Serry A. A. El Bialy, Ali M. Abdelal A. El Shorbagy, Samy M. M. Kheira
- Enantioselective Synthesis of a-Alkyl Malates as the Pharmacophoric Group of Several Natural Alkaloids and Glycosides
Eur. J. Org. Chem., الصفحات 2965-2972 , 2005
Serry A. A. El Bialy
Serry A. A. El Bialy, Holger Braun, Lutz F. Tietze
- A Highly efficient synthesis of Erythrina and B-Homoerythrina skeleton by AlMe3-mediated domino reaction
Angew. Chem.Int.Engl, الصفحات 43, 5391-5393 , 2004
Serry A. A. El Bialy
A. A. El Bialy, Holger Braun, Lutz F. Tietze
- Enantioselective synthesis of(1S,2S)-1,2-di-tert-butyl and (1R,2R)-1,2-di(1-adamantyl)ethylenediamines
Tetrahedron lett.,, الصفحات 45, 8073-8077 , 2004
Serry A. A. El Bialy
Alaa A.-Abdel-Aziz, Serry A. A. El Bialy, Fatma E. Goda, Takehisa Kunieda
- Synthesis of azaspiro[4.4]nonanes as key structures of bioactive natural products
Synthesis, الصفحات 2249-2262 , 2004
Serry A. A. El Bialy
products Serry A. A. El Bialy, Holger Braun, Lutz F. Tietze
- A New approach to the bridged indole alkaloids
Medicinal Chem. Research, الصفحات 12 (8), 415-434 , 2003
Serry A. A. El Bialy
Serry A. A. El Bialy
- Efficient formal total syntheses of (-)-cephalotaxine using reductive intramolecular Heck reaction and optical resolution
Medicinal Chem. Research, الصفحات 11, 293-300 , 2003
Serry A. A. El Bialy
Serry A. A. El Bialy, Mohamed A. Ismail , Laila M. Gad, and Ali M. M. Abdelal
- 5-Endo-trig radical cyclization of N-benzyl-2-halo-N-(6-oxo-1-cyclohexen-1-yl)-acetamides.
Heterocycles, الصفحات 54 (2), 1021-1025 , 2001
Serry A. A. El Bialy
Shinji Ohtani, Tatsunori Sato, Masazumi Ikeda
- A facile One-Pot Synthesis of Pyrido[2,3-d]- and Quinolino[2,3-d]pyrimidines
Heterocycles, الصفحات 1315-1321 , 2001
Serry A. A. El Bialy
Ismail M. A.
- A one-pot synthesis of pyrido[2,3-d]-andquinolino[2,3-d]pyrimidines
Heterocycles, الصفحات 55, (7) 1315-1321 , 2001
Serry A. A. El Bialy
Abdel Aziz S. El-Ahl, Serry A. A. El Bialy, Mohamed A. Ismail
- Diastereoselective synthesis of 2-alkylated 4-silyloxyproline esters
J. Chem. Soc. Perki Trans., الصفحات 1, 2623-2631 , 2001
Serry A. A. El Bialy
Tatsunori Sato, Satomi Kawasaki, Nobuo Oda, Shoko Yagi, Serry A. A. El Bialy, Jun`ichi Uenishi, Masashige Yamauchi, Masazumi Ikeda
- Synthesis of bridged benzoazabicyclic compounds using radical translocation/ cyclization reactions of 1-alkynyl-2-(o-iodobenzoyl) tetrahydroisoquinolines.
Heterocycles, الصفحات 52 (2), 571-574, 2000
Serry A. A. El Bialy
Yuka Nakano
Said M. M. Bayomi
Tatsunori Sato
Masazumi Ikeda
Masahiro Hamada
Katsuaki Matsui
Shimpei Kawakami
- A Formal Total Synthesis of(-)-Cephalotaxine
Chem. Pharm. Bull. 47 (1999) 983-987, الصفحات 983 -987, يناير 1999
Masazumi Ikeda - Kyoto Pharmaceutical University
أ.د. سعيد محمد محمود بيومى
Abdelal A. M.
Serry A. A. El Bialy
- A formal total synthesis of(-)-cephalotaxine.
Chem. Pharm. Bull. , الصفحات 47(7) 983-987 , 1999
Serry A. A. El Bialy
Masazumi Ikeda
Ken-ichi Hirose
Miho Kotake
Tatsunori Sato
- Synthesis of heterocycles using the intramolecular Heck reaction involving a ‘formal’ anti-elimination process.
Heterocycles, الصفحات 51(8),1957-1970 , 1999
Serry A. A. El Bialy
Masazumi Ikeda
Takayuki Yakura
- Approaches to the cephalotaxine skeleton using an intramolecular Heck reaction.
Chem. Pharm. Bull. , الصفحات 46(7) 1084-1089, 1998
Serry A. A. El Bialy
Masazumi Ikeda, Ken-ichi Hirose,
- Synthesis of certain benzothiazole derivatives to be evaluated as anthelmintics
Man. J. Pharm. Sci., الصفحات 79-88
H. M. Eisa
Magda N. A. Nasr
Serry A. A. El Bialy
مامون يوسف يوسف - جامعه المنصورة- كلية الصيدلة-قسم الكيمياء الطبية
الملخص الملخص Synthesis of certain benzothiazole derivatives to be evaluated as anthelmintics New derivatives of 6-nitro-2-substitutedacetamidobenzothiazole (2a,3a-e), 3-substituted 2-iminothiazolidin-4-one (4a-e) and 5-arylidene-2-iminothiazolidin-4-one (5a-j) were prepared. The testing for the anthelmintic activity of two of the newly prepared compounds using the earthworm method showed that they produce a promising effect. The detailed synthesis, spectroscopic and biological data are reported .
- Synthesis and anthelmintic properties of new benzimidazoles
Alexandria J.Pharm. Sci.,, الصفحات 155-160, 1996
Serry A. A. El Bialy
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