Tarek Aboul-Fadl

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The new title derivatives (4b-h and 5a-i) were synthesized by reaction of the appropriate primary amine, carbon disulphide, and formaldehyde. These derivatives were prepared in order to study the effects of introducing polar groups at N3 or N5 or at both positions on the biological activity. The compounds were tested for their antifungal activity in vitro(More)
Two series of tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivatives were synthesized, 2a-f and 3a-f, by incorporation of beta-alanine and beta-phenylalanine, respectively, at the 5th position of the THTT moiety. Structures of these derivatives were verified by spectral and elemental methods of analyses. The lipophilic properties of the synthesized(More)
3-Substituted-5-(4-pyridylcarboxamido)tetrahydro-2H-1,3,5-thiad iazine-2- thione derivatives 5a-e were synthesized as prodrugs for isoniazid (INH) to overcome the resistance developed with its therapeutic use. These prodrugs revealed higher lipophilicity compared with INH. Their degradation kinetics were studied in vitro using aqueous buffer solutions of pH(More)
Selenite and organoselenium compounds have been examined at supranutritional levels for their ability to influence the activity and mRNA levels of chemoprotective enzymes in the livers of selenium-sufficient mice and the changes compared to those elicited by oltipraz. Compounds investigated included novel selenocysteine prodrugs that have previously been(More)
A series of 5-phenyl-1-(3-pyridyl)-1H-1,2,4-triazole-3-carboxylic acid derivatives 4-10 were synthesized by rearrangement of 4-(3-pyridyl)-hydrazono-2-phenyl-2-oxazolin-5-one 3 in the presence of different nucleophiles to afford derivatives 4, 7, and 8, while hydroxamic acid derivative 6 was prepared from reaction of methyl ester 4 with hydroxylamine(More)
AIMS The aims of this study were to identify analogues of L-proline which inhibit the growth of Escherichia coli in both laboratory culture media and normal human urine and to study their mechanisms of uptake. METHODS AND RESULTS The susceptibility of E. coli to L-proline analogues was studied by radial streak assays on agar plates and by minimal(More)
The use of antisense oligonucleotides as therapeutic agents has generated considerable enthusiasm in the research and medical community. Antisense oligonucleotides as therapeutic agents were proposed as far back as in the 1970s when the antisense strategy was initially developed. Nonetheless, it has taken almost a quarter of a century for this potential to(More)
A series of disubstituted tetrahydro-W-1,3,5-thiadiazine-2-thione (THTT) derivatives 4a-g were prepared and found to be promising prodrugs for amino acids and similar compounds. The pH profile for the degradation of the THTT derivatives in aqueous buffer solutions was determined using HPLC and was accounted for in terms of specific base-catalyzed reactions.(More)
UNLABELLED BACKGROUND Cancer is one of the most dreaded diseases and it is a leading cause of mankind death worldwide. Recent reports documented a remarkable antiproliferative activity of isatin nucleus against various cancer cell lines. The current work describes the antiproliferative activity of Schiff bases of combinatorial mixtures of the isatin(More)
N'-(1-alkyl-2,3-dihydro-2-oxo-1H-3-indolyliden)-4-pyridinecarboxylic acid hydrazide derivatives, 3(a-g), were synthesized in a trial to overcome the resistance developed with the therapeutic uses of isoniazid (INH). The lipophilicity of the synthesized derivatives supersedes that of the INH as expressed by Clog p values. The synthesized compounds and INH(More)