N. M. Khalifa

HIV-1 and HSV-1 virus activities of some new polycyclic nucleoside pyrene candidates.

In continuation of our previous work, a novel series of polycyclic derivatives 2-8 incorporated heterocyclic and sugar moieties were synthesized by using pyren-1-aldehyde (1) as starting material and their tested as antiviral activities. Initially, the toxicity of the compounds was assayed via the determination of their EC(50). Some of the synthesized compounds were tested as antiviral activity against HIV-1 and HSV-1. The structure of the new compounds was confirmed by using chemical and spectroscopic evidences. The detailed of synthesis, spectroscopic data, antiviral activities of the synthesized compounds were reported.

Biological Validation of Novel Polysubstituted Pyrazole Candidates with in Vitro Anticancer Activities

With the aim of developing novel antitumor scaffolds, a novel series of polysubstituted pyrazole derivatives linked to different nitrogenous heterocyclic ring systems at the C-4 position were synthesized through different chemical reactions and characterized by means of spectral and elemental analyses and their antiproliferative activity against 60 different human tumor cell lines was validated by the U.S. National Cancer Institute using a two stage process. The in vitro anticancer evaluation revealed that compound 9 showed increased potency toward most human tumor cell lines with GI50MG-MID = 3.59 µM, as compared to the standard drug sorafenib (GI50 MG-MID = 1.90 µM). At the same time, compounds 6a and 7 were selective against the HOP-92 cell line of non-small cell lung cancer with GI50 1.65 and 1.61 µM, respectively.

Synthesis and biological evaluation of some novel fused thiazolo[3,2-a]pyrimidines as potential analgesic and anti-inflammatory agents

Some novel bicyclic thiazolopyrimidine derivatives bearing various substituents have been synthesized through one-pot three-component method. Structures of the target compounds were confirmed by elemental analysis and spectral data. Some selected members of the newly synthesized compounds were investigated for their analgesic and anti-inflammatory activities and revealed pronounced anti-inflammatory activity greater than that of indomethacin (reference drug).

Synthesis and Anti-Inflammatory Activities of Some Novel S-Pyridyl Glycosides Derivatives

A series of some new acetylated S-glycosides of pyridine-2-thione derivatives, including D-glucose, D-galactose, D-xylose and L-arabinose derivatives were synthesized. Oxidation of some formed S-glycosides derivatives with H2O2 afforded the corresponding sulfones. S-Alkylation of pyridine-2-thione derivatives was performed to furnish the S-acyclo deazauridine derivatives. The entire tested compound showed potent anti-inflammatory activity were potent against edema and in the same time inhibited the prostaglandine formation. It is work mention that all the tested compounds showed high safety margin. The structures of the new synthesized compounds have been proved by IR, 1 HNMR, mass spectra and elemental analysis.

Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents

With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound 6b showed increased potency with % inhibition of edema 85.23 ± 1.92 and 85.78 ± 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior.

Synthesis, characterization and pharmacological investigations of some novel heterocyclic derivatives incorporating pyrene and sugar moieties

A series of substituted pyrene derivatives 2–15 incorporated heterocyclic and sugar moieties were synthesized and evaluated as antiviral activities using 1-acetylpyrene as a starting material. The structure assignment of the new compounds was based on chemical and spectroscopic evidence. The detailed synthesis, spectroscopic data and pharmacological activities of the synthesized compounds were reported.

Synthesis, reactions, and antimicrobial activity of some novel fused thiazolo[3,2-a]pyrimidine-5H-indeno[1,2-d]pyrimidine derivatives

Series of novel substituted thioxopyrimidine and thiazolo[3,2-a]pyrimidine compounds that combine various heteroaryl rings have been synthesized via Biginelli one-pot three-component reaction and elucidated with chemical and spectral analysis. Several products were tested for their antimicrobial properties.

Synthesis and Reactions of New Chiral Linear Carboxamides with an Incorporated Peptide Linkage Using Nalidixic Acid and Amino Acids as Starting Materials

4b A series of chiral linear carboxamide derivatives (2- 15) with an incorporated peptide linkage have been prepared via the coupling of 1-ethyl-1,4-dihydro-7-methyl-4-oxo-quinoline-3-carboxylic acid (nalidixic acid, 1) with appropriate amino acid methyl esters. Coupling of 1 with amino acid methyl esters gave the corresponding peptide methyl esters 2, which were hydrolyzed with methanolic sodium hydroxide to the corresponding acids 3. Hydrazinolysis of esters 2with hydrazine hydrate afforded the corresponding acid hydrazide derivatives 4. The latter compounds were coupled with appropriate aldehydes or acetophenone derivatives to afford the corresponding Schiff base derivatives 5 and 6, respectively. The hydrazide derivative was reacted with phenyl isothiocyanate or carbonyl derivatives to give the corresponding thiosemicarbazide 7 and compounds 8- 10, respectively. Also, 4b was treated with acid monoanhydrides to give the corresponding imide derivatives 11- 13. Finally, 4b was reacted with tetracarboxylic acid dianhydride derivatives to afford the corresponding diimido carboxamide derivatives 14 and 15 Graphical Abstract Synthesis and Reactions of New Chiral Linear Carboxamides with an Incorporated Peptide Linkage Using Nalidixic Acid and Amino Acids as Starting Materials

Synthesis and evaluation of novel 6-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents

A novel series of uracil derivatives with a 3,5-dimethylbenzyl group at the C-6 position were synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Purity of the compounds has been confirmed by TLC. Structures of these compounds were established on the basis of elemental analyses and spectral studies. Some of the tested compounds showed moderate to potent activities against wildtype HIV-1, and N-1 alkylated derivatives were highly active.

Synthesis and antimicrobial activities of some newly 2,4,6-tri-substituted pyridine derivatives

A series of novel 2-(2-(substituted benzylidene)hydrazinyl)-N′-(substituted benzylidene)-6-chloropyridine-4-carbohydrazide (5a–e), 2-(2-cycloalkylidenehydrazinyl)-6-chloro-N’-cyclo-alkylidenepyridine-4-carbohydrazide (6a,b), 2-(2-(1-(4-substituted phenyl)ethylidene)hydrazinyl)-6-chloro-N′-(1-(4-substituted phenyl)ethylidene)pyridine-4-carbohydrazide (7a,b) and 2-(2-(1-(pyridinyl)ethylidene)hydrazinyl)-6-chloro-N′-(1-(pyridinyl) ethylidene)pyridine-4-carbo-hydrazide (8a–c) derivatives have been synthesized by treating treating 2-chloro-6-hydrazinoisonicotinic acid hydrazide 4 with selected active reagents. Their structures were confirmed by spectral and analytical data. The synthesized compounds were investigated for antimicrobial activities. The antimicrobial screening showed that many of these obtained compounds have good activities comparable to Streptomycin and Fusidic acid as reference drugs.