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Staff Researches

Salwa Abdelwahhab

Regioselective Reactions, Spectroscopic Characterization, and Cytotoxic Evaluation of Spiro-pyrrolidine Thiophene

Salwa Saleh Abdelwahhab El Sayed

Sameh A. Rizk,a* Salwa S. Abdelwahab,b and Hanan A. Sallama

J. Heterocyclic Chemestry

2018

Spiro-oxo-indole/pyrrolidine-thiophene base possessed significant pharmacological activity. The [3 + 2] cycloaddition reactions of thia-methine ylide respected through multi-component reaction affording regioselective and stereoselective spiroindoline-3,20-tetrahydrothiophene derivative 3. Reaction of such compound with different electrophilic and nucleophilic reagents afforded bioactive heterocyclic compounds 4–16. Biological evaluation showed that these synthesized spiro-pyrrolidine exhibited moderate to good cytotoxic activity. Among them, compounds 7 and 14 displayed the best cytotoxic activity against MCF-7 and Wl-38 cells with the IC50 values of 7.02 ± 0.6 and 8.97 ± 0.9 μm (very strong), respectively. Compounds 4, 5, and 12 exhibited strong cytotoxicity’s with IC50 16.28 ± 1.7, 11.16 ± 1.1, and 19.14 ± 1.7 μm, respectively, against MCF-7 mammary gland cell line. All compound structures were supported by spectroscopic data and elemental analysis.

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Synthesis of novel 2,3- disubstituted quinazoline- 4(3H) ones and their effect on the ultrastructure of some pathogenic microorganisms

Salwa Saleh Abdelwahhab El Sayed

MAHMOUD. M.Ra, SALWA.S. ABD EL WAHABb.

Egyptian journal of chemistry

2017

A series of highly functionalized hitherto unreported quinazolinones with different substituent at position 3 have been concisely synthesized in good yields via the reaction of 3-amino-6-bromo-2-undecylquinazoline-4(H)one with one carbon donor such as phenylisothiocyanate, α- halogenated compounds and chloroacetylchloride. Moreover, the reaction of 6-bromo-2-undecylbenzoxazin-4(H)onewith different hydrazides and 2-aminothiophenol was also investigated.The structures of all new synthesized compounds in this investigation were determined using spectroscopic tools (IR, 'HNMR, MS and 13C-NMR).

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Formulation Of Ciprofloxacin Hydrochloride Loaded Biodegradable Nanoparticles: Optimization Of Technique And Process Variables

Salwa Saleh Abdelwahhab El Sayed

Pharmaceutical Development And Technology

2013

Poly lactic-co-glycolic acid (PLGA 502 H) nanoparticles incorporating ciprofloxacin HCI (CP) were prepared by double emulsion solvent diffusion technique. Methods: The influence of the application of probe sonication besides the high pressure homogenization in the preparation of the secondary emulsion and its application during the solidification step were studied. Their effect of the addition of polyvinyl alcohol (PVA) during the preparation of the primary emulsion was studied. Moreover, the effect of the addition of 0.1 M sodium chloride and/or adjusting the external and extracting phases of pH 7.4 were investigated. The selected formula was examined using IR, X-ray, DSC and SEM and in vitro drug release. Results: These formulations showed an appropriate particle size ranges between 135.7 – 187.85 nm, a mean zeta potential ranging from 0.839 to 6.81 mV and a mean of EE% which ranged from 35% to 69% Conclusion: The presented data revealed the superiority of using probe sonication besides high pressure homogenization during the formation of secondary emulsion. Moreover, the results indicated that the tested factors had a pronounced significant effect on the EE%.

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Novel Bridgehead Thiadiazolopyrimidine Derivatives with Antimicrobial and Antitumor Activities

Salwa Saleh Abdelwahhab El Sayed

Galal A. Elsayed1, Mohammad E. Azab1, Salwa S. Abdel-Wahab2

J. Heterocyclic Chemestry

1900

Due to the remarkable pharmacodynamics and chemotherapeutics activities of thiadiazolopyrimidines, A new series of 1,3,4-thiadiazolo[3,2-a] pyrimidine derivatives have been synthesized by reacting 5-substituted-2-aminothiadiazoles 1a,b with different reagents; active methylenic compounds, benzaldehyde under different conditions, isatin, and cyclic ketones. The structures of the novel compounds have been inferred by spectroscopic methods (IR, 1H-NMR, 13C-NMR, MS), and elemental analyses. The newly synthesized compounds were screened against four bacterial strains (Staphylococcus aureus and Listeria monocytogenes as Gram positive; Pseudomonas aeruginosa and Salmonella typhimurium as Gram negative) and two Fungi (Aspergillus Niger and Candida Albicans) using agar diffusion assay. Most of the compounds showed activity against the tested microorganisms with different extents. The in-vitro anticancer activities of these compounds were assessed against four human tumor cell lines, they were found to exhibit different cytotoxic effects. Such results mean that these derivatives can be further utilized as promising anticancer agents.

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Utility of 2,3-Diaryloxirane-2,3-Dicarbonitriles in Synthesis and QSAR Study of Newly Heterocyclic Derivatives as in Vitro Cytotoxic Agents

Salwa Saleh Abdelwahhab El Sayed

Sameh A. Rizk1, Salwa S. Abdelwahab1,2, Eman Zaglol3

J. Heterocyclic Chemestry

1900

2,3-Diaryloxirane-2,3-dicarbonitriles have employed in heterocyclic synthesis in many organic reactions. Authors highlight its use as intermediate in the synthesis of various organic compounds through the reaction with different nitrogen nucleophiles as methyl hydrazine, thiourea, thiosemicarbazide, methyl glycinate and others to furnish new heterocyclic derivatives. They are also used as key starting materials to construct some important heterocyclic compounds. Structures of all newly synthesized products are substantiated by studying their micro analytical and spectral data. Some of newly synthesized compounds were evaluated for their in vitro cytotoxic effects against Hep-G2 carcinoma cell lines. Most of the newly synthesized compounds (1a, 2a, 2d, 3, 4, 5, 6a, 6c, 6d, 7a and 7b) inhibited cell proliferation with IC50 values in range of 0.52–5.21 μΜ. Compounds 5, 6a, 6d, and 7b emerged as the most active members.

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Anticancer and Antioxidant Activity of Novel 5-Substituted- 2-ylidene-1,3-Thiazolidin-4-one Derivatives

Salwa Saleh Abdelwahhab El Sayed

Khaled F. Saieda*, Kamal A. Kandeelb, Salwa S. Abdelwahabc, and Osama M. Ahmedd

1900

Summary Open and heterocyclic active methylene compounds were added to isothiocyanatobenzene, then, cyclized with (Z)-4-aryl-4-oxobut-2-enoic and/or 2-chloro ethanoic acids, giving 5-(2-oxo-2-arylethyl)- and 1,3-thiazolidin-2-yliden-4-ones. Bromination of these two classes of products yielded their (E,Z)- 5-(2-oxo-2- arylethylidene)- and 5-bromo analogues, respectively. A methanolysis process has occurred at the ethyl derivatives, during purification with boiled methanol. On treatment with alkali salts, the 5-bromo derivatives were dimerized, at C-5, but in diluted solutions, it reacted with phenylmethanamine, providing the corresponding 5-benzylamino derivative. Reactions of 4-methoxybenzaldehyde with the 5-unsubstituted-1,3- thiazolidinone products gave their (E,Z) 5-(4-methoxybenzylidene) homologues. Structures of all products were established by spectroscopic data. The tested samples showed interesting anticancer and antioxidant potential.

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