DNA Binding, Antiviral Activities and Cytotoxicity of New Furochromone and Benzofuran Derivatives

Omaima Mohamed Abdelhafez,Nehad Ahmed Abedelatif,Farid A. Badria 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.10

Bromination of visnagin (1) afforded 9-bromovisnagin (2) which on its alkaline hydrolysis afforded the 3-acetyl benzofuran derivative (3). The condensation of (3) with hydrazine hydrate, phenylhydrazine and/or hydroxylamine hydrochloride afforded the corresponding pyrazole derivatives (4a, b) and isoxazole derivative (4c). On the other hand, when compound 3 was condensed with some aromatic aldehydes, this yielded corresponding α, β-unsaturated keto derivatives (5a-e). Furthermore, when 1 was subjected to chlorosulfonation, the visnaginsulfonylchloride derivative 6 was afforded, which on amidation using morpholine, a sulonamido derivative (7) was obtained. Alkaline hydrolysis of the latter compound yielded 7-N-morpholinosulsamidobenzofuran (8) which was condensed with some aromatic aldehydes to yield the corresponding chalcone compounds (9a-e). Demethylation of visnagin afforded norvisnagin (10). The reaction of 10 with ethylbromoacetate in dry acetone yielded the ester benzopyran derivative (11) which reacted with hydrazine hydrate to afford the corresponding hydrazide derivative (12) and this was condensed with 3,4,5-trimethoxybenzaldehyde to give the corresponding hydrazone (13). A thaizolidinone derivative (14) was obtained by condensation of (13) with thioglycolic acid. Chloromethylation of norvisnagin afforded a 4-chloromethyl derivative (15) which reacted with different primary and secondary amines to yield the corresponding ethylamino derivative (16a, b). Moreover, mannich bases (16a, b) and (17a-c) were obtained by reacting norvisnagin with different primary and secondary amines in the presence of formalin but benzoylation of (16a, b) and (17a-c) afforded 4-oxybenzoyl derivative (18a-e). The prepared compounds were tested for their interaction with DNA; bromovisnagin 2 showed the highest affinity and compounds 6, 15, 8a, > 14, > 16b, 17a, and 16a showed moderate activity in decreasing potency. Moreover, compound 2 also was the most active as antiviral agent toward HS-I virus and compounds 6, 7, 15, 14, 16a, and 18a were found to be moderately active. CD50 of the active compounds were also measured.

Dose metrology: TLD/OSL dose accuracy and energy response performance

Belhaj Omaima Essaad,Boukhal Hamid,Chakir El Mahjoub,Bellahsaouia Meryeme,Belhaj Siham,Sadeq Younes,Tazi Mohammed,El Khoukhi Tahar,Hadouachi Maryam,Laazouzi Khaoula 한국원자력학회 2023 Nuclear Engineering and Technology Vol.55 No.2

An essential step in evaluating and comparing the performance of two passive radiation dosimeter types, thermosluminescent (TLD) and optically stimulated luminescence (OSL), used by workers in environments with ionizing radiation for individual radiological monitoring and control of external exposure at various times (cumulative dose for 1 month), is to compare the measured dose accuracy, energy response, and coefficient of variation. In fact this performance study consists in determining the accuracy of both R(10) and R(0.07) which are considered as the ratios of the measured dose (Hp(10) or Hp(0.07)) to the delivered dose (Hp(10) or Hp(0.07)) for each photon energy. The validity of the results of this test is based on the acceptance limits of the ICRP and the international standard IEC-62387. The relative energy response used is normalized to the 137Cs 662 keV energy to find which energy response is closest to the ideal case, and the coefficient of variation that allows to determine the statistical fluctuation of the Hp(10) and Hp(0.07) doses. The results of the accuracy test for the OSL and TLD dosimeters are acceptable because they fall within the ICRP limits. For the energy response, the OSL performs better than the TLD for Hp(10) and Hp(0.07), and for the coefficient of variation, the OSL satisfies the requirements of ISO 62387 for both Hp(10) and Hp(0.07), while the TLD satisfies these requirements only for the measurement of Hp (0.07).

Synthesis and Biological Investigations of New Thiazolidinone and Oxadiazoline Coumarin Derivatives

Abd Elhafez, Omaima Mohamed,El Khrisy, Ezz El Din Ahmed Mohamed,Badria, Farid,Fathy, Alaa El Din Mohamed The Pharmaceutical Society of Korea 2003 Archives of Pharmacal Research Vol.26 No.9

Ethyl (coumarin-4-oxy)acetate 1 was prepared through the reaction of 4-hydroxycoumarin with ethyl bromoacetate. Compound 1 was allowed to react with hydrazine hydrate to produce coumarin-4-oxyacetic hydrazide 2. The synthesis of N-(arylidene and alkylidene)-coumarin-4-oxyacetic hydrazones 3-20 was performed. The preparation of 2-substituted-3-[(coumarin-4-oxy) acetamido]thiazolidinones 21-26 and 2-[(coumarin-4-oxy )methyl]-4-acetyl-5-substituted-$\Delta^2$-1,3,4-oxadiazolines 27-33 was performed by the reaction of the hydrazones 3, 4, 7, 9, 12, 14 with mercaptoacetic acid and the hydrazones 3, 4, 5, 7, 12, 15, 16 with acetic anhydride, respectively. The antiviral activities, cytotoxicities and structure-activity relationship (SAR) towards different microorganisms of the prepared compounds were studied.

Optimization for glimepiride dissolution enhancement utilizing different carriers and techniques

Rana R. Makar,Randa Latif,Ehab A. Hosni,Omaima N. El Gazayerly 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.2

The present work is a comparative study that matches between carriers and techniques used to prepare solid mixtures with glimepiride. The study is directed towards elucidation of the most promising carrier capable of highly improving drug dissolution along with the most successful technique used for drug formulation. Mixtures were tested for drug content and dissolution. The most optimum formulae were characterized by DSC, IR and XRPD. Kinetic treatment of dissolution data was performed for physical and co-ground mixtures, solid dispersions and their adsorbates, triple solid dispersions and their adsorbates, microwave generated or treated solid dispersions. Results revealed that enhancing effectmostly reached maximum with ternary solid dispersion adsorbate (TSDads). The latter technique demonstrated a dramatic increase in drug dissolution rate which was reflected in the shortest half-life for most carriers at variable degrees. The highest dissolution rate was attained with pregelatinized starch and decreased to variable degrees with remaining carriers. Differences were ascribed to chemical nature as well as relative water solubility of carriers. The combined effects of incorporating surfactants, polymers and adsorbents to glimepiride contributed together to improve wetting, reduce crystallinity and caused substantial increase in the surface area which made TSDads the most promising technique for enhancing dissolution of glimepiride.

Attempts to enhance the anti-cancer activity of curcumin as a magical oncological agent using transdermal delivery

Abdel-Hafez Salma M.,Hathout Rania M.,Sammour Omaima A. 경희대학교 융합한의과학연구소 2021 Oriental Pharmacy and Experimental Medicine Vol.21 No.1

For the past few years, curcumin has drawn the attention of scientists in multidisciplinary fields related to oncology and therapeutics. However, despite its high potency, its delivery suffers from several limitations and challenges that hinders the complete benefit from this magical molecule. Accordingly, this review demonstrates the several attempts and endeavors that the scientists exerted in order to delivery this molecule successfully through the transdermal route. We believe that the transdermal route of delivery of drugs can pose a new platform of targeting solid tumors such as the breast carcinoma so that applying a transdermal patch over the skin or the membrane covering the solid tumor can provide a means of the cure.

Towards the production of monodisperse gelatin nanoparticles by modified one step desolvation technique

Khaled S. Shamarekh,Heba A. Gad,Mahmoud E. Soliman,Omaima A. Sammour 한국약제학회 2020 Journal of Pharmaceutical Investigation Vol.50 No.2

Purpose The aim of the present study was to prepare gelatin nanoparticles (GNPs) using modified one step desolvation method to obtain small, uniformly sized, and spherical GNPs. Methods The modifications involved the preparation of high molecular weight gelatin (HMWG) by fractionation of gelatin. HMWG was freeze-dried to be used in a specified concentration for preparation of GNPs with controllable properties. Furthermore, HMWG was cationized by dissolving it in acidified deionized water at pH value less than its isoelectric point. Factorial design analysis was utilized to investigate the effect of different preparation variables (viz. HMWG concentration, pH and ratio of HMWG solution volume to non-solvent volume) on particle size, polydispersity index (PDI), zeta potential and yield of GNPs. Results Results revealed the formation of monodisperse GNPs with small particle size, low PDI values (< 0.2) and high yield. FT-IR spectroscopy and differential scanning calorimetry studies revealed that the conformational structure of HMWG chains was altered within GNPs matrices. Conclusion The suggested modifications introduced on the one-step desolvation method enable to prepare successfully monodispersed GNPs with narrow size distribution and high particle yield.

Protein Hydrolysate from Underutilized Legumes: Unleashing the Potential for Future Functional Foods

Ain Tasnim Azman,Nur Suaidah Mohd Isa,Zamzahaila Mohd Zin,Mohd Aidil Adhha Abdullah,Omaima Aidat,Mohamad Khairi Zainol 한국식품영양과학회 2023 Preventive Nutrition and Food Science Vol.28 No.3

Proteins play a vital role in human development, growth, and overall health. Traditionally, animal-derived proteins were considered the primary source of dietary protein. However, in recent years, there has been a remarkable shift in dietary consumption patterns, with a growing preference for plant-based protein sources. This shift has resulted in a significant increase in the production of plant proteins in the food sector. Consequently, there has been a surge in research exploring various plant sources, particularly wild, and underutilized legumes such as Canavalia, Psophocarpus, Cajanus, Lablab, Phaseolus, and Vigna, due to their exceptional nutraceutical value. This review presents the latest insights into innovative approaches used to extract proteins from underutilized legumes. Furthermore, it highlights the purification of protein hydrolysate using Fast Protein Liquid Chromatography. This review also covers the characterization of purified peptides, including their molecular weight, amino acid composition, and the creation of three-dimensional models based on amino acid sequences. The potential of underutilized legume protein hydrolysates as functional ingredients in the food industry is a key focus of this review. By incorporating these protein sources into food production, we can foster sustainable and healthy practices while minimizing environmental impact. The investigation of underutilized legumes offers exciting possibilities for future research and development in this area, further enhancing the utilization of plant-based protein sources.

Synthesis of Thiazolo[4,5-d]pyrimidine Derivatives as Potential Antimicrobial Agents

Habib, Nargues S.,Soliman, Raafat,El-Tombary, Alaa A.,El-Hawash, Soad A.,Shaaban, Omaima G. 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12

In this study, we report the synthesis and antimicrobial evaluation of several new thiazolo[4,5-d]pyrimidine derivatives, namely 7-substituted amino-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 4a-e, 8, 13, 15, ethyl 2-cyano-2-(7-substituted-5-methyl-3-phenylthiazolo [4,5-d]-pyrimidin-2(3H)-ylidene)acetates 5a-b, 2-(7 -substituted-5-methyl-3-phenylthiazolo[4,5-d]pyrimidin-2(3H)-ylidene)malononitriles 6a-b, 5-methyl-7-morpholino-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-one 7, and 7-[4-(1-substituted-5-phenyl-4,5-dihydro-1H-pyrazolin-3-yl)anilino]-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E. coli and P. aeruginosa, and all were inactive against S. aureus.

Synthesis of Thiazolo[4,5-d]pyrimidine Derivatives as Potential Antimicrobial Agents

Nargues S. Habib,Raafat Soliman,Alaa A. El-Tombary,Soad A. El-Hawash,Omaima G. Shaaban 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12

In this study, we report the synthesis and antimicrobial evaluation of several new thiazolo[4,5- d]pyrimidine derivatives, namely 7-substituted amino-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine- 2(3H)-thiones 4a-e, 8, 13, 15, ethyl 2-cyano-2-(7-substituted-5-methyl-3-phenylthiazolo [4,5-d]-pyrimidin-2(3H)-ylidene)acetates 5a-b, 2-(7-substituted-5-methyl-3-phenylthiazolo[4,5- d]pyrimidin-2(3H)-ylidene)malononitriles 6a-b, 5-methyl-7-morpholino-3-phenylthiazolo[4,5-d] pyrimidine-2(3H)-one 7, and 7-[4-(1-substituted-5-phenyl-4,5-dihydro-1H-pyrazolin-3-yl)anilino]-5- methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E. coli and P. aeruginosa, and all were inactive against S. aureus.