Synthesis of New 2-Thiouracil-5-Sulphonamide Derivatives with Antibacterial and Antifungal Activity

O. A. Fathalla,S. M. Awad,M. S. Mohamed 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.11

2-Thiouracil-5-sulphonic acid N-(4-acetylphenyl) Amide (1) was reacted with a series of aromatic aldehydes giving chalcones 2 (Claisen-Schemidt reaction), some of these chalcones were reacted with urea and thiourea giving pyrimidine-2-one and pyrimidine-2 thione derivatives respectively of the type 3a,b and 4a,b. In addition many chalcones were reacted with hydroxylamine hydrochloride giving isoxazoline derivatives 5a,b. They could also reacted with phenylhydrazine to give pyrazoline derivatives 6a,b, chalcones also were reacted withethylcyano acetate and/or malononitryl in pyridine giving pyran derivatives 7a,c and 8a,c. In another pathway chalcones were epoxidised by H2O2 giving epoxides 9a,c which in turn were reacted with phenylhydrazine giving 4-hydroxypyrazoline derivatives 10a,c. In another reaction chalcones were reacted with ethylcyanoacetate in presence of amm.acetate giving pyridone derivatives 11a,d which could be prepared also in exellent yield from compound 1 by its reaction with certain aromatic aldehydes and ethylcyanoacetate in presence of ammonium acetate. Finally, compound 1 was reacted with semicarbazide giving semicarbazone intermediate 12 which in turn was reacted with thionyl chloride giving thiadiazole derivative 13. The biological effects of some of the new synthesized compounds were also investigated.

Synthesis of New 2-Thiouracil-5-Sulphonamide Derivatives with Antibacterial and Antifungal Activity

Fathalla O. A.,Awad S. M.,Mohamed M. S. The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.11

2-Thiouracil-5-sulphonic acid N-(4-acetylphenyl) Amide (1) was reacted with a series of aromatic aldehydes giving chalcones 2 (Claisen-Schemidt reaction), some of these chalcones were reacted with urea and thiourea giving pyrimidine-2-one and pyrimidine-2 thione derivatives respectively of the type 3a,b and 4a,b. In addition many chalcones were reacted with hydroxylamine hydrochloride giving isoxazoline derivatives 5a,b. They could also reacted with phenylhydrazine to give pyrazoline derivatives 5a,b, chalcones also were reacted withethylcyano acetate and/or malononitryl in pyridine giving pyran derivatives 7a,c and 8a,c. In another pathway chalcones were epoxidised by $H_{2}O_{2}$ giving epoxides 9a,c which in turn were reacted with phenylhydrazine giving 4-hydroxypyrazoline derivatives 10a,c. In another reaction chalcones were reacted with ethylcyanoacetate in presence of amm.acetate giving pyridone derivatives 11a,d which could be prepared also in exellent yield from compound 1 by its reaction with certain aromatic aldehydes and ethylcyanoacetate in presence of ammonium acetate. Finally, compound 1 was reacted with semicarbazide giving semicarbazone intermediate 12 which in turn was reacted with thionyl chloride giving thiadiazole derivative 13. The biological effects of some of the new synthesized compounds were also investigated.

Synthesis of New 2-Thiouracil-5-Sulfonamide Derivatives with Biological Activity

Fathalla, O.A.,Zaghary, W.A.,Radwan, H.H.,Awad, S.M.,Mohamed, M.S. The Pharmaceutical Society of Korea 2002 Archives of Pharmacal Research Vol.25 No.3

2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

Effect of stretching exercises versus autogenic training on preeclampsia

Mohamed A. Awad,Marwa E. Hasanin,Mona Mohamed Taha,Amir A. Gabr 한국운동재활학회 2019 JER Vol.15 No.1

NEW SERIES IDENTITIES FOR ${\frac{1}{\Pi}}$

Awad, Mohammed M.,Mohammed, Asmaa O.,Rakha, Medhat A.,Rathie, Arjun K. Korean Mathematical Society 2017 대한수학회논문집 Vol.32 No.4

In the theory of hypergeometric and generalized hypergeometric series, classical summation theorems have been found interesting applications in obtaining various series identities for ${\Pi}$, ${\Pi}^2$ and ${\frac{1}{\Pi}}$. The aim of this research paper is to provide twelve general formulas for ${\frac{1}{\Pi}}$. On specializing the parameters, a large number of very interesting series identities for ${\frac{1}{\Pi}}$ not previously appeared in the literature have been obtained. Also, several other results for multiples of ${\Pi}$, ${\Pi}^2$, ${\frac{1}{{\Pi}^2}}$, ${\frac{1}{{\Pi}^3}}$ and ${\frac{1}{\sqrt{\Pi}}}$ have been obtained. The results are established with the help of the extensions of classical Gauss's summation theorem available in the literature.

ON AN INTERESTING EXTENSION OF KUMMER'S SECOND THEOREM WITH APPLICATIONS

Awad, Mohammed M.,Mohammed, Asmaa O.,Rakha, Medhat A.,Rathie, Arjun K. Korean Mathematical Society 2021 대한수학회논문집 Vol.36 No.1

In this research paper, an attempt has been made to provide an interesting extension of the well-known and useful Kummer's second theorem. Several applications have also been given.

Potentiometric determination of iron in polluted water samples using new modified Fe(III)-screen printed ion selective electrode

Tamer Awad Ali,Ahmed A. Farag,Gehad G. Mohamed 한국공업화학회 2014 Journal of Industrial and Engineering Chemistry Vol.20 No.4

This article is focused on the determination of Fe(III) ion as an important factor in water pollution. A potentiometric method based on screen-printed ion-selective electrode was described for the determination of Fe(III) ion in different polluted water samples. It is based on incorporation of the Fe-phosphotungstate ion-associate in a screen-printed electrode (SPE) composition and tricresylpho-sphate (TCP) as plasticizer. The influences of the paste composition, different conditioning parameters and foreign ions on the electrode performance were investigated. The reversibility and also response time of the electrode have been studied. The electrode showed Nernstian response of 19.20 ± 0.73 mV decade-1 in the concentration range of 1 × 10-7–2.5 × 10-2 mol L-1. The electrode was found to be usable within the pH range of 3–7.5 and exhibited a fast response time (about 7 s), low detection limit (1.57 × 10-7 mol L-1), long lifetime (>6 months) and good stability. The isothermal temperature coefficient (dE0/dt) of the electrode was calculated. The electrode was successfully applied for the determination of Fe(III) ion in pure solutions and polluted water samples (formation, tab and sea water samples) using potentiometric determination technique. The results obtained applying this potentiometric electrode is comparable with those obtained using inductive coupled plasma technique.

Transepithelial Laser versus Alcohol Assisted Photorefractive Keratectomy Safety and Efficacy: 1-Year Follow-up of a Contralateral Eye Study

Hesham Mohamed Gharieb,Mo’mena Ahmad A Awad-Allah,Anas Adel Ahmed,Ihab Saad Othman 대한안과학회 2021 Korean Journal of Ophthalmology Vol.35 No.2

Purpose: To compare single-step transepithelial photorefractive keratectomy (TPRK) to conventional alcohol assisted epithelialremoval then photorefractive keratectomy (AAPRK) regarding pain, epithelial healing, visual acuity, corneal haze measuredsubjectively and objectively, higher order aberrations changes, contrast sensitivity and vector analysis of astigmatic correctionwith one year follow-up. Methods: A prospective double-blind randomized study of 29 subjects (58 eyes) who underwent myopic aberration-freelaser correction by smart pulse technology using Schwind Amaris 1050 Hz with 1-year follow-up. Right eye was randomlytreated by AAPRK or TPRK. Postoperative assessment was performed on day 1 and 3, at 1st week, and 1st, 3rd, 6th, and 12thmonths. Patients were assessed for pain, epithelial healing, visual acuity, corneal haze, astigmatic correction, higher order aberrationsand contrast sensitivity. Results: Epithelial healing was complete by the 3rd day in 62.1% of AAPRK eyes and in 89.7% of TPRK eyes. First day postoperativepain was higher in TPRK group (p = 0.0134). The decimal uncorrected visual acuity at 12 months was 1.47 ± 0.39 and1.57 ± 0.38 in the AAPRK and TPRK groups respectively (p = 0.3719). Post-photorefractive keratectomy haze reached a finallevel of 0.04 ± 0.14 and 0.02 ± 0.1 in AAPRK and TPRK groups respectively (p = 0.5607). Contrast sensitivity was comparable inlow and high frequency cycles per degree. Vector analysis of astigmatic correction showed correction index at one year of 0.99and 1.05 for AAPRK and TPRK groups respectively. Conclusions: Alcohol assisted and transepithelial photorefractive keratectomy have comparable results regarding safety andefficacy.

Synthesis of New 2-Thiouracil-5-Sulfonamide Derivatives with Biological Activity

O.A.Fathalla,W.A.Zaghary,H.H.Radwan,S.M.Awad,M.S.Mohamed 대한약학회 2002 Archives of Pharmacal Research Vol.25 No.3

Graviola leaves extract enhances the anticancer effect of cisplatin on various cancer cell lines

Mai G. Awad,Ramadan A. Ali,Dalia D. Abd El‑Monem,Mohammed A. El‑Magd 대한독성 유전단백체 학회 2020 Molecular & cellular toxicology Vol.16 No.4

Background Cisplatin (CIS) is widely applied as an anticancer drug for various cancer types, including liver, breast, colorectal, and pancreatic cancers; however, its usage is limited due to side efects. Objective We investigated whether combined therapy of Graviola (Annona muricata) leaves extract (GLE) and CIS could reduce CIS doses without decreasing its anticancer potential. Methods The MCF7, HepG2, CaCo2, or PANC1 cells were divided into four groups for each cell line as follows: group1 (G1): untreated cells, G2: cells treated with GLE, G3: cells treated with CIS, and G4: cells treated with GLE, after 2 h treated with CIS. All combinations were prepared as non-constant ratio from GLE. The cytotoxicity, gene expression, cell cycle arrest were determined by MTT assay, real-time PCR, and cell fow cytometry, respectively. Results Treatment with GLE and/or CIS-induced cytotoxic efect on HepG2, MCF7, CaCo2, and PANC1 cancer cells with the best efect of combined therapy. All twelve non-constant ratio combinations (GLE+CIS) for each cell line resulted in a signifcant higher cytotoxic efect than single drug treatment. The combination index (CI) values for all combinations were less than one, indicating the presence of synergistic cytotoxic efect between CIS and GLE against the four cancer cell lines. This anticancer efect was triggered through mitochondrial-dependent apoptosis with the downregulation of caspase3, Bax, and p53 and upregulation of Bcl2. GLE also shifted G0/G1 phase of cell cycle arrest induced by CIS to S and G2/M phases. Interestingly, this combined therapy did not afect oxidative stress (indicated by higher malondialdehyde level and lower activities of SOD, CAT, and GPX) induced by CIS; however, it downregulated the expression of MAPK1 and multidrug resistance gene MDR1.