Synthesis of New Uraci1-5-Sulphonamide-p-Phenyl Derivatives and Their Effect on Biomphalaria alexandrina Snail's Nucleoproteins

Fathalla, O.A.,Gad, H.S.M.,Maghaby, A.S. The Pharmaceutical Society of Korea 2000 Archives of Pharmacal Research Vol.23 No.2

In continuation of the previous work (Fathalla, 1992) on the synthesis of some heterocycles containing uracil moiety, we report herein the incorporation of uracil moiety into cyan-opyridine thione, thiosemecarbazone, semicarbazone, cyanopyridine, ami nocyano pyridine, isoxazoline, pyrazoline, pyrimidine, triazolo pyrimidine, pyran, selena and thiazole derivatives which might modify their biological activities. The biological studies revealed that the chemical compound III f showed high molluscicdal activity than other compounds. The profile of the nucleoprotein extracted from chemically (compound IIIc, e, f and g) treated or UV-irradiated B.alexandrina snails did not show appreciable differences when compared to non-treated (native) snails by using SDS-PAGE, where no obvious qualitative or quantitative differences were observed. Immunization of experimental animals with the nucleoprotein extracted from native, chemically (compound III f & g) treated or physically treated B.alexandrina snails induced significant protection against challenge with normal S.mansoni cercariae, as compared to the non-immunized challenged control. As well as , a decrease in the number of granuloma formation and the size range of granuloma was also observed in immunized animals. It is concluded that, compounds III f and g have a potent molluscicidal activity. They also induced chemical modification comparable to that induced by physical treatment in the snail's nucleoprotein, which could possibly be used in immunization against S. mansoni infection.

Synthesis of New Uracil-5-Sulfonamide Derivatives and Immuno-Stimulatory Effect of a Chemically Modified Hemolymph of Biomphalaria alexandrina on Schistosoma mansoni Infected Mice

Fathalla, O.A.,Haiba, M.E.,Maghraby, A.S. The Pharmaceutical Society of Korea 2003 Archives of Pharmacal Research Vol.26 No.5

Some N-p-substituted phenyl uracil-5-sulphonamide derivatives have been synthesized to be evaluated as molluscicides against Biomphalaria alexandrina snails, the intermediate host of Schistosoma mansoni. Schistosoma mansoni infected mice were treated with hemolymph obtained from pre-treated Biomphalaria alexandrina snails with the products 4a, 10a, 10b and 4b or obtained from non-treated snails. The selection of the concentration based on the predetermined dose which caused mortality of less than 50% of snails/24 h. $LC_{50}$ of compounds 4a, 10a, 10b and 4b was 50, 100, 200 and 50 ppm respectively. The result showed that immuno-stimulatory effect of treated hemolymph with compounds 4a, 10a and 4b was related to significant protective effects (44.4, 34.6 and 50.4% reduction in worm burden respectively). In addition, mean total worm burdens were significantly reduced in non treated hemolymph by 33.8%. The effect of hemolymph obtained from treated or non treated snails on S. mansoni adult worms antigens was studied by indirect immunofluorescence technique using chronic mouse sera (CMS). The results indicated that there was a strong reaction with epitopes in gut epithelium, tubercles, teigument and subtegumental musculature of untreated and treated S. mansoni adult worms antigens. Therefore, treatment of hemolymph obtained from pre-treated snails with compounds 4a, 10a, and 4b can stimulate specific immune response and induce protective effects against S. mansoni infection.

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.

Extent of Hyperostotic Bone Resection in Convexity Meningioma to Achieve Pathologically Free Margins

Fathalla, Hussein,Tawab, Mohamed Gaber Abdel,El-Fiki, Ahmed The Korean Neurosurgical Society 2020 Journal of Korean neurosurgical society Vol.63 No.6

Objective : Hyperostosis in meningiomas can be present in 4.5% to 44% of cases. Radical resection should include aggressive removal of invaded bone. It is not clear however to what extent bone removal should be carried to achieve pathologically free margins, especially that in many cases, there is a T2 hyperintense signal that extends beyond the hyperostotic bone. In this study we try to investigate the perimeter of tumour cells outside the visible nidus of hyperostotic bone and to what extent they are present outside this nidus. This would serve as an initial step for setting guidelines on dealing with hyperostosis in meningioma surgery. Methods : This is a prospective case series that included 14 patients with convexity meningiomas and hyperostosis during the period from March 2017 to August 2018 in two university hospitals. Patients demographics, clinical, imaging characteristics, intraoperative and postoperative data were collected and analysed. In all cases, all visible abnormal bone was excised bearing in mind to also include the hyperintense diploe in magnetic resonance imaging (MRI) T2 weighted images after careful preoperative assessment. To examine bony tumour invasion, five marked bone biopsies were taken from the craniotomy flap for histopathological examinations. These include one from the centre of hyperostotic nidus and the other four from the corners at a 2-cm distance from the margin of the nidus. Results : Our study included five males (35.7%) and nine females (64.3%) with a mean age of 43.75 years (33-55). Tumor site was parietal in seven cases (50%), fronto-parietal in three cases (21.4%), parieto-occipital in two cases (14.2%), frontal region in one case and bicoronal (midline) in one case. Tumour pathology revealed a World Health Organization (WHO) grade I in seven cases (50%), atypical meningioma (WHO II) in five cases (35.7%) and anaplastic meningioma (WHO III) in two cases (14.2%). In all grade I and II meningiomas, bone biopsies harvested from the nidus revealed infiltration with tumour cells while all other bone biopsies from the four corners (2 cm from nidus) were free. In cases of anaplastic meningiomas, all five biopsies were positive for tumour cells. Conclusion : Removal of the gross epicentre of hyperostotic bone with the surrounding 2 cm is adequate to ensure radical excision and free bone margins in grade I and II meningiomas. Hyperintense signal change in MRI T2 weighted images, even beyond visible hypersototic areas, doesn't necessarily represent tumour invasion.

Synthesis, CO2 Adsorption and Catalytic Properties of Porphyrin- Pyromellitic Dianhydride Based Porous Polymers

Maher Fathalla 한국고분자학회 2021 Macromolecular Research Vol.29 No.4

The synthesis, characterization and CO2 uptake tendency of a new porous organic polymer (POP) based on porphyrin-pyromellitic dianhyderide is enclosed. The reported porphyrin POP was achieved by exploiting the condensation reaction between tetraaminophenylporphyrin (TAPP) with benzenetetracarboxylic (pyromellitic) diahhydride in dry dimethylforamide (DMF). The structure of the resulting polymer was confirmed by FT-IR as well as solid state 13C cross-polarization magic angle spinning (CP/MAS) NMR studies. In addition, the post-synthetic metallation of the free-base porphyrin macrocycles of the resulting POP with either Zn or Mn metals afforded the metallo-porphyrin POP analogues in excellent yields. The morphology of the reported porphyrin POPs were investigated by scanning electron microscopy (SEM) which demonstrated the porosity of the resulting POPs. Furthermore, CO2 adsorption capabilities of the synthesized POPs were evaluated and Brunauer-Emmett-Teller (BET) surface area was found to be 542, 597 and 828 m2/g for free-base, Zn- and MnIII-POP, respectively. Finally, MnIII-POP was found to be an effective catalyst for the selective epoxidation of styrene to the corresponding epoxide.

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-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

Protective effect of dates (Phoenix dactylifera L.) and licorice (Glycyrrhiza glabra) on carbon tetrachloride–induced hepatotoxicity in dogs

Abdelrahman Hassan Abdelrahman,Fathalla Said Ibrahim,Ashraf Abdelrahman,Jun HK,Kim DH 한국식품영양과학회 2015 한국식품영양과학회 학술대회발표집 Vol.2015 No.8

Effect of turmeric (Curcuma Longa), fenugreek (Trigonella foenum-graecum L.) and/or bioflavonoid supplementation to the broiler chicks diet and drinking water on the growth performanceand intestinal morphometeric parameters

Hassan Abdel-Rahman Abdel-Rahm,Said Ibrahim Fathalla,Mohamed Atef Helal,Abeer Abdel-aleem Nafeaa,Ibrahim Selim Zahran 한국식품영양과학회 2015 한국식품영양과학회 학술대회발표집 Vol.2015 No.8