2024-03-28T13:14:42Z
https://bpsa.journals.ekb.eg/?_action=export&rf=summon&issue=9815
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS OF SOME THIAZOLIDINE DERIVATIVES OF 1,4-BENZOQUINONE AS POTENTIAL ANTIMICROBIAL AGENTS
I.
Chaaban
A.
Bekhit
Elsayed
Aboulmagd
A series of 2,5-disubstituted-1,4-benzoquinone derivatives were synthesized and evaluated for their antimicrobial activity. Coupling of 2,5-dihydroxybenzoic acid (gentisic acid) with the selected thiazolidine derivative using EDC and HOBt afforded the corresponding (4R)-3-(2,5dihydroxybenzoyl)-5,5-dimethyl-N-substituted benzylthiazolidine-4-carboxamide 2a-d. These compounds were subsequently oxidized with ferric chloride to afford the corresponding 1,4benzoquinones 3a-d. The reaction between 1,4-benzoquinone derivatives and the appropriate amine resulted in the targeted 2,5-disubstituted-1,4-benzoquinone derivatives 4a-l. The structure of the newly synthesized compound were confirmed by elemental microanalyses, IR and 1H NMR spectra. The antimicrobial activity of target compounds 4a-l was performed against Escherichia coli (E. coli) ATCC 25922 as Gram-negative bacteria, Staphylococcus aureus (S. aureus) ATCC 19433 as Gram-positive bacteria and Candida albicans (C. albicans) as yeast like fungi were determined
2005
06
30
1
7
https://bpsa.journals.ekb.eg/article_64882_abc3ee9c53778c085bdfabb6a6d8967a.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME 3,5DISUBSTITUTED-TETRAHYDRO-2H-1,3,5-THIADIAZINE-2-THIONE DERIVATIVES
Samia
Abdel Moty
Twelve new 3-(isobutyl)-5-substituted-tetrahydro-2H-1,3,5-thiadiaz- ine-2-thiones were synthesized by the reaction of isobutylamine with carbon disulfide and potassium hydroxide, followed by formaldehyde and appropriate alkyl, cycloalkyl aralkyl amines, amino acid, and INH. Their structures have been elucidated by spectral data and elemental analysis. The title compounds were tested for antimicrobial activity in vitro against gram-positive bacteria (Staphylococcus aureus,and Micrococcus leuteus), gram-negative bacteria (Serratia marcescens and Escherichia coli) and some fungi (Candida albicans, Scopulariopsis brevicalus, Geotrichum candidum, Macrophomina phaseolina, Fusarium oxysporum and Trichoderma harzianum) using agar cup diffusion method. The antimicrobial activity was found to be greatly affected by the bulkiness of the side chain and the presence of polar carboxylic group. Highest activity was obtained with compounds 4a and 4k (R= CH3, CH2-COOH).
2005
06
30
9
15
https://bpsa.journals.ekb.eg/article_64884_798dcfb799a76fea9307618e0f556e2c.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS OF SOME PYRIMIDINE DERIVATIVES OF EXPECTED BIOLOGICAL ACTIVITIES
Wafaa
Zaghary
Aida
El-Azzouny
Mohammed
Motaleb
Mohammed
Kedr
A series of 4-substituted pyrimidines and fused pyrimidine ring system e.g. pyrido[2,3-d] pyrimidine were synthesized and the antitumor activity have been carried out for 8 compounds. Compound 4a also, which carries the pharmacophoric group IDA was tested for the hepatobilliary imaging effect.
2005
06
30
17
25
https://bpsa.journals.ekb.eg/article_64886_731956fe6fd4d12fed7fd24b81f394b5.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS OF SOME NEW 1,4-DISUBSTITUTED PIPERAZINE-2,3- DIONE DERIVATIVES OF POTENTIAL ANTHELMINTIC ACTIVITY
Mostafa
Hussein
Ahmed
Diab
The purpose of this study based upon design and synthesis of a new series of 1,4-
disubstituted piperazine-2,3-dione derivatives through two steps reaction. This protocol
involves the formation of N,N\-Bis-(4-substituted benzyl)-ethane-1,2-diamine and N,N\-Bis-[1-
(4-substituted phenyl)-ethyl]-ethane-1,2-diamine derivatives (1a-i) through reductive alkylation
reaction from ethylenediamine and different carbonyl compounds in the presence of sodium
cyanoborohydride. The second step involves reaction of compounds (1a-i) with diethyl oxalate
affording the target compounds. Consequently, nine new 1,4-disubstituted piperazine-2,3-dione
derivatives were synthesized as the target compounds, 1,4-Bis-(4-substituted benzyl)-
piperazine-2,3-dione and 1,4-Bis-[1-(4-substituted phenyl)-ethyl]-piperazine-2,3-dione
derivatives (2a-i). The structures of the target compounds were elucidated depending upon the
data of the different spectral as well as the elemental methods of analyses. In addition, a mass
spectrum, for a representative example, was carried out where the expected fragmentation
pattern is in accordance with the structure of the considered compound. The lipophilicity of the
target compounds as expressed from the ClogP and the measured R f remarkably supercede that
of piperazine. The preliminary anthelmintic activity of the newly synthesized derivatives (2a-i)
was investigated in vitro against Enterobiuos vermicularis and Fasciola hepatica. The tested
compounds exhibited, in all cases, considerable inhibitory effects on the growth of the tested
parasites in comparison with piperazine hydrate as a reference drug.
2005
06
01
37
44
https://bpsa.journals.ekb.eg/article_64993_bdf855ffe96e110e9bfb9e91c9c6199d.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS OF SOME POTENTIAL ANTIESTROGENIC AGENTS
Hany
Safwat
Gehan
Hegazy
Ghaneya
Hassan
Some novel steroidal arylidene derivatives were synthesized and representative examples were tested for their antiestrogenic activity. The active compounds were subjected for antitumor activity screening. The compounds tested displayed aromatase inhibitory activity as shown by decrease in estradiol and increase in testosterone levels. Further, some compounds were tested for androgenic/anabolic activity. The steroids used for preparation of these arylidene derivatives are the clinically applied: levo-Norgestrel, Testosterone, Mesterolone and Norethisterone.
2005
06
30
27
35
https://bpsa.journals.ekb.eg/article_65181_da0c206a4077126abdb4c6b121a75a65.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 1,3-DISUBSTITUTED 2,4(1H,3H)QUINAZOLINEDIONE
Abdel
El-Helby
Some new 2,4(1H,3H)-quinazolinedione were synthesized and characterized by elemental analysis, IR, 1HNMR and Ms spectral data. Pharmacological evaluation of some of the synthesized compounds as anticonvulsants showed that they displayed weak anticonvulsant activity relative to phenobarbitone sodium as reference drug.
2005
06
30
45
56
https://bpsa.journals.ekb.eg/article_65182_b8ad1f33ce0d19c654d64137f77b949c.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS AND ANTIHYPERLIPIDEMIC ACTIVITY OF CERTAIN NICOTINIC ACID DERIVATIVES
Abdel Ghany
El-Helby
Mohamed
Abdel-Wahab
3-Ethoxycarbonyl-4,6-dimethyl-2(1H)-pyridone I was prepared and converted to the corresponding sodium salt II. The latter reacted with certain chloroacetanilides to afford the corresponding ethers III. In addition 3-cyano-4,6-dimethyl-2(1H)-pyridone IV was prepared and converted to the corresponding potassium salt V which was allowed to react with chloroacetyl and -chloropropionyl derivatives of certain aromatic amines to afford VI. Furthermore, IV was converted to 3-cyano-4,6-dimethyl pyridine-2-thione IX. Potassium salt of the latter upon reaction with -chloroacetyl and -chloropropionyl derivatives of some aromatic amines gave the expected thioethers X. Compounds III2, V4, X1 and X12 were selected for testing for antihyperlipidemic effect and revealed promising hypolipidemic effect on cholesterol, triglyceride, LDL and have no effect on HDL.
2005
06
30
57
69
https://bpsa.journals.ekb.eg/article_65233_6fc7d20ae91f41c32fd7bf4e7c4399a4.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
CHEMICAL CONSTITUENTS OF GLADIOLUS SEGETUM KER-GAWL
Khaled
Mohamed
From the chloroform soluble fraction of the methanolic extract of the corms of Gladiolus segetum Ker-Gawl (Iridaceae), nine compounds were isolated and identified as follows: the lignans (+)-demethoxypinoresinol (1), (+)-pinoresinol (2) and (+)-pinoresinol monomethylether (3); the neolignan (–)-dehydrodiconiferyl alcohol (4) and the anthraquinones deoxyerythrolaccin (5), physcion (6) and laccaic acid D methylester (7) together with 6′-O-palmitoyl3-O -sitosterol glucoside (8) and -sitosterol-3-O-glucoside (9). The structures of the isolated compounds were determined by physical and spectroscopic methods including NMR and MS spectral analysis. Compounds 1-4 and 6-9 are reported here for the first time from the genus Gladiolus while compound 5 was previously isolated from the same plant.
2005
06
30
71
78
https://bpsa.journals.ekb.eg/article_65234_8422027548a53768a8010f235733a093.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS OF SOME QUINOLINE THIOSEMICARBAZONE DERIVATIVES OF POTENTIAL ANTIMICROBIAL ACTIVITY
Samia
Abdel-Moty
Mostafa
Abdel-Rahman
Hosney
Elsherief
Abdel-Hamid
Kafafy
5-Acetyl (or 5-benzoyl)-8-hydroxyquinoline-4-substituted thiosemi- carbazones (IIa-m, IIIa-m respectively) have been prepared via the condensation of 5-acetyl (or 5-benzoyl)-8hydroxyquinoline with the appropriate 4-substituted-3-thiosemicabazides (Ia-l). The thiosemicarbazones (IIa-l, IIIa-f) were subjected to cyclization into the corresponding thiazolidinones (IVa-l, Va-f) by the reaction with ethyl bromoacetate in the presence of anhydrous sodium acetate. The structures of the thiosemicarbazones as well as the corresponding thiazolidinones were assigned based on both elemental and spectroscopic evidences. The prepared compounds were also evaluated for antibacterial and antifungal activities.
2005
06
30
79
93
https://bpsa.journals.ekb.eg/article_65235_5f1fa035682f622735e8ca5e9ef3e547.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
ALLOPHENYLNORSTATINE-CONTAINING HIV-1 PROTEASE INHIBITORS: DESIGN, SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS FOR SELECTED P2 LIGANDS
Hamdy
Abdel-Rahman
Nawal
El-Koussi
Gamal
Alkaramany
Adel
Youssef
Yoshiaki
Kiso
The design and development of potent HIV protease inhibitors remain an attractive target for antiviral therapy. A novel class of HIV protease inhibitors containing allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid] as a transition state mimic have been reported. In this work we fixed P2` (as tert-butylamino or 2-methylbenzylamino) and changed P2 moiety to provide two series of dipeptide analogs. Preliminary evaluation of the activity of the synthesized derivatives were determined as percentage of enzyme inhibition at 5 M level. The results showed that the introduction of 2-methylbenzylamino moiety as P2` ligand 6a-e considerably improved HIV inhibitory activity in comparison with the tert-butyl amino analogs 5a-e. It was found that compounds in both series retained activity still less than the lead compounds KNI-577 and KNI-727.
2005
06
30
95
103
https://bpsa.journals.ekb.eg/article_65236_06c1f7613d68416bccd67a4860b18a00.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
BIOTRANSFORMATION OF FLAVONOLS TO FLAVONOLS-3-OGLUCOSIDE IN CELL CULTURES OF ASTRAGALUS SIEBERI DC.
A.
Abd El-Mawla
Zedan
Ibraheim
One distinct glucosyltransferase (GT) has been partially purified and characterized from cell cultures of Astragalus sieberi DC.; Family Leguminosae. Callus cultures were established from shoots of sterile germinated seeds maintained on solid MS medium supplemented with 4.5 M 1-naphthylacetic acid (NAA) and 2.3 M kinetin (KIN). The cell suspension cultures were obtained by transport of callus cultures to liquid MS medium with the same hormone supplementation. The GT was found to exhibit maximum activity at pH 7.5 and an incubation temperature of 35°. The preferred substrate of GT was found to be kaempferol, the second best substrate was quercetin. The isolated enzymatic products were detected by TLC and HPLC and identified by spectral analysis and comparison with authentic compounds. This experiment from economic point of view provides the best conditions for large scale production of glucosides of kaempferol, quercetin and isorahmnetin.
2005
06
30
113
117
https://bpsa.journals.ekb.eg/article_65237_31b15b7b8898bfc4b08ae855bbcee446.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
INCLUSION COMPLEXES OF NICARDIPINE - HCl FOR ORAL ADMINISTRATION
F.
Ghazy
O.
Sammour
S.
Ghareeb
H.
El-Ghamry
M.
Issa
G.
Atia
Inclusion complexes of nicardipine HCl (NIC) with β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were prepared using different methods: coevaporation, kneading and co-precipitation. Inclusion complexation in aqueous solution and in solid state was studied by the solubility method, Fourier transform-infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). The solubility of (NIC) increased as a function of cyclodextrin concentration, showing Bs and AL type diagrams for (β-CD) and (HP-β-CD), respectively. The dissolution rate of (NIC) / cyclodextrin complexes were investigated and compared with those of the physical mixtures and pure drug. The dissolution efficiency of (NIC) increased by complexation with cyclodextrins to 2.8-2.9 fold than (NIC) alone. Oral bioavailability in rabbits increased to ~ 6 fold by complexation with (β-CD).
2005
06
30
119
129
https://bpsa.journals.ekb.eg/article_65238_dce226594f376925ff044061e9572049.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF SOME MANNICH BASES DERIVED FROM ISATIN ISONICOTINIC ACID HYDRAZONE
Mostafa
Hussein
Tarek
Aboul-Fadl
Asmma
Hussein
The purpose of this study based on the design and synthesis of a new series of 4-[1(substitutedaminomethyl)]-2-oxo-2,3-dihydro-1H-3-indolylidene-pyridine- carboxylic acid hydrazones (2a-g) in a trial to overcome the resistance developed with the therapeutic uses of isonicotinic acid hydrazide (isoniazid, INH). The new compounds were prepared by reacting isatin isonicotinic acid hydrazone with formalin and the appropriate secondary amines. The structures of the newly synthesized compounds were elucidated using different spectral data (IR, 1HNMR, and 13CNMR) as well as elemental methods of analyses. The lipophilicity of the synthesized compounds supercedes that of INH as expressed by Clog P. The new compounds (2a-g) as well as INH as a reference drug were tested for their antitubercular activity against bovine Mycobacterium tuberculosis at a dose level of 10 μmol. The tested compounds exhibited comparable inhibitory activity against the tested TB strain comparing to INH a reference drug.
2005
06
30
131
136
https://bpsa.journals.ekb.eg/article_65240_3499ef9c0309f4e3bd420844f185f31d.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
THE EFFECT OF CIPROFLOXACIN AND CLARITHROMYCIN ON SILDENAFIL ORAL BIOAVAILABILITY IN HUMAN VOLUNTEERS
Mohsen
Hedaya
Dalia
El-Afify
Gamal
El-Maghraby
Sildenafil is the first oral therapeutic agent for the management of male erectile dysfunction. Its oral bioavailability is only 40% due to extensive presystemic elimination, mainly by CYP3A4. This study examined the effect of coadministration of ciprofloxacin or clarithromycin which inhibit CYP3A4 on the bioavailability and pharmacokinetics of sildenafil. Twelve healthy male volunteers received sildenafil alone or after pretreatment with the inhibitors in a balanced three-way crossover design. The pharmacokinetic analysis showed that ciprofloxacin coadministration with sildenafil significantly increased the AUC from 1336±407 to 2751±968 µg hr/L and the Cmax from 236±71 to 478±210 µg/L. The CLtot/F was decreased from 40.1±9.9 to 20.9±8.6 L/hr and the Vd/F from 134.9±9.9 to 89.1±31.8 L, without affecting sildenafil elimination and absorption rate constants. Similarly, clarithromycin coadministration increased sildenafil AUC from 1336±407 to 2920±666 µg hr/L and Cmax from 236±71 to 520±176 µg/L. The CLtot/F significantly decreased from 40.1±9.9 to 18.1±5.0 L/hr and the Vd/F from 134.9±9.9 to 71.6±27.4 L, without affecting sildenafil elimination and absorption rate constants. These results indicate that coadministration of ciprofloxacin and clarithromycin significantly increased sildenafil bioavailability which can be inhibitory effect of ciprofloxacin and clarithromycin on CYP3A4. Dose adjustment of sidenafil is thus necessary when administered with such drugs.
2005
06
30
137
142
https://bpsa.journals.ekb.eg/article_65246_b3724778cba7d886da60877b81e564b9.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
CYTOTOXIC PHENOLICS FROM THE FLOWERS OF HIPPEASTRUM VITTATUM
Diaa
Youssef
Bioassay-guided fractionation and purification of the ethanolic extract of the fresh flowers of Hippeastrum vittatum (Amaryllidaceae) cultivated in Egypt yielded three compounds viz. caffeic acid (1), dihydrocaffeic acid methyl ester (2), together with the polyhydroxylated alkaloid pancratistatin (3). The structures of the isolated compounds were determined on the basis of extensive 1D (1H and 13C) and 2D (COSY, HMQC, and HMBC) NMR studies, and mass spectral measurements. The cytotoxic activity of compounds 1-3 is presented and discussed
2005
06
30
143
148
https://bpsa.journals.ekb.eg/article_65247_6ef74d5dd54aa010bfb8a33e876b6547.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2005
28
1
XANTHONES FROM CELL CULTURES OF HYPERICUM GNIDIOIDES SEEM.
A.
Abd El-Mawla
Oxygenated and prenylated xanthones were isolated from the cell cultures of Hypericum gnidioides Seem. when grown in modified B5 medium in the dark. Based on the spectral methods, the structure of the isolated compounds were elucidated as 1,7-dihydroxyxanthone (euxanthone), 1,3,7-trihydroxyxanthone, 1,3,5,6-tetrahydroxyxanthone, 1,3,6,7-tetrahydroxy-8(3-methylbut-2-enyl) xanthone and 1,3,6,7-tetrahydroxy-2,8-di(3-methylbut-2-enyl) xanthone ( -mangostin). The occurrence of both 1,7-dihydroxyxanthone and 1,3,7- trihydroxyxanthone which is recorded for the first time in cell cultures of Hypericum species indicate the presence of a reductase activity responsible for eliminating the 3-hydroxy group and confirm the biosynthetic pathway of xanthones in Hypericum species respectively.
2005
06
30
105
111
https://bpsa.journals.ekb.eg/article_65249_1da752d45a7db994cfad637fec79728d.pdf