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1.
Braz. j. biol ; 82: 1-7, 2022. tab
Article in English | LILACS, VETINDEX | ID: biblio-1468540

ABSTRACT

In the present study, the biochemical composition of some Echinodermata (Holothuroidea, Echinoidea) from the Red Sea, Egypt was investigated. The results showed that the highest percentage of saturated fatty acids (SFA) was in Holothuria nobilis and the lowest percentage was recorded in Holothuria scabra. The highest percentage of monounsaturated fatty acids (MUFA) was recorded in Pearsonothuria graeffei while the lowest percentage was recorded in Holothuria atra. The highest percentage of polyunsaturated fatty acids (PUFA) was recorded in Holothuria nobilis and the lowest percentage was recorded in Holothuria atra. The highest percentage of omega-3 fatty acids was recorded in Stichopus hermanni however, the lowest percentage was recorded in Diadema setosum. The highest percentage of omega-6 fatty acids was recorded in Bohadschia vitiensis where, the lowest percentage was recorded in Holothuria atra. In addition, nonessential amino acid (NEAA) glycine were the highest in all species and serine was the lowest while Essential amino acid (EAA) arginine was the highest and cysteine was the lowest. All of the NEAA recorded highest concentrations in S. hermanni except proline. The recorded essential amino acids were histidine, isoleucine, phenylalanine, and leucine. The latter was high in Pearsonothuria graeffei. Tyrosine, valine, threonine, and arginine were high in Stichopus hermanni. The present study proved that sea cucumbers has great nutritional value.


No presente estudo, investigou-se a composição bioquímica de algumas espécies Echinodermata (Holothuroidea, Echinoidea) do Mar Vermelho no Egito. Os resultados mostraram que a maior porcentagem de ácidos graxos saturados (SFA) foi na espécie Holothuria nobilis e a menor porcentagem foi registrada em Holothuria scabra. A maior porcentagem de ácidos graxos monoinsaturados (MUFA) foi registrada na espécie Pearsonothuria graeffei, enquanto a menor porcentagem foi registrada em Holothuria atra. O maior percentual de ácidos graxos poli insaturados (PUFA) foi registrado em Holothuria nobilis e o menor percentual foi registrado em Holothuria atra. A maior porcentagem de ácidos graxos ômega-3 foi registrada na espécie Stichopus hermanni, entretanto, a menor porcentagem foi registrada em Diadema setosum. A maior porcentagem de ácidos graxos ômega-6 foi registrada em Bohadschia vitiensis e a menor porcentagem foi registrada em Holothuria atra. Além disso, o nível de aminoácido não-essencial (NEAA) glicina foi o mais alto em todas as espécies e o de serina foi o mais baixo, enquanto o nível de aminoácido essencial (EAA) arginina foi o mais alto e a cisteína foi o mais baixo. Todos os NEAA registraram concentrações mais altas em S. hermanni, exceto prolina. Os aminoácidos essenciais registrados foram histidina, isoleucina, fenilalanina e leucina. A leucina apresentou alto nível na espécie Pearsonothuria graeffei. Tirosina, valina, treonina e arginina apresentaram níveis elevados em Stichopus hermanni. Assim, o presente estudo comprovou que o pepino-do-mar possui grande valor nutricional.


Subject(s)
Animals , Amino Acids/analysis , Echinodermata/chemistry , Biochemical Phenomena , Fatty Acids/analysis , Sea Cucumbers , Stichopus
2.
Braz. j. biol ; 822022.
Article in English | LILACS-Express | LILACS, VETINDEX | ID: biblio-1468727

ABSTRACT

Abstract In the present study, the biochemical composition of some Echinodermata (Holothuroidea, Echinoidea) from the Red Sea, Egypt was investigated. The results showed that the highest percentage of saturated fatty acids (SFA) was in Holothuria nobilis and the lowest percentage was recorded in Holothuria scabra. The highest percentage of monounsaturated fatty acids (MUFA) was recorded in Pearsonothuria graeffei while the lowest percentage was recorded in Holothuria atra. The highest percentage of polyunsaturated fatty acids (PUFA) was recorded in Holothuria nobilis and the lowest percentage was recorded in Holothuria atra. The highest percentage of omega-3 fatty acids was recorded in Stichopus hermanni however, the lowest percentage was recorded in Diadema setosum. The highest percentage of omega-6 fatty acids was recorded in Bohadschia vitiensis where, the lowest percentage was recorded in Holothuria atra. In addition, nonessential amino acid (NEAA) glycine were the highest in all species and serine was the lowest while Essential amino acid (EAA) arginine was the highest and cysteine was the lowest. All of the NEAA recorded highest concentrations in S. hermanni except proline. The recorded essential amino acids were histidine, isoleucine, phenylalanine, and leucine. The latter was high in Pearsonothuria graeffei. Tyrosine, valine, threonine, and arginine were high in Stichopus hermanni. The present study proved that sea cucumbers has great nutritional value.


Resumo No presente estudo, investigou-se a composição bioquímica de algumas espécies Echinodermata (Holothuroidea, Echinoidea) do Mar Vermelho no Egito. Os resultados mostraram que a maior porcentagem de ácidos graxos saturados (SFA) foi na espécie Holothuria nobilis e a menor porcentagem foi registrada em Holothuria scabra. A maior porcentagem de ácidos graxos monoinsaturados (MUFA) foi registrada na espécie Pearsonothuria graeffei, enquanto a menor porcentagem foi registrada em Holothuria atra. O maior percentual de ácidos graxos poli-insaturados (PUFA) foi registrado em Holothuria nobilis e o menor percentual foi registrado em Holothuria atra. A maior porcentagem de ácidos graxos ômega-3 foi registrada na espécie Stichopus hermanni, entretanto, a menor porcentagem foi registrada em Diadema setosum. A maior porcentagem de ácidos graxos ômega-6 foi registrada em Bohadschia vitiensis e a menor porcentagem foi registrada em Holothuria atra. Além disso, o nível de aminoácido não-essencial (NEAA) glicina foi o mais alto em todas as espécies e o de serina foi o mais baixo, enquanto o nível de aminoácido essencial (EAA) arginina foi o mais alto e a cisteína foi o mais baixo. Todos os NEAA registraram concentrações mais altas em S. hermanni, exceto prolina. Os aminoácidos essenciais registrados foram histidina, isoleucina, fenilalanina e leucina. A leucina apresentou alto nível na espécie Pearsonothuria graeffei. Tirosina, valina, treonina e arginina apresentaram níveis elevados em Stichopus hermanni. Assim, o presente estudo comprovou que o pepino-do-mar possui grande valor nutricional.

3.
Braz. j. biol ; 82: e246309, 2022. tab
Article in English | LILACS, VETINDEX | ID: biblio-1278504

ABSTRACT

In the present study, the biochemical composition of some Echinodermata (Holothuroidea, Echinoidea) from the Red Sea, Egypt was investigated. The results showed that the highest percentage of saturated fatty acids (SFA) was in Holothuria nobilis and the lowest percentage was recorded in Holothuria scabra. The highest percentage of monounsaturated fatty acids (MUFA) was recorded in Pearsonothuria graeffei while the lowest percentage was recorded in Holothuria atra. The highest percentage of polyunsaturated fatty acids (PUFA) was recorded in Holothuria nobilis and the lowest percentage was recorded in Holothuria atra. The highest percentage of omega-3 fatty acids was recorded in Stichopus hermanni however, the lowest percentage was recorded in Diadema setosum. The highest percentage of omega-6 fatty acids was recorded in Bohadschia vitiensis where, the lowest percentage was recorded in Holothuria atra. In addition, nonessential amino acid (NEAA) glycine were the highest in all species and serine was the lowest while Essential amino acid (EAA) arginine was the highest and cysteine was the lowest. All of the NEAA recorded highest concentrations in S. hermanni except proline. The recorded essential amino acids were histidine, isoleucine, phenylalanine, and leucine. The latter was high in Pearsonothuria graeffei. Tyrosine, valine, threonine, and arginine were high in Stichopus hermanni. The present study proved that sea cucumbers has great nutritional value.


No presente estudo, investigou-se a composição bioquímica de algumas espécies Echinodermata (Holothuroidea, Echinoidea) do Mar Vermelho no Egito. Os resultados mostraram que a maior porcentagem de ácidos graxos saturados (SFA) foi na espécie Holothuria nobilis e a menor porcentagem foi registrada em Holothuria scabra. A maior porcentagem de ácidos graxos monoinsaturados (MUFA) foi registrada na espécie Pearsonothuria graeffei, enquanto a menor porcentagem foi registrada em Holothuria atra. O maior percentual de ácidos graxos poliinsaturados (PUFA) foi registrado em Holothuria nobilis e o menor percentual foi registrado em Holothuria atra. A maior porcentagem de ácidos graxos ômega-3 foi registrada na espécie Stichopus hermanni, entretanto, a menor porcentagem foi registrada em Diadema setosum. A maior porcentagem de ácidos graxos ômega-6 foi registrada em Bohadschia vitiensis e a menor porcentagem foi registrada em Holothuria atra. Além disso, o nível de aminoácido não-essencial (NEAA) glicina foi o mais alto em todas as espécies e o de serina foi o mais baixo, enquanto o nível de aminoácido essencial (EAA) arginina foi o mais alto e a cisteína foi o mais baixo. Todos os NEAA registraram concentrações mais altas em S. hermanni, exceto prolina. Os aminoácidos essenciais registrados foram histidina, isoleucina, fenilalanina e leucina. A leucina apresentou alto nível na espécie Pearsonothuria graeffei. Tirosina, valina, treonina e arginina apresentaram níveis elevados em Stichopus hermanni. Assim, o presente estudo comprovou que o pepino-do-mar possui grande valor nutricional.


Subject(s)
Animals , Sea Cucumbers , Sea Urchins , Indian Ocean , Echinodermata , Egypt
4.
Braz J Biol ; 82: e246309, 2021.
Article in English | MEDLINE | ID: mdl-34133577

ABSTRACT

In the present study, the biochemical composition of some Echinodermata (Holothuroidea, Echinoidea) from the Red Sea, Egypt was investigated. The results showed that the highest percentage of saturated fatty acids (SFA) was in Holothuria nobilis and the lowest percentage was recorded in Holothuria scabra. The highest percentage of monounsaturated fatty acids (MUFA) was recorded in Pearsonothuria graeffei while the lowest percentage was recorded in Holothuria atra. The highest percentage of polyunsaturated fatty acids (PUFA) was recorded in Holothuria nobilis and the lowest percentage was recorded in Holothuria atra. The highest percentage of omega-3 fatty acids was recorded in Stichopus hermanni however, the lowest percentage was recorded in Diadema setosum. The highest percentage of omega-6 fatty acids was recorded in Bohadschia vitiensis where, the lowest percentage was recorded in Holothuria atra. In addition, nonessential amino acid (NEAA) glycine were the highest in all species and serine was the lowest while Essential amino acid (EAA) arginine was the highest and cysteine was the lowest. All of the NEAA recorded highest concentrations in S. hermanni except proline. The recorded essential amino acids were histidine, isoleucine, phenylalanine, and leucine. The latter was high in Pearsonothuria graeffei. Tyrosine, valine, threonine, and arginine were high in Stichopus hermanni. The present study proved that sea cucumbers has great nutritional value.


Subject(s)
Sea Cucumbers , Animals , Echinodermata , Egypt , Indian Ocean , Sea Urchins
5.
Eur Rev Med Pharmacol Sci ; 25(24): 7926-7933, 2021 Dec.
Article in English | MEDLINE | ID: mdl-34982455

ABSTRACT

OBJECTIVE: This paper aims to review the literature systematically on warfarin adherence in patients with atrial fibrillation and to assess the anticoagulation control focused on patient clinical outcomes. Atrial Fibrillation (AF) is a cardiac disease defined by abnormal heart rhythm, which significantly impacts a patient's health status, quality of life, and heart output, and thus a greater risk of stroke and hospitalization. Most AF patients should be managed with long-term anticoagulation, either with vitamin K antagonists such as warfarin or new oral anticoagulants (NOACs). Anticoagulants have been a core in treating AF and weighing the consequences of thrombosis with the risk of bleeding. This systematic review aimed to assess the impact of warfarin adherence on AF patients. MATERIALS AND METHODS: A systematic search of the literature was conducted on electronic databases of PubMed/MEDLINE, EBSCO, Cochrane library, Google, and Google Scholar from January 2011 to April 2021 to determine studies that reported warfarin adherence on patients with atrial fibrillation. RESULTS: Out of 1429 titles and abstracts were retrieved, 12 studies fulfilled and met the inclusion criteria. From the included studies, two were carried out in Brazil and one from the following nations: Libya, Jordan, Iran, KSA, Canada, Malaysia, Bahrain, UAE, Singapore, and the USA. The study designs identified were cross-section, retrospective, and prospective studies. Warfarin adherence was influenced by multiple causes, including pharmaceutical services, the number of medications, and warfarin knowledge regarding anticoagulation control. Warfarin adherence illustrates its positive association with TTR and INR as a measure of anticoagulation control. CONCLUSIONS: While the available evidence is limited, this systematic review demonstrated a positive finding of the association between warfarin adherence and anticoagulation control in patients with AF.


Subject(s)
Anticoagulants/therapeutic use , Atrial Fibrillation/drug therapy , Medication Adherence , Warfarin/therapeutic use , Blood Coagulation/drug effects , Humans , Treatment Outcome
6.
Eur J Med Chem ; 45(11): 5265-77, 2010 Nov.
Article in English | MEDLINE | ID: mdl-20875694

ABSTRACT

Versatile simple efficient routes with good to excellent yields towards different functionalized 1,ω-bis(1,2,4-triazoles), 21-28 membered 1,2,4-triazole fused macrocyclic and/or lariat macrocyclic oxaazathia crown Schiff bases and/or amines have been investigated. Antimicrobial screening of some selected compounds revealed different inhibitory effects against Aspergillus fumigatus RCMB 002008 (1), Penicillium italicum RCMB 001018 (1), Syncephalastrum racemosum RCMB 016001 Candida albicans RCMB 005003, Staphylococcus aureus RCMB 106-001 (1), Pseudomonas aeruginosa RCMB 102-002, Bacillus subtilis RCMB 101-001 and Escherichia coli RCMB 103-001.


Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Macrocyclic Compounds/chemical synthesis , Macrocyclic Compounds/pharmacology , Triazoles/chemical synthesis , Triazoles/pharmacology , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Spectrometry, Mass, Electrospray Ionization , Spectrophotometry, Infrared
7.
Carbohydr Res ; 344(13): 1654-9, 2009 Sep 08.
Article in English | MEDLINE | ID: mdl-19570527

ABSTRACT

Synthesis of some novel 4-arylhydrazono-5-trifluoromethyl-2,4-dihydropyrazol-3-ones, their N- and N,O-bis- beta-D-glucosides is described. Antimicrobial evaluation of eight selected compounds against Aspergillus fumigatus RCMB 002008 (1), Penicillium italicum RCMB 001018 (1), Syncephalastrum racemosum RCMB 016001, Candida albicans RCMB 005003, Staphylococcus aureus RCMB 106-001 (1), Pseudomonas aeruginosa RCMB 102-002, Bacillus subtilis RCMB 101-001, and Escherichiacoli RCMB 103-001 has been achieved. The screening results indicated that all the tested compounds exhibited different inhibitory effects against five to seven different organisms of the eight test organisms.


Subject(s)
Bacteria/drug effects , Glucosides/chemistry , Nitrogen/chemistry , Oxygen/chemistry , Pyrazolones/chemical synthesis , Pyrazolones/pharmacology , Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Microbial Sensitivity Tests , Pyrazolones/chemistry , Stereoisomerism
8.
Article in English | MEDLINE | ID: mdl-17479431

ABSTRACT

Novel simple and efficient synthetic approach for the synthesis of 6-substituted-2H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole-3-thiones is described. Glucosidation of these novel bases with 2,3,4,6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide followed by chromatographic separation gave the corresponding N-and S-ss-D-glucosides. The structure of these two regiosiomers was established chemically and spectroscopically. Antimicrobial screening of two selected regioisomeric compounds against Aspergillus fumigatus, Penicillium italicum, Syncephalastrum racemosum, Candida albicans, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, and Escherichia coli are compared.


Subject(s)
Anti-Infective Agents/chemical synthesis , Glucosides/chemical synthesis , Thiadiazoles/chemical synthesis , Triazoles/chemical synthesis , Anti-Infective Agents/pharmacology , Bacteria/growth & development , Fungi/growth & development , Glucosides/pharmacology , Microbial Sensitivity Tests , Thiadiazoles/pharmacology , Triazoles/pharmacology
9.
Article in English | MEDLINE | ID: mdl-17479432

ABSTRACT

Arabinosylation of some 4-amino- and 4-arylideneamino-5-(pyridin-3-yl)-2,4-dihydro-[1,2,4]-triazole-3-thiones with 2,3,4-tri-O-acetyl-beta-L-arabinopyranosyl bromide led to an efficient synthetic approach to the corresponding N-and S-alpha-L-arabinopyranosides. Structure assignment of these two regiosiomers was based on chemical and spectroscopic evidences. Antimicrobial activities of two selected regioisomeric N-and S-alpha-L-arabinopyranosides were compared. The N-alpha-L-arabinopyranoside showed higher inhibitory effect than its regioisomeric S-alpha-L-arabinopyranoside against Aspergillus fumigatus, Penicillium italicum, Staphylococcus aureus, and Pseudomonas aeruginosa.


Subject(s)
Anti-Infective Agents/chemical synthesis , Triazoles/chemical synthesis , Anti-Infective Agents/pharmacology , Aspergillus fumigatus/growth & development , Microbial Sensitivity Tests , Penicillium/growth & development , Pseudomonas aeruginosa/growth & development , Staphylococcus aureus/growth & development , Triazoles/pharmacology
10.
Eur J Med Chem ; 42(9): 1193-9, 2007 Sep.
Article in English | MEDLINE | ID: mdl-17408811

ABSTRACT

First synthesis of N- and S-alpha-l-arabinopyranosyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles is described. Antimicrobial screening of two selected regioisomeric compounds against Aspergillus fumigatus, Penicillium italicum, Syncephalastrum racemosum, Candida albicans, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis and Escherichia coli are compared.


Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Thiadiazoles/chemical synthesis , Thiadiazoles/pharmacology , Bacteria/classification , Bacteria/drug effects , Drug Evaluation, Preclinical , Fungi/classification , Fungi/drug effects , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests
11.
Carbohydr Res ; 341(13): 2187-99, 2006 Sep 25.
Article in English | MEDLINE | ID: mdl-16839524

ABSTRACT

Glucosidation of some 4-amino- and 4-arylideneamino-5-(pyridin-3-yl)-2,4-dihydro-[1,2,4]-triazole-3-thiones with 2,3,4,6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide followed by chromatographic separation gave the corresponding N- and S-beta-D-glucosides. The structure of these two regiosiomers was established chemically and spectroscopically. Deamination as well as deacetylation of some selected nucleosides have been achieved. Antimicrobial screening of 14 selected compounds resulted in their activity against Aspergillus fumigatus, Penicillium italicum, Syncephalastrum racemosum, Candida albicans, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, and Escherichia coli.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Antifungal Agents/chemical synthesis , Glucosides/chemistry , Triazoles/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Bacillus subtilis/drug effects , Candida albicans/drug effects , Escherichia coli/drug effects , Glucosides/chemical synthesis , Glucosides/pharmacology , Microbial Sensitivity Tests , Models, Chemical , Molecular Structure , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects , Structure-Activity Relationship , Triazoles/chemistry , Triazoles/pharmacology
12.
Article in English | MEDLINE | ID: mdl-16252664

ABSTRACT

Synthetic routes toward the synthesis of some novel 1-(2,3,4-tri-O-acetyl-alpha-L-arabinopyranosyl)-azetidin-2-ones are described. Antimicrobial screening of three selected compounds revealed their activity against Bacillus subtilis and Escherichia coli


Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Biochemistry/methods , beta-Lactams/chemistry , Arabinose/chemistry , Bacillus subtilis/drug effects , Escherichia coli/drug effects , Microbial Sensitivity Tests
13.
Article in English | MEDLINE | ID: mdl-16252672

ABSTRACT

Glucosidation of the appropriate 1,3 or 1,4-bis(4-amino or arylideneamino-2,4-dihydro-3-thioxo-3H-1,2,4-triazol-5-ylthio)propanes or butanes with 2,3,4,6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide followed by chromatographic separation gave the corresponding N-, S-, and N,S-bis(glucosides). Chemical transformation leading to new functionalities has been achieved. Antimicrobial screening of 10 selected compounds resulted in their activity against Aspergillus fumigatus, Penicillium italicum, Syncephalastrum racemosum, Candida albicans, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, and Escherichia coli.


Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Biochemistry/methods , Bacillus subtilis/drug effects , Butanes/chemistry , Candida albicans/drug effects , Drug Evaluation, Preclinical/methods , Escherichia coli/drug effects , Glucosides/chemistry , Microbial Sensitivity Tests , Propane/chemistry , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects , Triazoles/chemistry
14.
Article in English | MEDLINE | ID: mdl-15822617

ABSTRACT

Ribosylation of 3-aryl-5-benzyl(or substituted benzyl)-1,2,4-triazin-6(1H)-/ones or thiones with 1-O-acetyl-2,3,5-tri-O-benzoyl-beta-D-ribofuranose gave the corresponding 3-aryl-5-benzyl(or substituted benzyl)-1-(2,3,5-tri-O-benzoyl-beta-D-ribofuranosyl)-1,2,4-triazin-6(1H)-/ones or thiones. The structure of the new ribosides was confirmed chemically and spectroscopically.


Subject(s)
Ribonucleosides/chemical synthesis , Thiones/chemical synthesis , Triazines/chemical synthesis , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Molecular Structure , Ribonucleosides/chemistry , Thiones/chemistry , Triazines/chemistry
15.
Nucleosides Nucleotides Nucleic Acids ; 23(12): 1889-910, 2004.
Article in English | MEDLINE | ID: mdl-15628747

ABSTRACT

Glucosidation of the new 8-amino-6-benzyl(or substituted benzyl)-2,8-dihydro-1,2,4-triazolo[4,3-b][1,2,4]triazin-7(3H)-ones (3a-d) with 2,3,4,6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide 4 gave the corresponding N-glucosides 5a-d. Chemical transformations leading to new functionalities have also been achieved to give compounds 7-12. Antimicrobial activity of compounds 5a-c against Aspergillus fumigatus, Penicillium italicum, Syncephalastrum racemosum, Candida albicans, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Escherichia coli is described.


Subject(s)
Anti-Bacterial Agents , Heterocyclic Compounds , Triazines , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Glucose/analogs & derivatives , Glucose/chemistry , Heterocyclic Compounds/chemical synthesis , Heterocyclic Compounds/pharmacology , Microbial Sensitivity Tests , Molecular Structure , Structure-Activity Relationship , Triazines/chemical synthesis , Triazines/pharmacology
16.
Nucleosides Nucleotides Nucleic Acids ; 22(9): 1805-23, 2003 Sep.
Article in English | MEDLINE | ID: mdl-14533883

ABSTRACT

Synthetic routes towards different 2-alpha-L-arabinopyranosyl-3-thioxo-2,3-dihydro-1,2,4-triazin-5(4H)-/ones or thiones were investigated. Primary human anticancer screening of two selected compounds resulted in an active compound against SF-268 (CNS) cell line.


Subject(s)
Antineoplastic Agents/chemical synthesis , Triazines/chemical synthesis , Antineoplastic Agents/therapeutic use , Cell Line, Tumor , Drug Screening Assays, Antitumor , Humans , Molecular Structure , Triazines/therapeutic use
17.
Nucleosides Nucleotides Nucleic Acids ; 22(9): 1825-33, 2003 Sep.
Article in English | MEDLINE | ID: mdl-14533884

ABSTRACT

The 1-(2,3,4,6-tetra-O-acetyl-beta-D-galactopyranosyl)-3-aryl-5-benzyl (or substituted benzyl)-1,2,4-triazin-6(1H)-/ones or thiones were prepared via galactosidation of 3-aryl-5-benzyl (or substituted benzyl)-1,2,4-triazin-6(1H)-/ones or thiones with 2,3,4,6-tetra-O-acetyl-alpha-D-galactopyranosyl bromide. The structure of the new galactosyl derivatives was based on both spectroscopic and chemical evidences.


Subject(s)
Antineoplastic Agents/chemical synthesis , Galactosides/chemistry , Triazines/chemical synthesis , Molecular Structure
18.
Article in English | MEDLINE | ID: mdl-12708799

ABSTRACT

Selective synthesis and reactions of different 6-substituted-2-beta-D-galactosyl-3-thioxo-2,3-dihydro-1,2,4-triazin-5(4H)-ones using the developed amino or aryl protecting group strategy were investigated. Primary human anticancer screening of twelve selected compounds (in vitro) resulted in an active compound against both MCF7 (Breast) and SF-268(CNS) cell lines.


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Galactosides/chemical synthesis , Galactosides/chemistry , Galactosides/pharmacology , Humans , Hydrocarbons, Iodinated/chemistry , Triazines/chemical synthesis , Triazines/chemistry , Triazines/pharmacology
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