Immunotropic Properties of 2-Aminobenzimidazole Derivatives in Cultures of Human Peripheral Blood Cells, Part 5
العنوان: | Immunotropic Properties of 2-Aminobenzimidazole Derivatives in Cultures of Human Peripheral Blood Cells, Part 5 |
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المؤلفون: | Tomasz Kuznicki, Maria W. Kowalska, Wanda Nawrocka, Michał Zimecki |
المصدر: | Archiv der Pharmazie. 332:85-90 |
بيانات النشر: | Wiley, 1999. |
سنة النشر: | 1999 |
مصطلحات موضوعية: | chemistry.chemical_classification, Bicyclic molecule, medicine.drug_class, Stereochemistry, Lymphocyte, Nitro compound, Pharmaceutical Science, Carboxamide, Lymphocyte proliferation, Chemical synthesis, In vitro, chemistry.chemical_compound, medicine.anatomical_structure, chemistry, Drug Discovery, medicine, Lactam |
الوصف: | The reaction of 2-aminobenzimidazole with selected 4-methoxy-,2,4-dimethoxy-, 4-chloro-, 4-nitro-, and 2-nitrocinnamic acid under different conditions has been described. Two series of derivatives were obtained: 4-aryl-1,2,3,4-tetrahydropyrimido[1,2-a]-benzimidazol-2-ones (1-3) or substituted amides 4, 5, 7. The following compounds: 4-(p-methoxyphenyl)- (1), 4-(2,4-dimethoxyphenyl)- (2), 4-(p-chlorophenyl)-1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazo l-2-one (3), amides: 2-(p-nitrocinnamoylamino)- (4), 2-(p-methoxycinnamoylamino)-benzimidazole (5), and 3-methyl-1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazol-2-one (6), recently synthesized, have been selected for further studies. Among the studied compounds, 3 and 4 strongly inhibited PHA-induced proliferation of human lymphocytes and weaker, but significantly, MLC-induced lymphocyte proliferation. 3 and 4 inhibited also LPS- or MLC-induced TNF-alpha production. In addition, TNF-alpha production, induced by LPS, was inhibited by compounds 1 and 2. Higher activity of 3 and 4 could be associated with the presence in their structures of -Cl and -NO2 substituents as compared with compounds possessing -OCH3 groups. Compounds 3 and 4 were not toxic when administered orally to mice which predisposes them for further investigations with a chance of clinical application. |
تدمد: | 1521-4184 0365-6233 |
DOI: | 10.1002/(sici)1521-4184(19993)332:3<85::aid-ardp85>3.0.co;2-s |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::2590bbe7b6bc33fc920fcced1576f15f https://doi.org/10.1002/(sici)1521-4184(19993)332:3<85::aid-ardp85>3.0.co;2-s |
Rights: | CLOSED |
رقم الانضمام: | edsair.doi...........2590bbe7b6bc33fc920fcced1576f15f |
قاعدة البيانات: | OpenAIRE |
تدمد: | 15214184 03656233 |
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DOI: | 10.1002/(sici)1521-4184(19993)332:3<85::aid-ardp85>3.0.co;2-s |