mannich-bases and morpholine

Leishmaniasis is an important parasitic disease in many countries, including ours. A variety of drugs are currently used for its treatment. However, certain side effects of these drugs, such as teratogenicity, hepatotoxicity and nephrotoxicity, have been reported in some patients. The goal of this research is to determine the antileishmanial effects of eight different previously synthesised compounds containing Schiff and Mannich bases (morpholine) against. Compounds containing Schiff bases (a-d) and both Schiff bases and morpholine rings (e-h) were tested. Compounds were diluted in the range of 20000-39 μg/mL.. These compounds may be potential drug candidates for the treatment of leishmaniasis. According to the results, there is a need for further studies, such as in vivo experimental animal models and

Topics: Antiprotozoal Agents; Cell Proliferation; Leishmania infantum; Mannich Bases; Morpholines; Parasitic Sensitivity Tests; Schiff Bases

Topics: Anti-Bacterial Agents; Antifungal Agents; Antioxidants; Bacteria; Dose-Response Relationship, Drug; Fungi; Mannich Bases; Microbial Sensitivity Tests; Molecular Structure; Morpholines; Schiff Bases; Structure-Activity Relationship; Triazoles

4-Amino-2-[(5-arylamino-4,5-dihydro-1,3,4-thiadiazol-2-yl)methyl]-5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-ones (3a-c) were obtained in acidic media via the formation of 2-[(4-amino-3-aryl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)acetyl]-N-arylhydrazinecarbothioamides (2a-c), and then, compound 3b was converted to methylated derivative, 4. The basic treatment of carbothioamide derivatives, 2a-c, afforded 4-amino-2-[(4-aryl-5-sulphanyl-4H-1,2,4-triazol-3-yl)methyl]-5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-ones (5a-c). The alkylation reactions of compounds 4H-1,2,4-triazol-3-ylmethyl-5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one derivatives (5a-c) were performed by using methyl iodide or ethyl bromide in the presence of sodium ethoxide, while the treatment of the same intermediates, 5a-c, with aromatic aldehydes produced 2-{[4-(4-aryl)-5-sulphanyl-4H-1,2,4-triazol-3-yl]methyl}-4-(arylmethylene)amino-5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-ones (8a-d). The synthesis of 4-amino-(or arylideneamino)-5-(4-methylphenyl)-2-{[(4-methylpiperazin-1-yl or morpholin-4-ylethyl)methyl]-4-aryl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl}methyl-2,4-dihydro-3H-1,2,4-triazol-3-ones (7a, b and 9) was performed by a one pot three-component Mannich reaction involving the corresponding compounds, 4-(substituted)amino-4H-1,2,4-triazol-3-ylmethyl-5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one derivatives 5a, b and 8a, methylpiperazine or 2-(4-morpholino)ethylamine and formaldehyde. The newly synthesized compounds were well characterized by elemental analyses, IR, (1)H NMR, (13)C NMR and mass spectral studies. They were also screened for their microbial activities. The antimicrobial activity study revealed that some of which 2a, c, 3c, 5a-c, 8a-d showed good activity against a variety of microorganisms.

Topics: Anti-Infective Agents; Bacteria; Drug Design; Fungi; Mannich Bases; Morpholines; Piperazine; Piperazines; Triazoles