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Synthesis, characterization, and anti-amoebic activity of N-(pyrimidin-2-yl)benzenesulfonamide derivatives. 2013

Abdul Roouf Bhat, and Mohammad Arshad, and Eun Ju Lee, and Smritee Pokharel, and Inho Choi, and Fareeda Athar
School of Biotechnology, Yeungnam University, Gyeongsan 712 - 749, Republic of Korea, (phone: +82-53-810-3024; fax: +82-53-810-4769).

A new series of N-(pyrimidin-2-yl)benzenesulfonamide derivatives, 3a-3i and 4a-4i, was synthesized from pyrimidin-2-amines, 2a-2i, with the aim to explore their effects on in vitro growth of Entamoeba histolytica. The chemical structures of the compounds were elucidated by elemental analysis, FT-IR, (1) H- and (13) C-NMR, and ESI mass-spectral data. In vitro anti-amoebic activity was evaluated against HM1 : IMSS strain of Entamoeba histolytica. The IC50 values were calculated by using the double dilution method. The results were compared with the IC50 value of the standard drug 'metronidazole'. The selected compounds were tested for their cytotoxic activities by cell-viability assay using H9C2 cardiac myoblasts cell line, and the results indicated that all the compounds displayed remarkable >80% viabilities to a concentration of 100 μg/ml.

UI MeSH Term Description Entries
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D002470 Cell Survival The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability. Cell Viability,Cell Viabilities,Survival, Cell,Viabilities, Cell,Viability, Cell
D004748 Entamoeba histolytica A species of parasitic protozoa causing ENTAMOEBIASIS and amebic dysentery (DYSENTERY, AMEBIC). Characteristics include a single nucleus containing a small central karyosome and peripheral chromatin that is finely and regularly beaded. Endamoeba histolytica,histolytica, Endamoeba
D000096926 Benzenesulfonamides A group of compounds that contain sulfonamide group S-linked to a benzene ring. Many benzenesulfonamide derivatives are pharmaceuticals (e.g., BOSENTAN; SULFAPYRIDINE; and SULFADIAZINE; CELECOXIB) as their sulfonamide moiety target various enzymes (e.g., CARBONIC ANHYDRASES; ACETYLCHOLINESTERASE; BUTYRYLCHOLINESTERASE; and CYCLOOXYNENASE 2). Benzenesulfonamide,Benzenesulfonamide Derivatives,Benzenesulfonamide Monosodium Salt,Benzenesulphonamides,Benzosulfonamides
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000981 Antiprotozoal Agents Substances that are destructive to protozoans. Schizonticides,Agents, Antiprotozoal
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D013449 Sulfonamides A group of compounds that contain the structure SO2NH2. Sulfonamide,Sulfonamide Mixture,Sulfonamide Mixtures,Mixture, Sulfonamide,Mixtures, Sulfonamide
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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