- Synthesis of carboxyimidamide-substituted benzo[c][1,2,5]oxadiazoles and their analogs, and evaluation of biological activity against Leishmania donovani
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A facile synthesis route to carboxyimidamide-substituted benzoxadiazoles and related derivatives was developed. A total of 25 derivatives were synthesized. They were evaluated for antileishmanial activity by inhibition of Leishmania donovani axenic amastigote growth using a fluorescent viability microplate assay. The most promising derivative (14) demonstrated an antileishmanial EC50 of 4.0 μM, and it also showed activity in infected macrophages (EC50 5.92 μM) without signs of cytotoxicity.
- Keurulainen, Leena,Heiskari, Mikko,Nenonen, Satu,Nasereddin, Abedelmajeed,Kopelyanskiy, Dmitry,Leino, Teppo O.,Yli-Kauhaluoma, Jari,Jaffe, Charles L.,Kiuru, Paula
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p. 1673 - 1678
(2015/09/15)
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- 1, 2 DISUBSTITUTED HETEROCYCLIC COMPOUNDS
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1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.
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