- Antileishmanial activity screening of 5-nitro-2-heterocyclic benzylidene hydrazides
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A series of 53 nitro derivatives rationally designed were obtained by parallel synthesis and screened against Leishmania donovani. Six compounds exhibited IC50 values lower than standard drugs. Brief SAR analysis revealed that substitution is important to the activity. Nitrothiophene analogues were more potent than the nitrofuran ones. This was attributed to the ability of sulfur atoms in accommodating electrons from nitro group, which facilitate its reduction and therefore the formation of free radicals lethal to parasites.
- Rando, Daniela G.,Avery, Mitchell A.,Tekwani, Babu L.,Khan, Shabana I.,Ferreira, Elizabeth I.
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p. 6724 - 6731
(2008/12/22)
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- NOVEL PIPERIDINE DERIVATIVE
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The invention provides a compound of the following formula (1): wherein m, n, and p are independently an integer of 0 - 4, provided 3 ≤ m + n ≤ 8; X is nitrogen atom or a group of the formula: C-R15; Y is a substituted or unsubstituted aromatic group, etc.; R15, R1, R2, R3, R4 , R5, R6 and R7 are hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and Z is hydrogen atom, cyano group, etc., or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which exhibits an action for enhancing LDL receptor expression, and is useful as a medicament for treating hyperlipidemia, atherosclerosis, etc.
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Page/Page column 91
(2008/06/13)
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- NOVEL COMPOUNDS
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Novel inhibitors of Rho-kinases are disclosed.
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Page/Page column 73
(2008/06/13)
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