158890-32-5Relevant articles and documents
AN ACTIVITY-GUIDE MAP OF ELECTROPHILE-CYSTEINE INTERACTIONS IN PRIMARY HUMAN IMMUNE CELLS
-
Paragraph 0250-0251; 0262, (2021/04/23)
Disclosed herein are methods, pharmaceutical compositions, and vaccines for modulating an immune response. Also disclosed herein are methods, pharmaceutical compositions, and vaccines for inducing an immune response.
Novel 3-nitro-1 H -1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents
Papadopoulou, Maria V.,Bloomer, William D.,Rosenzweig, Howard S.,Chatelain, Eric,Kaiser, Marcel,Wilkinson, Shane R.,McKenzie, Caroline,Ioset, Jean-Robert
experimental part, p. 5554 - 5565 (2012/08/29)
A series of novel 3-nitro-1H-1,2,4-triazole-based (and in some cases 2-nitro-1H-imidazole-based) amides and sulfonamides were characterized for their in vitro antitrypanosomal and antileishmanial activities as well as mammalian toxicity. Out of 36 compounds tested, 29 (mostly 3-nitro-1H-1,2,4-triazoles) displayed significant activity against Trypanosoma cruzi intracellular amastigotes (IC50 ranging from 28 nM to 3.72 μM) without concomitant toxicity to L6 host cells (selectivity 66-2782). Twenty-three of these active compounds were more potent (up to 58-fold) than the reference drug benznidazole, tested in parallel. In addition, nine nitrotriazoles which were moderately active (0.5 μM ≥ IC50 6.0 μM) against Trypanosoma brucei rhodesiense trypomastigotes were 5-31-fold more active against bloodstream-form Trypanosoma brucei brucei trypomastigotes engineered to overexpress reduced nicotinamide adenine dinucleotide dependent nitroreductase. Finally, three nitrotriazoles displayed a moderate activity against the axenic form of Leishmania donovani. Therefore, 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides are potent antitrypanosomal agents.
Pyridazinone derivatives with pharmaceutical activity
-
, (2008/06/13)
A 3(2H)-pyridazinone derivative of the formula (I) its salt, a process for its production and a pharmaceutical composition containing it. STR1 wherein each of R1, R2 and R3 which are independent of one another, is a hydrogen atom or a C1-4 alkyl group, X is a chlorine atom or a bromine atom, Y1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or a C1-4 alkoxy group, Y2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C1-4 alkyl group or a C1-4 alkoxy group, A is a C1-5 alkylene chain which may be substituted by a hydroxyl group, B is a carbonyl group or a methylene chain which may be substituted by a C1-4 alkyl group, and each of R4 and R5 which are independent of each other, is a C1-4 alkyl group, or R4 is a hydrogen atom and R5 is --Z--Ar (wherein Z is a C1-5 alkylene chain, and Ar is an aromatic 6-membered ring which may contain a nitrogen atom), or R4 and R5 together form a C2-6 cyclic alkylene group, or R4 and R5 form together with the adjacent nitrogen atom a 4-substituted piperazine ring of the formula: STR2 wherein R6 is a C1-4 alkyl group.