147397-31-7Relevant academic research and scientific papers
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0331, (2016/02/28)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.
Virtual screening identification of nonfolate compounds, including a CNS drug, as antiparasitic agents inhibiting pteridine reductase
Ferrari, Stefania,Morandi, Federica,Motiejunas, Domantas,Nerini, Erika,Henrich, Stefan,Luciani, Rosaria,Venturelli, Alberto,Lazzari, Sandra,Calò, Samuele,Gupta, Shreedhara,Hannaert, Veronique,Michels, Paul A. M.,Wade, Rebecca C.,Costi, M. Paola
experimental part, p. 211 - 221 (2011/03/19)
Folate analogue inhibitors of Leishmania major pteridine reductase (PTR1) are potential antiparasitic drug candidates for combined therapy with dihydrofolate reductase (DHFR) inhibitors. To identify new molecules with specificity for PTR1, we carried out a virtual screening of the Available Chemicals Directory (ACD) database to select compounds that could interact with L. major PTR1 but not with human DHFR. Through two rounds of drug discovery, we successfully identified eighteen drug-like molecules with low micromolar affinities and high in vitro specificity profiles. Their efficacy against Leishmania species was studied in cultured cells of the promastigote stage, using the compounds both alone and in combination with 1 (pyrimethamine; 5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine). Six compounds showed efficacy only in combination. In toxicity tests against human fibroblasts, several compounds showed low toxicity. One compound, 5c (riluzole; 6-(trifluoromethoxy)- 1,3-benzothiazol-2-ylamine), a known drug approved for CNS pathologies, was active in combination and is suitable for early preclinical evaluation of its potential for label extension as a PTR1 inhibitor and antiparasitic drug candidate.
Aminoalkyl-substituted 2-amino-1,3,4-thiadiazoles, the preparation and use thereof
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, (2008/06/13)
Aminoalkyl-substituted 2-amino-1,3,4-thiadiazoles of the formula STR1 where n and A have the meanings stated in the description, and the preparation thereof are described. The compounds are suitable for controlling diseases.
PHARMACOLOGICALLY ACTIVE GUANIDINE COMPOUNDS
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, (2008/06/13)
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-guanidines which are inhibitors of histamine activity.
PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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, (2008/06/13)
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
