34631-53-3Relevant academic research and scientific papers
Optimization of Novel 1-Methyl-1 H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber's Pole Worm
Le, Thuy G.,Kundu, Abhijit,Ghoshal, Atanu,Nguyen, Nghi H.,Preston, Sarah,Jiao, Yaqing,Ruan, Banfeng,Xue, Lian,Huang, Fei,Keiser, Jennifer,Hofmann, Andreas,Chang, Bill C. H.,Garcia-Bustos, Jose,Jabbar, Abdul,Wells, Timothy N. C.,Palmer, Michael J.,Gasser, Robin B.,Baell, Jonathan B.
, p. 10875 - 10894 (2019/01/04)
A phenotypic screen of a diverse library of small molecules for inhibition of the development of larvae of the parasitic nematode Haemonchus contortus led to the identification of a 1-methyl-1H-pyrazole-5-carboxamide derivative with an IC50 of 0.29 μM. Medicinal chemistry optimization targeted modifications on the left-hand side (LHS), middle section, and right-hand side (RHS) of the scaffold in order to elucidate the structure-activity relationship (SAR). Strong SAR allowed for the iterative and directed assembly of a focus set of 64 analogues, from which compound 60 was identified as the most potent compound, inhibiting the development of the fourth larval (L4) stage with an IC50 of 0.01 μM. In contrast, only 18% inhibition of the mammary epithelial cell line MCF10A viability was observed, even at concentrations as high as 50 μM.
Synthesis of 2-aminothiazole derivatives from easily available thiourea and alkyl/aryl ketones using aqueous NaICl2
Ghodse, Shrikant M.,Telvekar, Vikas N.
, p. 472 - 474 (2015/03/05)
A simple methodology was developed to synthesize substituted aminothiazoles from the corresponding thiourea and substituted ketones using aqueous NaICl2 at reflux temperature in THF. The products were obtained in good to excellent yields.
Carbon tetrabromide mediated oxidative cyclocondensation of ketones and thioureas: An easy access to 2-aminothiazoles
Keshari, Twinkle,Kapoorr, Ritu,Yadav, Lal Dhar S.
supporting information, p. 5623 - 5627 (2015/09/21)
A simple, mild, and efficient one-pot method for the synthesis of substituted 2-aminothiazoles has been reported. The reaction involves the formation of sulfenyl bromide as an umpolung intermediate of nucleophilic sulfur, which is responsible for C-S bond formation leading to oxidative cyclization of ketones and thioureas to furnish the desired products. Carbon tetrabromide was used as a convenient and mild brominating reagent under basic condition at room temperature to give 2-aminothiazoles in good to excellent yields.
NEW AMINOTHIAZOLES AS FBPASE INHIBITORS FOR DIABETES
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, (2009/06/27)
Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS AND USES THEREOF
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Page/Page column 126, (2008/06/13)
The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in th
Positive allosteric modulators of the nicotinic acetylcholine receptor
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Page 27, (2010/02/05)
The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which α7 nAChR is known to be involved.
Polycyclic dyes
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, (2008/06/13)
A benzodifuranone dye carrying at least one thiazolyl group, the dye may be of Formula (3) or Formula (5): in which Ris -H or alkyl; Xis -H, alkyl or alkylcarbonyl; Ais a phenyl group which is unsubstituted by from one to three substituents or Ais a group
