Our unique design elements are highlighted in this poster and include pharmacophore modification, prodrug utilization, thioamide
isosteres, and strategic lipophilicity incorporation.
DERIVATIVE MODULATES ANNEXIN V EXPRESSION IN HUMAN LIVER CARCINOMA HEPG2) CELLS 35.
The structural modifications from previously known antagonists were primarily in the D-ring region, involving a thioamide
replacement of an amide.
Compound 4 was subjected to a standard procedure of transforming the cyano group into amidine via thioimidate salt , that is nitrile 4 was reacted with hydrogen sulphide affording thioamide
5, which was converted to thioimidate salt 6 with methyl iodide.
The sulfur atom of this compound, which is engaged in a thioamide
bond with the indole ring, is responsible for a weak part of the toxicity of Amanita (e.
The antituberculous activity of thioamide
in vitro and in the experimental animal (mouse and guinea pig).
Specifically, we demonstrate how these derivatives undergo aminolysis under mild conditions with both protected and unprotected amino acids, giving rise to stable thioamide
9:15 Amide and Thioamide
Based Receptors for Anions
Studies indicated that thioamide
based macrocycles show superior binding affinity for anions.
Susceptibility to ethambutol was found in 42% and to thioamides
in 82% of candidates for the short regimen.
ciprofloxacin, levofloxacin and moxifloxacin); thioamides
This suggests that the atypical Beijing genotype clone is evolving toward total drug resistance (defined as in vitro resistance to all first-line drugs, as well as aminoglycosides, cyclic polypeptides, fluoroquinolones, thioamides
, serine analogs, and salicylic acid derivatives ) with acknowledgment of WHO's concern over the definition (31).