Gs-9137

Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors

“…β-Diketo acid derivatives as represented by S-136016 was the first integrase inhibitor class to have entered clinical trials. Naphthyridine carboxamides such as L-870,81017 have also advanced to clinical trials as have novel mono keto quinolone carboxylic acids18,19 such as GS-9137 which is currently undergoing Phase III clinical trials. Inspite of over two decades of extensive research leading to promising IN inhibitors,20–25 hitherto only one IN inhibitor, raltegravir,26 a pyrimidinone carboxamide, has been approved for clinical use.…”

Aryldiketo Acids Have Antibacterial Activity Against MDR Staphylococcus aureus Strains: Structural Insights Based on Similarity and Molecular Interaction Fields

“…GS-9137 (elvitegravir, CAS 697761-98-1), a 4-quinolone-3-carboxylic acidbased HIV-1 integrase inhibitor is presently in phase III clinical trials. [4] The similarity between these two scaffolds ( Figure 1), both of which are integrase inhibitors, inspired our study of aryldiketo acids (ADK) as potential antibacterial agents. To the best of our knowledge, the antibacterial activity of ADK, the scaffold of an important class of HIV-1 integrase inhibitors, [5] has not been reported in the literature so far.…”

An Improved Synthesis of Elvitegravir

“…Scheme 8. Synthesis of elvitegravir (1). corresponding (R)-enantiomer of 28a were used as standards for the chiral purity HPLC determination, which proved that no evident racemization takes place during the reaction sequences used.…”

“…For the reasons given earlier, we decided to develop a new synthesis of elvitegravir (1) starting from easily available 2,4-dimethoxyacetophenone. We also decided to introduce the 2-fluoro-3-chlorobenzyl group in a late step of the synthesis.…”