Bonini, C. published the artcileSynthesis and biological evaluation of new simple indolic non peptidic HIV Protease inhibitors: The effect of different substitution patterns, Name: (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, the publication is Bioorganic & Medicinal Chemistry (2014), 22(17), 4792-4802, database is CAplus and MEDLINE.
New structurally simple indolic non peptidic HIV Protease inhibitors were synthesized from (S)-glycidol by regioselective methods. Following the concept of targeting the protein backbone, different substitution patterns were introduced onto the common stereo-defined isopropanolamine core modifying the type of functional group on the indole, the position of the functional group on the indole and the type of the nitrogen containing group (sulfonamides or perhydroisoquinoline), alternatively. The systematic study on in vitro inhibition activity of such compounds confirmed the general beneficial effect of the 5-indolyl substituents in presence of arylsulfonamide moieties, which furnished activities in the micromolar range. Preliminary docking anal. allowed to identify several key features of the binding mode of such compounds to the protease.
Bioorganic & Medicinal Chemistry published new progress about 115314-17-5. 115314-17-5 belongs to esters-buliding-blocks, auxiliary class Epoxides,Chiral,Nitro Compound,Sulfonate,Benzene, name is (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, and the molecular formula is C9H9NO6S, Name: (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate.
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