Bharate, Sandip B.; Khan, Shabana I.; Tekwani, Babu L.; Jacob, Melissa; Khan, Ikhlas A.; Singh, Inder Pal published the artcile< S-Euglobals: Biomimetic synthesis, antileishmanial, antimalarial, and antimicrobial activities>, SDS of cas: 4396-13-8, the main research area is euglobal analog preparation antileishmanial antimalarial antimicrobial structure.
Several new euglobal analogs (named as S-euglobals) were synthesized from phloroglucinol using a biomimetic three-component reaction involving Knoevenagel condensation and Diels-Alder cycloaddition with a monoterpene. Newly synthesized euglobal analogs involve monoterpenes that have not yet been encountered in natural euglobals. S-Euglobals along with previously synthesized robustadial A and B were evaluated for in vitro antileishmanial, antimalarial, antimicrobial, and cytotoxic activities. Out of sixteen analogs prepared, nine analogs were found to exhibit antileishmanial activity against Leishmania donovani promastigotes. A 2-carene-derived S-euglobal was the most potent antileishmanial with IC50 of 2.4 μg/mL and IC90 of 8 μg/mL, followed by a second 2-carene-derived S-euglobal and a nopol-derived S-euglobal (IC50 5.5 and 9.5 μg/mL). Antileishmanial activity of robustadial A (5) and B (6) was moderate with IC50 of 20 and 16 μg/mL, resp. Robustadial A and B and a 2-carene-derived S-euglobal exhibited weak antimalarial activity against Plasmodium falciparum (IC50 of 2.7-4.76 μg/mL). Few of the euglobal analogs showed antibacterial activity against methicillin-resistant Staphylococcus aureus. Amongst these, a nopol-derived S-euglobal was the most potent with IC50 of 1.0 μg/mL and MIC of 5.0 μg/mL. Most of the compounds were not cytotoxic up to 25 μg/mL in a panel of cell lines consisting of both cancer (SK-MEL, KB, BT-549, and SK-OV-3) as well as non-cancer kidney (Vero and LLC-PK11) cells.
Bioorganic & Medicinal Chemistry published new progress about Antimalarials. 4396-13-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H6O5, SDS of cas: 4396-13-8.
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