Singh, Kawaljit; Kaur, Gurminder; Shanika, Petrus Siningu; Dziwornu, Godwin Akpeko; Okombo, John; Chibale, Kelly published the artcile< Structure-activity relationship analyses of fusidic acid derivatives highlight crucial role of the C-21 carboxylic acid moiety to its anti-mycobacterial activity>, SDS of cas: 29335-36-2, the main research area is fusidic acid fusidane triterpenoid synthesis SAR tuberculostatic tuberculosis; Anti-mycobacterial activity; Bioisosteres; Cytotoxicity; Fusidic acid.
Fusidic acid (FA) is a potent congener of the fusidane triterpenoid class of antibiotics. Structure-activity relationship (SAR) studies suggest the chem. structure of FA is optimal for its antibacterial activity. SAR studies from our group within the context of a drug repositioning approach in tuberculosis (TB) suggest that, as with its antibacterial activity, the C-21 carboxylic acid group is indispensable for its anti-mycobacterial activity. Further studies have led to the identification of 16-deacetoxy-16β-ethoxyfusidic acid (58), an analog which exhibited comparable activity to FA with an in vitro MIC99 value of 0.8μM. Preliminary SAR studies around the FA scaffold suggested that the hydrophobic side chain at C-20, like the C-11 OH group, was required for activity. The C-3 OH group, however, can be functionalized to obtain more potent compounds
Bioorganic & Medicinal Chemistry published new progress about Structure-activity relationship. 29335-36-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C3H8N2O, SDS of cas: 29335-36-2.
Referemce:
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