Chiral compounds of varying conformational rigidity and methods of synthesis
OwnerGlenn C. Micalizio, Thomas Kodadek +1inventors
InventorsGlenn C. Micalizio, Thomas Kodadek, Mohosin Sarkar
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Abstract
Synthesis of compounds having varying degrees of conformational rigidity is obtained via a low cost, high yield and efficient synthetic reactions. The library of compounds is structurally diverse, having at least one or more chiral centers and providing large numbers of compounds having building block diversity and substantial scaffold diversity. The compounds further provide a novel method for obtaining candidate therapeutic agents for prevention, treatment or diagnosis of diseases.
Claims39
A method of synthesizing a chiral monomer comprising:
- obtaining a stereodefined allylic alcohol via a stereoselective aldol reaction or a related transformation reaction and proceeding via stereoselective allylic transposition of the resulting allylic alcohol;
- and
- converting the resulting rearranged product to a chiral acid having a general structure of Formula I′:
A compound comprising a monomer set forth in Formula I:
- wherein, X and Y comprise any molecular motifs or functional groups compatible with oligomerization of two or more monomers of Formula I.
A method of identifying a candidate therapeutic agent, comprising:
- screening a library comprising one or more monomers, oligomers, or polymers of Formula I:
- contacting a biological sample, cell, tissue, or molecule in solution or attached to a solid or semi-solid support, with a compound of Formula I;
- assaying for any desired therapeutic effects;
- and,
- identifying a candidate therapeutic agent.
A pharmaceutical composition comprising a compound having a structure of Formula I:
A compound comprising:
A compound of Formula I comprising a monomer set forth in Formula I:
- wherein, X and Y comprise any molecular motif or functional group compatible with oligomerization of monomers of Formula I.;
- and, one or more monomers of an oligomer of Formula I are conjugated to a cytotoxic agent or detectable label.
Dependencies are inferred from the claim text.