193206-49-4Relevant articles and documents
PENICILLIN-BINDING PROTEIN INHIBITORS
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Paragraph 00208, (2021/06/04)
Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds describ
A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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Page/Page column 12; 214-215, (2019/07/17)
The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
Polyamidoamines as drug carriers: Synthesis of polymers featuring extrachain-type primary amino groups as drug-anchoring sites
N'Da, David D.,Neuse, Eberhard W.
, p. 65 - 70 (2007/10/03)
The versatile polymerization of bisacrylamides with mono- and difunctional amines, first investigated and greatly expanded in Ferruti's laboratory, 1-3 is utilized in the present project for the synthesis of macromolecular drug carriers. Specifically, we report on the preparation of linear polyamidoamines possessing primary amino groups as terminals of short side chains, designed to function as drug attachment sites. In the first reaction step, performed in aqueous medium, methylenebisacrylamide (MBA) is copolymerized with two types of comonomer: (1) primary amines bearing solubilizing functionality, such as tert-amine or hydroxyl groups, and (2) a variety of mono-N-Boc-protected primary diamines (Boc = tert-butoxycarbonyl). In other reactions, MBA is allowed to react with a mono-N-protected diamine to give a macromonomer, which is polymerized with an oligo- or poly(ethylene oxide) terminated at both ends by a primary amino group. The intermediary polymers so obtained, as yet featuring N-protected amino side groups, are treated with trifluoroacetic acid for deprotection. Further work-up by aqueous dialysis (25 000 mwco tubing) and freeze-drying affords the target polymers as water- and methanol-soluble solids in ultimate yields of 10-25%. 1H NMR spectroscopy serves to confirm the structural assignments 1-12. In order to demonstrate the drug-carrying potential of these polymers, an exemplifying polyamidoamine (11) is allowed to react with an active ester of 4-ferrocenylbutanoic acid in methanolic solution. A water-soluble conjugate (11-Fc) is thus obtained, in which 93% of available primary amine side-chain terminals are acylated by the ferrocenylation agent.