Dipeptides as linker for multicomponent presentation —a facile, robust, and high-bioactivity yielding strategy

AbstractThe need for multiple drugs arises when the response to pharmacological inflection is complicated and the disease conditions get worsened. The treatment requires a common platform to which multiple drugs are linked and this methodology is proven to be useful in drug delivery, biomaterial research, biomedicine, and vaccine development. In view of this, the present work is centered on dipeptides (KW/ KD/ KE/ kW/ kD/ kE), which are used as linkers and can potentially hold different functional group containing molecules (here, amino and carboxyl). First, we have demonstrated the incorporation of three components to the linker successfully followed by tetra component linking to those dipeptides, which contain trifunctional groups. To provide a proof of concept, these multisubstituted constructs were subjected to microbial growth suppression assay as well as anti-inflammatory assay. The biological results revealed that the multimers play a key role in enhancing the activity. Hence, the present system may be regarded as simple and straight forward which can be employed to develop various therapeutic agents as well as in different methodologies.

Source: Medicinal Chemistry Research - April 17, 2018 Category: Chemistry Source Type: research