Sibi et al. reported an enantioselective rhodium catalysed enolate protonation method for the synthesis of β²-amino acid (Scheme 4). Rh(acac)(ethylene) 2 and difluorophos used to form a complex which catalyzed the conjugate addition of aryl boronic acids to β-acrylates. The intermediate oxa-β-allyl-Rh resulted in good yields using one equivalent of phthalimideas proton source [15].
Abstractβ-amino acids are an important class of macromolecules. They play role in life for survival. β-amino acids gained significant interest due to their interesting pharmaceutical uses as hypoglycemic, antiketogenic characteristics, sterile and antifungal activities, anthelminthic as well as potent insecticidal characteristics. These are vital building blocks for the preparation of pharmaceutical and agrochemical target molecules. These are utilized in development of drugs, bimolecular structure and molecular recognition. They are also important in treatment of different diseases which are viral to human health. They play important role in regulation of nutritional metabolism and immunity. It has also led to their wider adoption as intermediates in new drugs and has been a focus of considerable attention in medicinal chemistry. β-amino acids have found extensive applications as components of biologically active peptides and small molecule pharmaceuticals. Synthetic derivatives of biologically relevant peptides incorporating β-amino acids often display interesting pharmacological activity, with increased potency and enzymatic stability. β-peptides participate in arrangement of incredible stable auxiliary structures. This review summarizes recent developments about the different roles of β-amino acids in human biology and some implications in medicinal chemistry.
Molecularly imprinted biodegradable polymers are receiving
considerable
attention in drug delivery due to their ability of targeted recognition
and biocompatibility. This study reports the synthesis of a novel
fluorescence-active magnetic molecularly imprinted drug carrier (MIDC)
using a glucose-based biodegradable cross-linking agent for the delivery
of anticancer drug docetaxel. The magnetic molecularly imprinted polymer
(MMIP) was characterized through scanning electron microscopy (SEM),
Fourier transform infrared spectroscopy (FTIR), X-ray diffraction
spectroscopy, and vibrating sample magnetometry (VSM). The MMIP presented
a magnetization value of 0.0059 emu g
–1
and binding
capacity of 72 mg g
–1
with docetaxel.
In
vitro
and
in vivo
studies were performed
to observe the effectiveness of the MIDC for drug delivery. The cell
viability assay suggested that the MMIP did not present toxic effects
on healthy cells. The magnetic property of the MMIP allowed quick
identification of the drug carrier at the target site by applying
the external magnetic field to mice (after 20 min of loading) and
taking X-ray images. The novel MMIP-based drug carrier could thus
deliver the drug at the target site without affecting the healthy
cells.
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