Synthesis and biomedical potential of azapeptide modulators of the cluster of differentiation 36 receptor (CD36)

C Proulx, J Zhang, D Sabatino, S Chemtob, H Ong… - Biomedicines, 2020 - mdpi.com
The innovative development of azapeptide analogues of growth hormone releasing peptide-
6 (GHRP-6) has produced selective modulators of the cluster of differentiation 36 receptor …

Azapeptides as an Efficient Tool to Improve the Activity of Biologically Effective Peptides

K Tarchoun, M Yousef, Z Bánóczi - Future Pharmacology, 2022 - mdpi.com
Peptides are highly potent biological active compounds with excellent selectivity and
binding, but they have some drawbacks (eg, low stability in vivo because of the enzymatic …

Diversity‐Oriented Synthesis of Cyclic Azapeptides by A3‐Macrocyclization Provides High‐Affinity CD36‐Modulating Peptidomimetics

J Zhang, M Mulumba, H Ong… - Angewandte Chemie …, 2017 - Wiley Online Library
Macrocyclization has enabled the use of peptides in drug discovery creating a need for
methods to synthesize diverse peptide macrocycles. Azapeptides have advanced to …

Controlling chemoselectivity in copper-catalyzed decarboxylative A 3/A 3 cross-couplings: direct formation of unsymmetrical 1, 4-diamino-2-butynes

P Zhao, H Feng, H Pan, Z Sun, M Tong - Organic Chemistry Frontiers, 2017 - pubs.rsc.org
A direct cross-coupling of propiolic acid with two kinds of in situ formed iminiums has been
achieved via the CuI/CuCl2-catalyzed decarboxylative A3/A3 domino process. This novel …

Azapeptides-A history of synthetic milestones and key examples

K Fan Cheng, S VanPatten, M He… - Current Medicinal …, 2022 - ingentaconnect.com
For over 50 years of azapeptide synthetic techniques, developments have renewed the field
of peptidomimetic therapeutics. Azapeptides are close surrogates of natural peptides: they …

[PDF][PDF] A review on Azapeptides: the promising Peptidomimetics

A Begum, D Sujatha, K Prasad, K Bharathi - Asian J. Chem, 2017 - researchgate.net
Peptidomimetics, the mimics of natural peptides are considered as promising therapeutics
with potential applications in modern medicine. Among the various structural variants of …

Computational investigation of conformational properties of short azapeptides: Insights from DFT study and NBO analysis

M El Khabchi, M Mcharfi, M Benzakour, A Fitri… - Molecules, 2023 - mdpi.com
Azapeptides have gained much attention due to their ability to enhance the stability and
bioavailability of peptide drugs. Their structural preferences, essential to understanding their …

Highly Selective Synergistic Copper(I/II)‐Catalyzed A3 Cross Coupling/Decarboxylative A3 Domino Reactions in Water

H Feng, P Zhao, L Huang, Z Sun… - Asian Journal of Organic …, 2017 - Wiley Online Library
A microwave‐assisted copper‐catalyzed A3 cross‐coupling/decarboxylative A3 domino
reaction of a propiolic acid, an aldehyde, a formaldehyde solution and an amine is …

Comparison of various coupling reagents in solid-phase aza-peptide synthesis

M Arujõe, A Ploom, A Mastitski, J Järv - Tetrahedron Letters, 2017 - Elsevier
Aza-peptides are promising drug leads, however extensive study of their properties is
hampered by low yielding aza-peptide bond formation during conventional Fmoc SPPS. The …

A general and convenient synthesis of 4-(tosylmethyl) semicarbazones and their use in amidoalkylation of hydrogen, heteroatom, and carbon nucleophiles

AA Fesenko, AN Yankov, AD Shutalev - Tetrahedron, 2019 - Elsevier
A general synthesis of previously unknown semicarbazone-based α-amidoalkylating
reagents, 4-(tosylmethyl) semicarbazones, has been developed. The synthesis involved …