So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Jain, Priyesh; Badger, David B.; Liang, Yi; Gebhard, Anthony W.; Santiago, Daniel; Murray, Philip; Kaulagari, Sridhar R.; Gauthier, Ted J.; Nair, Rajesh; Kumar, MohanRaja; Guida, Wayne C.; Hazlehurst, Lori A.; McLaughlin, Mark L. researched the compound: Boc-D-Prolinol( cas:83435-58-9 ).Safety of Boc-D-Prolinol.They published the article 《Bioactivity improvement via display of the hydrophobic core of HYD1 in a cyclic β-hairpin-like scaffold, MTI-101》 about this compound( cas:83435-58-9 ) in Peptide Science (Hoboken, NJ, United States). Keywords: cyclic peptidomimetic synthesis bioavailability antitumor structure activity; solid phase peptide synthesis macrocyclization; mol structure cyclic peptidomimetic NMR hairpin conformation. We’ll tell you more about this compound (cas:83435-58-9).
HYD1 is an all D-amino acid linear 10-mer peptide that was discovered by one-bead-one-compound screening. HYD1 has five hydrophobic amino acids flanked by polar amino acids. Alanine scanning studies showed that alternating hydrophobic amino acid residues and N- and C-terminal lysine side chains were contributors to the biol. activity of the linear 10-mer analogs. This observation led us to hypothesize that display of the hydrophobic pentapeptide sequence of HYD1 in a cyclic beta-hairpin-like scaffold could lead to better bioavailability and biol. activity. An amphipathic pentapeptide sequence was used to form an antiparallel strand and those strands were linked via dipeptide-like sequences selected to promote β-turns. Early cyclic analogs were more active but otherwise mimicked the biol. activity of the linear HYD1 peptide. The cyclic peptidomimetics were synthesized using standard Fmoc solid phase synthesis (Fmoc = 9-fluorenylmethoxycarbonyl) to form linear peptides, followed by solution phase or on-resin cyclization. SAR studies were carried out with an aim to increase the potency of these drug candidates for the killing of multiple myeloma cells in vitro. The solution structures of cyclic peptidomimetics were elucidated using NMR spectroscopy. 1H NMR and 2D TOCSY studies of these peptides revealed a downfield Hα proton chem. shift and 2D NOE spectral anal. consistent with a β-hairpin-like structure.
There is still a lot of research devoted to this compound(SMILES：O=C(N1[C@@H](CO)CCC1)OC(C)(C)C)Safety of Boc-D-Prolinol, and with the development of science, more effects of this compound(83435-58-9) can be discovered.
Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica