Constricting the peptide backbone into a more defined conformational form through cyclization is an activity evolved in nature and in synthetic work, the latter straddling only the most recent decades. The resulting conformational constraints increase the probability of an optimum response with bio-receptors. The purpose of this review is to highlight developments that have proved to be reasonably efficient in the macrocyclization of linear precursors into cyclic peptides and depsipeptides.

https://onlinelibrary.wiley.com/doi/pdf/10.1002/psc.491

The cyclization of peptides and depsipeptides

Synthesis of some new [1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and [1,2,4]triazolo[3,4-b][1,3,4] thiadiazoles starting from 5-nitro-2-furoic acid and evaluation of their antimicrobial activity

On-bead cyclization in a combinatorial library of 15,625 octapeptides.

A series of N-phenyl-substituted and disubstituted guanidinyl benzothiazole derivatives 4a–4m were synthesized and characterized as novel antimicrobial and antioxidant agents. The in-vitro antioxidant activities of these compounds were evaluated and compared with commercial antioxidants, using ascorbic acid (AA) and employing 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and 2,2′-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid (ABTS) assay. The results showed that IC50 values of compounds 4a and 4m were similar to the IC50 values of the standard. This assay indicates the good activities of these compounds. In addition, the in-vitro antimicrobial activities of these compounds were evaluated and the results demonstrated that the compounds 4i and 4l exhibited excellent antimicrobial activities. Compounds 4c and 4i having electron withdrawing groups at p-position and compound 4l and 4m having electron donating groups at o-position showed better antimicrobial activities compared to the standard.

Guanidinyl benzothiazole derivatives: Synthesis and structure activity relationship studies of a novel series of potential antimicrobial and antioxidants

Synthetic studies on cyclic octapeptides: Yunnanin F and Hymenistatin.

A series of new furanopeptides (3) are prepared by the coupling of arylsubstituted furoic acids (1) with amino acid methyl esters, di and tetra-peptide methyl esters using dicyclohexyl carbodiimide (DCC) as coupling agent. Some of the newly synthesized compounds are characterized on the basis of IR, 1H NMR, mass spectral data and elemental analysis. Some of the selected compounds are also tested for their antibacterial properties.

Synthetic and antibacterial studies on some new furanopeptides.

Synthesis and biological evaluation of Pseudostellarin D

A new potent bioactive cyclic peptide pseudostellarin B has been synthesised The structure was elucidated by elemental analyses, IR, 1H NMR, 13C NMR and FAB mass spectral data The synthesised compound was also screened for its antibacterial, antifungal, antiinflammatory and anthelmintic activities

Synthesis and biological evaluation of pseudostellarin B

A new biologically active cyclic peptide, Pseudostellarin G was synthesized and the structure was established on the basis of analytical, IR, NMR and mass spectral data. The newly synthesized compound was screened for its antimicrobial and pharmacological activities.

/pdf/synthesis-of-a-new-cyclic-peptide-pseudostellarin-g-1ff0hvemsm.pdf

Synthesis of a new cyclic peptide, Pseudostellarin G

Synthetic studies on pseudostellarin a

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