Novel glycosylated VIP analogs: synthesis, biological activity, and metabolic stability

2008 ◽  
Vol 14 (3) ◽  
pp. 321-328 ◽  
Author(s):  
David Dangoor ◽  
Barbara Biondi ◽  
Marina Gobbo ◽  
Yelena Vachutinski ◽  
Mati Fridkin ◽  
...  
Keyword(s):  
Biological Activity ◽  
Metabolic Stability

Inhibitors of cytosolic phospholipase A2α with carbamate structure: synthesis, biological activity, metabolic stability, and bioavailability

2014 ◽  
Vol 23 (12) ◽  
pp. 5250-5262 ◽  
Author(s):  
Julian Schwarzkopf ◽  
Tom Sundermann ◽  
Martina Arnsmann ◽  
Walburga Hanekamp ◽  
Jörg Fabian ◽  
...  
Keyword(s):  
Biological Activity ◽  
Metabolic Stability ◽  
Cytosolic Phospholipase ◽  
Structure Synthesis ◽  
Cytosolic Phospholipase A2α

ω-Imidazolyl- and ω-Tetrazolylalkylcarbamates as Inhibitors of Fatty Acid Amide Hydrolase: Biological Activity and in vitro Metabolic Stability

ChemMedChem ◽  
2016 ◽  
Vol 11 (4) ◽  
pp. 429-443 ◽  
Author(s):  
Tobias Terwege ◽  
Walburga Hanekamp ◽  
David Garzinsky ◽  
Simone König ◽  
Oliver Koch ◽  
...  
Keyword(s):  
Biological Activity ◽  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Metabolic Stability ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

In vitroandin vivocharacterization of an interleukin-15 antagonist peptide by metabolic stability,99mTc-labeling, and biological activity assays

2018 ◽  
Vol 24 (4-5) ◽  
pp. e3078 ◽  
Author(s):  
Yunier Rodríguez-Álvarez ◽  
Ania Cabrales-Rico ◽  
Alejandro Perera-Pintado ◽  
Anais Prats-Capote ◽  
Hilda E. Garay-Pérez ◽  
...  
Keyword(s):  
Biological Activity ◽  
Metabolic Stability ◽  
Interleukin 15 ◽  
99Mtc Labeling

scholarly journals Increasing the bioactive space of peptide macrocycles by thioamide substitution

2018 ◽  
Vol 9 (9) ◽  
pp. 2443-2451 ◽  
Author(s):  
Hitesh Verma ◽  
Bhavesh Khatri ◽  
Sohini Chakraborti ◽  
Jayanta Chatterjee
Keyword(s):  
Biological Activity ◽  
Metabolic Stability ◽  
Conformational Rigidity ◽  
Macrocyclic Peptides

Thioamide substitution into macrocyclic peptides increases the conformational rigidity of the backbone resulting in enhanced biological activity and metabolic stability.

Design, synthesis, and biological activity of novel factor Xa inhibitors: Improving metabolic stability by S1 and S4 ligand modification

2006 ◽  
Vol 14 (5) ◽  
pp. 1309-1330 ◽  
Author(s):  
Satoshi Komoriya ◽  
Shozo Kobayashi ◽  
Ken Osanai ◽  
Toshiharu Yoshino ◽  
Tsutomu Nagata ◽  
...  
Keyword(s):  
Biological Activity ◽  
Factor Xa ◽  
Metabolic Stability ◽  
Factor Xa Inhibitors ◽  
Design Synthesis ◽  
Ligand Modification

scholarly journals Macrolactam analogues of macrolide natural products

2016 ◽  
Vol 14 (48) ◽  
pp. 11301-11316 ◽  
Author(s):  
Helmut M. Hügel ◽  
Andrew T. Smith ◽  
Mark A. Rizzacasa
Keyword(s):  
Natural Products ◽  
Biological Activity ◽  
Chemical Modification ◽  
Metabolic Stability

The chemical modification of macrolide natural products into aza- or lactam analogues is a strategy employed to improve their metabolic stability and biological activity.

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