Unknown

Dataset Information

0

Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors.

ABSTRACT: Comprehensive synthetic strategies afforded a diverse set of structurally unique bicyclic proline-containing arginase inhibitors with a high degree of three-dimensionality. The analogs that favored the Cγ-exo conformation of the proline improved the arginase potency over the initial lead. The novel synthetic strategies reported here not only enable access to previously unknown stereochemically complex proline derivatives but also provide a foundation for the future synthesis of bicyclic proline analogs, which incorporate inherent three-dimensional character into building blocks, medicine, and catalysts and could have a profound impact on the conformation of proline-containing peptides and macrocycles.

SUBMITTER: Li D 

PROVIDER: S-EPMC8591728 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Comprehensive synthetic strategies afforded a diverse set of structurally unique bicyclic proline-containing arginase inhibitors with a high degree of three-dimensionality. The analogs that favored the Cγ-exo conformation of the proline improved the arginase potency over the initial lead. The novel synthetic strategies reported here not only enable access to previously unknown stereochemically complex proline derivatives but also provide a foundation for the future synthesis of bicyclic proline  ...[more]

Similar Datasets

Unknown 3-Substituted prolines: from synthesis to structural applications, from peptides to foldamers.
| S-EPMC6270394 | biostudies-literature
Unknown Synthesis of potent bicyclic bisarylimidazole c-Jun N-terminal kinase inhibitors by catalytic C-H bond activation.
| S-EPMC2556147 | biostudies-literature
Unknown Nature Inspired Molecular Design: Stereoselective Synthesis of Bicyclic and Polycyclic Ethers for Potent HIV-1 Protease Inhibitors.
| S-EPMC6781882 | biostudies-literature
Unknown Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.
| S-EPMC7153280 | biostudies-literature
Unknown The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors.
| S-EPMC8591741 | biostudies-literature
Unknown Discovery and Pharmacokinetics of Sulfamides and Guanidines as Potent Human Arginase 1 Inhibitors.
| S-EPMC7153016 | biostudies-literature
Unknown Discovery and crystallography of bicyclic arylaminoazines as potent inhibitors of HIV-1 reverse transcriptase.
| S-EPMC4607639 | biostudies-literature
Unknown C-3- and C-4-Substituted Bicyclic Coumarin Sulfamates as Potent Steroid Sulfatase Inhibitors.
| S-EPMC6173509 | biostudies-literature
Unknown Synthesis, evaluation and molecular modelling of piceatannol analogues as arginase inhibitors.
| S-EPMC7593889 | biostudies-literature
Other Synthesis of immunogenicity-free RNA circles as potent PKR inhibitors
2021-12-23 | GSE183941 | GEO