132622-81-2

Usage

Uses

Used in Pharmaceutical Industry:
(2R,4R)-4-(aMinoMethyl)-1-(tert-butoxycarbonyl)pyrrolidine-2-carboxylic acid is used as a building block for the development of peptide-based therapeutics, contributing to the creation of novel drugs with specific targeting and therapeutic properties.
Used in Biotechnology Industry:
(2R,4R)-4-(aMinoMethyl)-1-(tert-butoxycarbonyl)pyrrolidine-2-carboxylic acid is used as a component in the synthesis of peptidomimetics, which are analogs of peptides with modified structures that can enhance stability and bioavailability, making them valuable for diagnostic and therapeutic applications.

Upstream product

• 77449-94-6 (2R,4R)-4-hydroxypyrrolidine-2-carboxylic acid hydrochloride 
• 77449-99-1 (2R,4R)-2-ethoxycarbonyl-4-hydroxypyrrolidine hydrochloride 
• 132622-75-4 (4R)-1-(tert-butoxycarbonyl)-4-<(methylsulfonyl)oxy>-D-proline ethyl ester 
• 132623-07-5 trans-1-(tert-butoxycarbonyl)-4-cyano-D-proline ethyl ester 
• 77450-00-1 (2R,4R)-4-hydroxyproline-1,2-dicarboxylic acid 1-tert-butyl 2-ethyl ester 
• 132622-80-1 (4S)-1-(tert-butoxycarbonyl)-4-cyano-D-proline 

Downstream Products

• 132622-82-3 (4S)-1-(tert-butoxycarbonyl)-4-<<<<(p-toluenesulfonyl)imino>aminomethyl>amino>methyl>-D-proline 

Relevant academic research and scientific papers

A Tobramycin Vector Enhances Synergy and Efficacy of Efflux Pump Inhibitors against Multidrug-Resistant Gram-Negative Bacteria

Drug efflux mechanisms interact synergistically with the outer membrane permeability barrier of Gram-negative bacteria, leading to intrinsic resistance that presents a major challenge for antibiotic drug development. Efflux pump inhibitors (EPIs) which block the efflux of antibiotics synergize antibiotics, but the clinical development of EPI/antibiotic combination therapy to treat multidrug-resistant (MDR) Gram-negative infections has been challenging. This is in part caused by the inefficiency of current EPIs to penetrate the outer membrane and resist efflux. We demonstrate that conjugation of a tobramycin (TOB) vector to EPIs like NMP, paroxetine, or DBP enhances synergy and efficacy of EPIs in combination with tetracycline antibiotics against MDR Gram-negative bacteria including Pseudomonas aeruginosa. Besides potentiating tetracycline antibiotics, TOB-EPI conjugates can also suppress resistance development to the tetracycline antibiotic minocycline, thereby providing a strategy to develop more effective adjuvants to rescue tetracycline antibiotics from resistance in MDR Gram-negative bacteria.

Conformationally Restricted Arginine Analogues

We report the practical synthesis and structural characterization of a set of conformationally constrained protected arginine analogues.These enantiomerically pure analogues have the general structure 1 and are prepared in seven to eight steps from the co