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15 Σεπ 2019 · This digest highlights the applications of most commonly employed amide isosteres in drug design aiming at improving potency and selectivity, optimizing physicochemical and pharmacokinetic properties, eliminating or modifying toxicophores, as well as providing novel intellectual property of lead compounds.
- Bioactive Hydroxyethylene Dipeptide Isosteres With Hydrophobic
The design and synthesis of new truncated δ-amino...
- Discovery of Isoxazole Voltage Gated Sodium Channel Blockers for Treatment of Chronic Pain
As shown in Table 1, substitution on the benzylic position...
- Potent and Selective Isophthalamide S2 Hydroxyethylamine Inhibitors of Bace1
Increasing the alkyl chain length of the C-5 amide to propyl...
- Rational Design of Novel, Potent Piperazinone and Imidazolidinone Bace1 Inhibitors
Stereoselective synthesis of these new inhibitors beginning...
- Benzamide Derivatives as Blockers of Kv1.3 Ion Channel
The trans alcohol 16 was prepared from 11.The amino group of...
- Piperazine Sulfonamide Bace1 Inhibitors
Synthesis of these novel inhibitors began with a...
- Cgrp
Given the promising attributes of 2, extensive SAR was...
- Pharmacological Characterization of Benzodiazepine Receptors in The Brain
Receptors in rat brain membranes which specifically bind 3...
- Bioactive Hydroxyethylene Dipeptide Isosteres With Hydrophobic
15 Σεπ 2019 · This digest highlights the applications of most commonly employed amide isosteres in drug design aiming at improving potency and selectivity, optimizing physicochemical and pharmacokinetic properties, eliminating or …
20 Ιουλ 2020 · Herein, we review the strategic decisions in selecting an amide bioisostere (the why), synthetic routes to each (the how), and success stories of each bioisostere (the implementation) to provide a comprehensive overview of this important toolbox for medicinal chemists.
BOMI 57 and BDMP 58 showed the best results, achieving 490% conversion within 10 min during the coupling of Z-Gly-Phe-OH with H-Val-OMe (Anteunis test). In addition, epimerisation was low, BOMI 57 displaying 3.1% and BDMP 58 2.3% of the DL-isomer.
2 ημέρες πριν · We conducted a fundamental evaluation of the 3 Screen ICA ELISA kit, which can simultaneously measure three major anti-islet autoantibodies important in diagnosing and predicting type 1 diabetes, to assess its usefulness as a measuring reagent. In autoantibody-positive samples, the coefficient of variation for intra-assay variation ranged from 1.37% to 2.50%, inter-assay variation from 2.81% ...
The current resurgence of electrosynthesis has led to new and more sustainable syntheses of (and using) amides to be published in recent times. As such, this tutorial review aims to highlight these reactions.
15 Νοε 2015 · This review showcases various coupling reagents which have been implemented specifically for large-scale amide synthesis via the condensation of an acid and amine, while highlighting the benefits and drawbacks of each reagent on an industrial scale.
