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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
The X-ray crystal structure of 19d in the BACE1 enzyme shows...
- 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
7 Απρ 2022 · A variety of protocols for amide/peptide bond formation in water as the bulk medium have recently emerged, enabling the removal of undesirable reprotoxic solvents.
Palmitoylethanolamide (PEA) is an endocannabinoid-like lipid mediator with extensively documented anti-inflammatory, analgesic, antimicrobial, immunomodulatory and neuroprotective effects. It is well tolerated and devoid of side effects in animals and humans.
11 Ιαν 2022 · Find your flow: This Review summarizes and compares flow-aided methodologies for basic amide formation, peptide synthesis, and peptidomimetic framework generation. Beyond describing the technological...
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.
1 Σεπ 2020 · Another strategy for electrochemically preparing amides is the use of a nitrile group and water. Often this can be achieved through the use of mixed solvent systems (particularly MeCN/H 2 O), making these reactions quite efficient and sustainable.
16 Ιαν 2019 · Chlorination is the most commonly used disinfection process to pretreat the water to reduce biofouling. Although chlorination is widely used, it has several disadvantages, such as formation of...
