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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
A survey of SAR around the lead 1 was carried out. A few...
- 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 · Isosteric replacement of amide groups is a classic practice in medicinal chemistry. 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 ….
A voltage-gated sodium channel blocker used for management of atrial or ventricular fibrillation, atrial flutter, and ventricular tachycardia, that is no longer used due to proarrhythmic adverse effects.
6 ημέρες πριν · Amide, any member of either of two classes of nitrogen-containing compounds related to ammonia and amines. The two classes are covalent amides, which are neutral or very weakly acidic substances, and ionic amides, which are strongly alkaline compounds.
Amide is a functional group in organic molecules that consists of an acyl group linked to a nitrogen atom. It provides structural rigidity and resistance to hydrolysis, and is found in proteins and drugs. It is formed through the reaction of a carboxylic acid with an amine or ammonia.
Applications. Amides are pervasive in nature and technology. Proteins and important plastics like nylons, aramids, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis.
10 Οκτ 2016 · Abstract. Amides are widespread in biologically active compounds with a broad range of applications in biotechnology, agriculture and medicine. Therefore, as alternative to chemical synthesis the biocatalytic amide synthesis is a very interesting field of research.
