Fluorine and fluorinated motifs in the design and application of bioisosteres for drug design
NA Meanwell - Journal of medicinal chemistry, 2018 - ACS Publications
The electronic properties and relatively small size of fluorine endow it with considerable
versatility as a bioisostere and it has found application as a substitute for lone pairs of …
versatility as a bioisostere and it has found application as a substitute for lone pairs of …
N-Acylethanolamine Acid Amidase (NAAA): Structure, Function, and Inhibition
N-Acylethanolamine acid amidase (NAAA) is an N-terminal cysteine hydrolase primarily
found in the endosomal–lysosomal compartment of innate and adaptive immune cells …
found in the endosomal–lysosomal compartment of innate and adaptive immune cells …
Diverse functionalization of strong alkyl C–H bonds by undirected borylation
The selective functionalization of strong, typically inert carbon-hydrogen (C–H) bonds in
organic molecules is changing synthetic chemistry. However, the undirected …
organic molecules is changing synthetic chemistry. However, the undirected …
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors
W Tuo, N Leleu-Chavain, J Spencer… - Journal of medicinal …, 2017 - ACS Publications
Fatty acid ethanolamides (FAEs) and endocannabinoids (ECs) have been shown to
alleviate pain and inflammation, regulate motility and appetite, and produce anticancer …
alleviate pain and inflammation, regulate motility and appetite, and produce anticancer …
HFIP solvent enables alcohols to act as alkylating agents in stereoselective heterocyclization
Y Zhu, I Colomer, AL Thompson… - Journal of the American …, 2019 - ACS Publications
A new method for the stereoselective synthesis of highly functionalized oxygen heterocycles
using allyl or benzyl alcohols as alkylating agents is presented. The process is efficient and …
using allyl or benzyl alcohols as alkylating agents is presented. The process is efficient and …
β-Lactams as promising anticancer agents: Molecular hybrids, structure activity relationships and potential targets
DJ Fu, YF Zhang, AQ Chang, J Li - European Journal of Medicinal …, 2020 - Elsevier
Abstract β-Lactam, commonly referred as azetidin-2-one, is a multifunctional building block
for synthesizing β-amino ketones, γ-amino alcohols, and other compounds. Besides its well …
for synthesizing β-amino ketones, γ-amino alcohols, and other compounds. Besides its well …
Molecular mechanism of activation of the immunoregulatory amidase NAAA
Palmitoylethanolamide is a bioactive lipid that strongly alleviates pain and inflammation in
animal models and in humans. Its signaling activity is terminated through degradation by N …
animal models and in humans. Its signaling activity is terminated through degradation by N …
N-acylethanolamine hydrolyzing acid amidase inhibition: tools and potential therapeutic opportunities
P Bottemanne, GG Muccioli, M Alhouayek - Drug discovery today, 2018 - Elsevier
Highlights•NAAA is a key enzyme controlling the levels of bioactive N-acylethanolamines.•
Novel, systemically active inhibitors are now available to study NAAA roles in vivo.•NAAA …
Novel, systemically active inhibitors are now available to study NAAA roles in vivo.•NAAA …
Peptide-β-lactam inhibitors of dengue and west nile virus NS2B-NS3 protease display two distinct binding modes
T Dražić, S Kopf, J Corridan… - Journal of medicinal …, 2019 - ACS Publications
The β-lactam ring represents a valuable moiety that can induce covalent binding of an
inhibitor to its target. In this study, we explored di-and tripeptides with β-lactam electrophilic …
inhibitor to its target. In this study, we explored di-and tripeptides with β-lactam electrophilic …
Active compound analysis of ethanolic extract of roselle calyces (Hibiscus sabdariffa L.)
SBS Arunasalam, N Karthikeyan, A Thangaiah… - Quality Assurance and …, 2023 - qascf.com
Roselle (Hibiscus sabdariffa L.) is a comestible plant known for its fleshy red calyces that are
used in making a wide range of foods such as wine, juice, jam, syrup, pudding, cakes, ice …
used in making a wide range of foods such as wine, juice, jam, syrup, pudding, cakes, ice …