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Chalcone (1,3-Diphenyl-2-Propene-1-One) Scaffold Bearing Natural Compounds as Nitric Oxide Inhibitors: Promising Antiedema Agents
Published in Debarshi Kar Mahapatra, Cristóbal Noé Aguilar, A. K. Haghi, Applied Pharmaceutical Practice and Nutraceuticals, 2021
Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Vivek Asati
Chemical reactions play a major role in the journey of chalcones.27 It interchanges into flavonoids in the presence of acid and the reversal into flavanone occurs by base.28 This scaffold serves as a template structure for the elucidation of flavanones, tannins, flavonoids, and chromanochro-manes.29 Nonpharmacological utilization such as insecticides, scintillator, sweeteners in confectionaries, polymerization agents in product development, chemosensor for detection, catalyst in specific reactions, chromophores in dying industries, fluorescent polymeric agents, fluorescent whitening agent, etc. have been reported.30 Numerous traditional high-yield methods such as Suzuki–Miyaura reaction, Claisen–Schmidt reaction, Julia–Kocienski reaction, Friedel–Crafts reaction, Sonogashira isomerization coupling, one-pot reactions, direct crossed-coupling reaction, microwave-assisted reactions, solvent-free reactions, carbonylative Heck coupling reaction, solid acid catalyst mediated reactions, etc. have been into applications in industrial-scale and academic-scale.31,32
Heat Shock Protein 90 (Hsp90) Inhibitory Potentials of Some Chalcone Compounds as Novel Anti-Proliferative Candidates
Published in P. Mereena Luke, K. R. Dhanya, Didier Rouxel, Nandakumar Kalarikkal, Sabu Thomas, Advanced Studies in Experimental and Clinical Medicine, 2021
Debarshi Kar Mahapatra, Sayan Dutta Gupta, Sanjay Kumar Bharti, Tomy Muringayil Joseph, Józef T. Haponiuk, Sabu Thomas
Chalcones (Figure 5.5) are the abundantly present natural products class in nature either in free or in diverse complexed forms. The term chalcone was coined by Kostanecki and Tambor in the 19th century who first synthesized these chromophoric compounds. The term originated from the word of Greek origin “chalcos” which means “bronze,” named after the bronze-like color of the natural chalcones [33]. The prop-2-ene-1-one scaffold comprising of two aromatic rings attached together with a three carbon α, β unsaturated carbonyl bridge. It has received attention among the research community owing to a large number of merits such as easy steps for laboratory-oriented synthesis via diverse procedures such as direct crossed-coupling reaction, Julia-Kocienski reaction, carbonylated Heck coupling reaction, Suzuki-Miyaura reaction, Sonogashira isomerization coupling, microwave-assisted reactions, solid acid catalyst mediated reactions, Friedel-Crafts reaction, one-pot reactions, solvent-free reactions, etc., [34].
Receptors for Neuropeptides: Receptor Isolation Studies and Molecular Biology
Published in Edwin E. Daniel, Neuropeptide Function in the Gastrointestinal Tract, 2019
Jean-Pierre Vincent, Patrick Kitabgi
The most important quality of an affinity gel is its receptor binding capacity. It is therefore necessary to achieve maximum efficiency in the coupling reaction. For this reason, neurotensin2—13 (which contains two reactive amine functions) was preferred over neurotensin1—13 (whose N-terminal residue is pGlu) for the preparation of an affinity gel designed for purification of the neurotensin receptor. The yield of covalent binding to glutaraldehyde-activated AcA22 was found to be 50 to 70% for neurotensin2_13 as compared to only 20 to 30% for the native peptide. Moreover, the affinity of the (2 — 13) sequence for the neurotensin receptor is slightly better than that of neurotensin itself.5
An update on late-stage functionalization in today’s drug discovery
Published in Expert Opinion on Drug Discovery, 2023
Andrew P. Montgomery, Jack M. Joyce, Jonathan J. Danon, Michael Kassiou
Organic synthesis is essential to modern drug design, allowing chemists to modify natural products or establish structure–activity relationships (SAR) to improve the pharmacological profile of bioactive compounds [1]. Late-stage diversification is an important paradigm in organic synthesis planning, as delaying key divergent chemical transformations until the end of a synthesis has the capacity to significantly reduce the synthetic effort required when generating molecular libraries. C–C and C–N cross-coupling reactions are established synthetic methodologies for divergent synthesis, which have allowed vast libraries to be generated with ease from pre-functionalized fragments [2]. However, cross-coupling methodology has historically favored the production of sp2 – sp2 linkages leading to an over-representation of flat, aromatic compounds in drug discovery representing a restricted chemical space and even a reduction in the developability of drug candidates [3–5]. The development of methodologies to selectively functionalize C–H bonds traditionally considered to be unreactive has provided organic chemists with new and unique classes of chemical transformations and increased flexibility in synthesis planning.
Transferrin receptor-mediated liposomal drug delivery: recent trends in targeted therapy of cancer
Published in Expert Opinion on Drug Delivery, 2022
Solmaz Mojarad-Jabali, Somayeh Mahdinloo, Masoud Farshbaf, Muhammad Sarfraz, Yousef Fatahi, Fatemeh Atyabi, Hadi Valizadeh
EDC/NHS coupling chemistry is also broadly used to conjugate the primary amino group of one moiety to the carboxyl group of the other one. When the carboxyl group of a targeting ligand is activated by 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and N-hydroxysuccinimide (NHS), it rapidly reacts with phospholipid-PEG-NH2via nucleophilic substitution reaction to form a stable amide bond. Similarly, phospholipid-PEG-COOH can also be activated by EDC/NHS to react with the amino group of a targeting ligand. Generally, EDC/NHS coupling reaction occurs faster in a weak acid solution (pH 6.0–6.5) [121,122]. Nevertheless, in some cases, the conjugation reaction of several targeting moieties and PEGylated phospholipids was performed in alkaline solutions (pH 7.5–10.0) [123].
Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracer
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Jonathan Elie, Johnny Vercouillie, Nicolas Arlicot, Lucas Lemaire, Rudy Bidault, Sylvie Bodard, Christel Hosselet, Jean-Bernard Deloye, Sylvie Chalon, Patrick Emond, Denis Guilloteau, Frédéric Buron, Sylvain Routier
The bromination step occurred smoothly and the desired products 11–13 were isolated in excellent yields. For the next C-3 (het)arylations, we successfully achieved the Suzuki-Miyaura cross-coupling reactions using several commercially available arylboronic acids (1.2 equiv.) under classical conditions15–17. The desired products 14–27 were isolated in moderate to excellent yields (Table 2). Most of the reactions appeared to be complete during the monitoring and variations in the efficiency of the cross-coupling reaction were mostly related to the purification step. Details of the structures and yield in final products are given in Table 2.