Receptor for advanced glycation end products (RAGE) is known to be involved in the transportation of amyloid β (Aβ) peptides and causes the accumulation of Aβ in the brain. Moreover, recent studies suggest that the interactions between RAGE and Aβ peptides may be the culprit behind Alzheimer...
The utility of Cp∗Co(III)-catalysts was expanded to oxidative C–C bond-forming reaction. In situ-generated Cp∗Co(III)-catalyst, rather than a preformed cationic Cp∗Co(III)-complex, was effective. Oxidative alkenylation of benzamides and acetanilide with ethyl acrylate proceeded with silver acet...
A series of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles (DPPs) was synthesized and evaluated for their ALK5 inhibition activity. The most potent compounds displayed submicromolar IC50 values for ALK5. Preliminary profiling of one of the most active compounds in a panel ...
The epidermal growth factor receptor (EGFR) is a well‑validated drug target for the treatment of non‑small cell lung cancer. Here we present an optimization approach and preliminary structure‑activity relationship for 1H‑pyrrolo[2,3‑b]pyridines as covalent irreversible mutant EGFR inhibitors. We...
A class of four-coordinate boron complexes is reported that contain both electron-rich and electron-poor functional groups. Judicious selection of donor and acceptor moieties with the use of a boron atom as a separating node yields charge transfer complexes capable of thermally activated delayed...
A convenient and regioselective cross-coupling of heteroaryl boronic acids with allylic alcohols under catalyst-free reaction conditions is described. The developed procedure is simple, works under external oxidant- and metal-free conditions, and proves to be very general with an unprecedented o...
The 4-(benzyloxy)benzyl chloride polymer-bound (BBC-Polym) was functionalized with Bismarck Brown Y (BBY: 4,4′-(1E,1E′)-1,3-phenylenebis(diazene-2,1-diyl)dibenzene-1,3-diamine ([email protected]), the corresponding novel nanoparticle Pd catalyst prepared by addition of PdCl2 ([email protected]...
The reactivity of the monomeric N-heterocyclic carbene silver(I) complexes, 1,3-bis-(2,4,6-trimethylphenyl)imidazol-2-ylidene-silver(I) chloride ([Ag(IMes)Cl], 1) and 1,3-bis-(4-bromo-2,6-dimethylphenyl)imidazol-2-ylidene-silver(I) chloride ([Ag(IMesBr)Cl], 2), toward the group 4 metal containin...
Palladium(II) complexes, LnPdCl2 (Ln = LA–LI), with N,N′-bidentate imine ligands derived from picolinaldehyde and substituted anilines have been synthesized and structurally characterized. Molecular structures revealed a distorted square plane geometry around Pd(II) centre in LnPdCl2 (Ln = LA–...
Three imidazolium salts having their two N-substituents equipped with remote calix[4]arenyl termini have been synthesised and converted into N-heterocyclic carbene (NHC) complexes of the type [PdCl2(NHC)(pyridine)]. An X-ray diffraction study carried out for one of the complexes, namely, trans-[...
In the present study, we report the micellization and clouding behavior of an amphiphilic antidepressant drug viz., amitriptyline hydrochloride (AMT) at different fixed temperatures and KCl concentrations in aqueous solutions. The critical micelle concentration (cmc) of AMT, as measured by condu...
The critical micelle concentration (cmc) of an amphiphilic drug amitriptyline hydrochloride (AMT) was determined in the presence of varying amounts of inorganic salts (NaF, NaCl, NaBr, LiCl, KCl), urea and thiourea over the temperature range 293–308 K by conductometric and dye solubilization (a...
The mixing behavior of amphiphilic drug amitriptyline hydrochloride (AMT) with bile salts (NaC, NaDC, NaTC) was studied at different compositions and temperatures by conductometry. Rubingh's, Motomura's and Clint's approaches were used to analyse the behavior. The obtained results...
The purpose of this study was to determine the aggregation behavior of amphiphilic drug amitriptyline hydrochloride (AMT) and to search for means which boost/suppress the aggregation behavior. Polyethylene glycols (PEGs) nonionic polymers (which are used as pharmaceutical excipients) of varying ...
Herein we report the micellization and cloud point of an amitriptyline hydrochloride (AMT) under the influence of cationic, anionic and nonionic hydrotropes. Anionic hydrotropes were employed to know the micellar and surface behaviors, besides studying the clouding behavior of AMT drug with cati...
Herein we have investigated the dealings between amphiphilic antidepressant drug amitriptyline hydrochloride (AMT) and gelatin interaction using different proposed techniques. AMT is used for the treatment of mental/mood problems such as depression. Gelatin interacts with this drug alike fashion...
The mixed micellization behavior of surface active ionic liquids (SAILs), 1-dodecyl-3-methylimidazolium chloride, [C12mim][Cl], and 1-tetradecyl-3-methylimidazolium chloride, [C14mim][Cl] with an amphiphilic drug amitriptyline hydrochloride (AMT) have been studied using surface tension and condu...
Conductivity method was carried out at various temperatures ranging from 293.15 K to 313.15 K to examine the monomeric as well as micellar phases of aqueous/brine/urea solutions of mixed systems composed of anionic surfactant sodium dodecyl sulfate (SDS) and cationic drug amitriptyline hydrochlo...
The present report highlights a cost effective and portable AMT–Ag nanocrystalline coordination polymer (NCCP) based electrochemical sensor for an efficient sensing of biologically active drug molecule ciprofloxacin hydrochloride (CFX). The AMT–Ag NCCP, is synthesized using an easily accessibl...
The thermodynamics and interfacial behavior of the mixed micellization of a trisubstituted imidazolium based surface active ionic liquid (SAIL), 1-dodecyl-2,3-dimethylimidazolium chloride [C12bmim][Cl], with an antidepressant amphiphilic drug amitriptyline hydrochloride (AMT) have been studied b...
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