The magnetic beads were synthesized using glycidylmethacrylate (GMA) and methylmethacrylate (MMA) monomers. A multimodal ligand (i.e., p-amino-benzamidine) was covalently immobilized onto magnetic beads after glutaraldehyde activation, and consequently used for purification of the trypsin from b...
This paper deals with the preparation of some 4‐carbobenzoxy‐3‐alkoxy benzamidines, N‐benzyl p‐N‐n‐alkylamidine benzamides and benzyl p‐N‐n‐butyl amidine thiobenzoate. It is hoped that these compounds can be screened for their anesthetic activities in order that they may be correlated ...
Two series of N,N′-diphenyl-benzamidines were synthesized as part of a study to search potential new drugs with antileishmanial activity. These compounds were obtained by anilides in PCl5 halogenation reaction with generation in situ of the corresponding benzimidoyl chlorides, and subsequently ...
In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies.
The potent fibrinolytic enzyme, plasmin has numerous clinical applications for recannulizing vessels obstructed by thrombus. Despite its diminutive size, 91 kDa, success in the recombinant expression of this serine protease has been limited. For this reason, a truncated non-glycosylated plasmin ...
A new single-step efficient photocchemical approach for α-arylpropanoic acids (4) from α chloro-propiophenones (5) is described. It involves carbonyl triplet excited state directed 1,2-aryl migration of the aryl group which has been found to be highly dependent upon the nature of the aryl subs...
Photochemistry of different α-substituted and phenyl-substituted propiophenones in methanol is investigated with a view to delineate the substituent effect with a special reference tu their rearrangement to α-arylpropanoic acids, an important class of nonsteroidal antiinflammatory agents. The ...
Synthesis and in vitro evaluation of [O-methyl-11C]1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide ([11C]-1), a potential imaging agent for CB1 receptors using PET is described. 1-(2-Chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-1H-pyrazole-3-carbox...
Publisher SummaryHeteropines received much attention, primarily because of continuous interest in the psychopharmacological activity of their bicyclic and tricyclic derivatives. Synthesis, structures, reactivity, and applications of tricyclic heteropines have been a part of the general indole an...
BackgroundTo uncover pharmacokinetic interactions between venlafaxine and doxepin or mirtazapine in a naturalistic sample.
In this study, the incompatibility of doxepin in solid physical mixtures with lactose (monohydrate and anhydrous) was investigated. The compatibility testing was made using various physicochemical techniques, such as differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR) spec...
SummaryDoxepin, a sedating tricyclic drug, at 3 mg and 6 mg doses was recently approved by the U.S. food and drug administration (FDA) for the treatment of insomnia. The objective of this systematic review was to obtain a precise summary of the efficacy and safety of doxepin as a hypnotic. We se...
A selective, sensitive and rugged liquid chromatography–tandem mass spectrometry (LC–MS/MS) assay has been developed for the simultaneous determination of doxepin (Dox) and its pharmacologically active metabolite, nordoxepin (NDox) in human plasma. The analytes and their internal standards (IS...
Histamine is an excitatory neurotransmitter in central nervous system. It plays an important role in the regulation of the sleep-wake cycle. Antidepressant with sleep-promoting effects, for example, doxepin, promotes sleep not through a sedative action but through resynchronisation of circadian ...
BackgroundDoxepin cream, an antihistaminic agent, has shown promising results in the treatment of pruritus in burn patients. However, its effectiveness has not been studied comprehensively.
The introductory section of the review will contain the description of a relatively new class of artificial biopolymers – polyamide nucleic acid (PNA) mimics. Their characteristic structural features and the most significant properties will be discussed. A particular focus will be on chiral PNA...
The molecular dynamics of solid L-alaninamide were studied by proton spin lattice relaxation times in the laboratory and rotating frames, and second moment measurements over temperature range of 100 to 350 K. The methyl group tunnelling was observed below 130 K. The rotational motions of both me...
Studies in humans indicate that acute administration of sub-anesthetic doses of ketamine, an NMDA receptor antagonist, provokes schizophrenic-like symptoms in healthy volunteers, and exacerbates existing symptoms in individuals with schizophrenia. These and other findings suggest that NMDA recep...
Silicon is one of the most promising anode materials for the next-generation high energy density lithium-ion batteries as its superior specific capacity and ultralow lithiation/delithiation voltage. Whereas, silicon suffers massive volume change during cycling, resulting in drastic pulverization...
Poly(N-acryloyl glycinamide) (PNAGA) with a protein-like thermoresponsive gelation behavior in water has been developed as a high strength self-healable supramolecular polymer(SP) hydrogels recently. However, harsh conditions, such as high temperature treatment and long waiting time, were requir...
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