Aplysia sea hares are harmless to humans and good materials for producing compounds with pharmacological properties. Aplysia species have been investigated for their human nutritional value. The knowledge on the metabolic machinery from edible Aplysia depilans Gmelin is herein broadened by ident...
Neurodegenerative processes involve numerous and closely related events that ultimately culminate in neuronal cell injury. The aim of this study was (i) to assess, for the first time, the neuroprotective potential of acetone extracts of six edible species of Ochrophyta, by evaluating their choli...
Fucoxanthin and fucosterol are archetypal lipid components of edible brown algae that provide several health benefits. Lately, their protective role in Aβ1-42-induced cognitive dysfunction in animal models has been reported (Alghazwi et al., 2019; Oh et al., 2018). However, their role in the am...
A headspace capillary gas chromatographic method was developed to determine trifluoroacetic acid (TFA) in a bulk substance (ceronapril). The bulk sample is reacted in a sealed headspace vial with dimethyl sulfate in concentrated sulfuric acid to convert TFA to methyl trifluoroacetate (MTFA). A p...
The angiotensin-converting enzyme (ACE)-inhibitor ceronapril (SQ 29852) is shown to be a substrate of the intestinal dipeptide transporter. Uptake by Caco-2 cells, grown as confluent monolayers, follows a major saturable pathway (Km, 0.91 ± 0.11 mM; ∼90% at 1 mM) together with a minor passive ...
Angiotensin converting enzyme (ACE) in brain, cerebrospinal fluid (C.S.F.) and peripheral tissues was studied ex vivo after oral administration of ceronapril (SQ 29,852) to male Sprague-Dawley rats. Angiotensin converting enzyme in tissue was measured by in vitro autoradiography or enzymatic ass...
Three experiments that used a latent inhibition procedure to investigate the effects of ceronapril on attentional processes in the rat are reported. Latent inhibition is a behavioural paradigm in which prior exposure to a stimulus with no significant consequences retards subsequent conditioning ...
Background: Behavioral evidence from animal studies has suggested that ceronapril and other angiotensin-converting enzyme (ACE) inhibitors have some anxiolytic activity.Objectives: The objectives of this trial were to assess the effects of ceronapril, a centrally acting ACE inhibitor, on psychom...
We report on novel 3-arylamino-6-benzylamino-1,2,4,5-tetrazines with potent activity against Plasmodium falciparum.
In this study we present surface-enhanced Raman spectroscopy (SERS) investigations of ortho-substituted N-benzylamino(boronphenyl)methylphosphonic acid (N-benzylamino-(2-boronphenyl)-R-methylphosphonic acid; o-PhR) adsorbed onto a roughened in oxidation–reduction cycles (ORC) Ag, Au, and Cu ele...
A series of 1-[4-(N-benzylamino)phenyl]-3-phenylurea derivatives 2a–r were synthesized as HIF-1α inhibitors. Among the compounds synthesized, compound 2k was found to be a potent inhibitor against HIF-1α accumulation under hypoxic condition and inhibited the hypoxia-induced HIF-1 transcriptio...
Here, we report a systematic surface-enhanced Raman spectroscopy (SERS) study of the structures of five N-benzylamino(boronphenyl)-methylphosphonic acids: N-benzylamino-(3-boronphenyl)-S-methylphosphonic acid (m-PhS), N-benzylamino-(4-boronphenyl)-S-methylphosphonic acid (p-PhS), N-benzylamino-(...
The treatment of 2(or 4)-benzylamino substituted quinolines, 9-benzylaminoacridine, 2-benzylaminopyridine, a 4-benzyloxyquinoline, and an N-benzyloxyamidine with BBr3 yields the corresponding amino or hydroxy substituted compounds. The scope and limitations of this novel reaction are discussed.
3-Benzoyl-4-benzylamino-7-dimethylaminocoumarin was synthesized and its conformation in solid state and solution was determined. While the X-ray crystal analysis showed an aromatic π–π stacking interaction in the solid state, the proton NMR studies suggested the presence of an intramolecular ...
The quinazoline scaffold is the main part of many marketed EGFR inhibitors. Resistance developments against those inhibitors enforced the search for novel structural lead compounds. We developed novel benzo-anellated 4-benzylamine pyrrolopyrimidines with varied substitution patterns at both the ...
A convenient and practical InCl3 catalyzed three-component reaction of 4-hydroxy coumarin/1,3 diones, aromatic aldehyde, and secondary amine for the synthesis of α-benzylamino coumarins and diketones in good yields has been reported.
Encouraging selectivity and low micromolar activity against HeLa cervical carcinoma (IC50 ⩾ 3.0 μM) and the aggressive MDA-MB-231 triple negative breast carcinoma (IC50 ⩾ 9.6 μM) cell lines has been exhibited by a number of readily accessible 4-(N-benzylamino)cinnamate esters. The potential of...
19, 20-Dehydro-PGE1 and 19, 20-dehydro-PGE2 were recently identified in human seminal fluid. These prostaglandins might be formed by dehydration of 19 (R̄)-hydroxy-PGE1 and 19 (R̄)-hydroxy-PGE2 or, conceivably, by biosynthesis from precursor fatty acids with a terminal double bond. To examine th...
Human seminal fluid was recently found to contain 18,19-dehydroprostaglandins E1 and E2 (E. H. Oliw, H. Sprecher, and M. Hamberg, (1986) J. Biol. Chem.261, 2675–2683). In the present study, the cis and trans isomers of 18,19-dehydroprostaglandins E1 and E2 were prepared by incubation of microso...
Growing interest in polyunsaturated fatty acid (PUFA) applications in various fields coupled with their significance in health and dietary requirements has focused attention on the provision of suitable sources of these compounds. Isolation of highly efficient oleaginous microorganisms has led t...
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