Abstract：
:Nitric Oxide Synthase (NOS) inhibitors could play a powerful role in inflammatory and neurodegenerative diseases. In this work, novel acetamidine derivatives of NOS were synthesized and the inhibitor activity was evalued. To screen the activity and selectivity, the l-citrulline residue, after the enzymatic NOS assay, was derivatized with o-phthaldialdehyde/N-acetyl cysteine (OPA/NAC) and then evaluated by RP-HPLC method with fluorescence detection. All compounds did not affect the activity of endothelial and neuronal isoforms, while nine of them possessed a percentage of iNOS activity at 10μM lower than 50%, and were selected for IC50 evaluation. Among them, a compound emerged as a very potent (IC50 of 53nM) and selective iNOS inhibitor.
journal_name
J Pharm Biomed Analjournal_title
Journal of pharmaceutical and biomedical analysisauthors
Fantacuzzi M,Maccallini C,Di Matteo M,Ammazzalorso A,Bruno I,De Filippis B,Giampietro L,Mollica A,Amoroso Rdoi
10.1016/j.jpba.2015.11.045subject
Has Abstractpub_date
2016-02-20 00:00:00pages
419-24eissn
0731-7085issn
1873-264Xpii
S0731-7085(15)30263-6journal_volume
120pub_type
杂志文章abstract：:Ten free fatty acids namely lauric acid, myristic acid, pentadecanoic acid, palmitoleic acid, palmitic acid, linoleic acid, oleic acid, stearic acid, docosanoic acid and lignoceric acid and four free sterols including ergosterol, cholesterol, campesterol and beta-sitosterol in natural (wild) Cordyceps sinensis, Cordyc...
journal_title：Journal of pharmaceutical and biomedical analysis
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journal_title：Journal of pharmaceutical and biomedical analysis
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journal_title：Journal of pharmaceutical and biomedical analysis
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doi：10.1016/j.jpba.2005.07.012
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journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2008.09.013
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journal_title：Journal of pharmaceutical and biomedical analysis
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journal_title：Journal of pharmaceutical and biomedical analysis
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journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
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更新日期：2013-09-01 00:00:00
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journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(99)00143-0
更新日期：1999-11-01 00:00:00
abstract：:In a multicentre study involving six laboratories, a microbiological assay was performed on three neomycin samples containing respectively, 0.12, 2.1 and 11% (m/m) of neomycin C, as well on a pure neomycin C sample. The potency was determined according to the European Pharmacopoeia method but using a neomycin B base s...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
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abstract：:Unknown by-product associated with the synthesis of dapoxetine was isolated. The structure elucidation of this new compound using accurate mass data and NMR spectroscopy is presented herein. The unambiguous resonance assignment concluded to the formation of a tricyclic compound 4-phenyl-2H,3H,4H-naphtho[1,2-b]pyran, a...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
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更新日期：2014-08-05 00:00:00
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journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章,评审
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更新日期：2019-09-10 00:00:00
abstract：:Homochirality is essential for life. For a long time, it was considered that d-amino acids were excluded from living systems. In the past 30 years, however, d-amino acids have been found in living organisms in the form of free amino acids, peptides and proteins, owing to advances in the analysis of optical isomers of ...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章,评审
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journal_title：Journal of pharmaceutical and biomedical analysis
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journal_title：Journal of pharmaceutical and biomedical analysis
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journal_title：Journal of pharmaceutical and biomedical analysis
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abstract：:A liquid chromatographic tandem mass spectrometric method for the quantitative determination of sumatriptan base in human plasma and urine has been developed and validated over the concentration range 0.2-20 ng base ml-1. Sumatriptan is a 5-HT1 receptor agonist which has found widespread use in the treatment of migrai...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
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journal_title：Journal of pharmaceutical and biomedical analysis
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abstract：:In this work, metabolites of cyadox (CYX) produced by liver microsomes, primary hepatocytes and intestinal microflora systems of rat, chicken and swine were identified and elucidated using ultra-performance liquid chromatography/quadrupole time-of-flight tandem mass spectrometry (UPLC/Q-TOF-MS). Expected and unexpecte...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2012.04.004
更新日期：2012-08-01 00:00:00
abstract：:A chiral liquid chromatographic method was developed for the enantiomeric resolution of Pramipexole dihydrochloride monohydrate, (S)-2-amino-4,5,6,7-tetra-hydro-6-(propylamino) benzothiazole dihydrochloride monohydrate, a dopamine agonist in bulk drugs. The enantiomers of Pramipexole dihydrochloride monohydrate were r...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
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abstract：:A method was developed for the assay of benzoic acid, 2-chloro-5-[[(1-methylethoxyl)thioxomethyl]amino]-,1-meth yle thyl ester (NSC 629243) in hamster, mouse, human and, to a limited extent, dog plasma. Protein in 0.5 ml of plasma was precipitated with four volumes of methanol and the supernatant was analysed for NSC ...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
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abstract：:A liquid chromatographic method was developed for the simultaneous separation of curcumin, β-arteether, tetrahydrocurcumin and dihydroartemisinin based on the design of experiments and the design space methodology. The influence of the percentage of organic modifier, flow rate of the mobile phase and column temperatur...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2013.09.009
更新日期：2014-01-01 00:00:00
abstract：:D-amino acids are currently recognized as naturally occurring physiologically active substances and biomarkers in mammals. The progress of analytical technologies, mostly high resolution chromatographic or electrodriven separation methods, has significantly contributed to the advances in D-amino acid research in real ...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章,评审
doi：10.1016/j.jpba.2012.01.041
更新日期：2012-10-01 00:00:00
abstract：:The present work describes a quantitative thin layer procedure for estimating primidone, clorazepate dipotassium and chlorzoxazone in bulk powders and in dosage forms, each in the presence of its degradation product. The method consists of dissolving the drug in ethanol (for primidone), or methanol (for clorazepate di...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(98)00043-0
更新日期：1999-09-01 00:00:00
abstract：:A new procedure for kinetic determination of paracetamol in pharmaceuticals is proposed. The method is based on potentiometric monitoring of the concentration perturbations of the matrix reaction system being in a stable non-equilibrium stationary state close to the bifurcation point. In the case considered as the mat...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2005.11.043
更新日期：2006-05-03 00:00:00
