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作者:Kumar Vipin , Sharma Archana , Sharma Prabodh Chander
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (2), pp.198-203PubMed
摘要:Some new decanoic acid [2,5-disubstituted-4-oxo-thiazolidin-3-yl]amides (6a-j) have been synthesised by the condensation of decanoic acid hydrazide with various aromatic aldehydes to yield the Schiff's bases. Cyclocondensation of the Schiff's bases with thioglycollic acid afforde...
作者:Patel Mohan N , Parmar Pradhuman A , Gandhi Deepen S
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (2), pp.188-97PubMed
摘要:The copper(II) complexes of the type [Cu(SPF)(A(n))Cl]/[Cu(PFL)(A(n))Cl] (where SPF is sparfloxacin, PFL is pefloxacin and A(n) is 2,2'-dipyridylamine/pyridine-2-carboxalehyde/thiophene-2-carboxaldehyde) were synthesised and were found to have a pyramidal geometry with a squ...
作者:Intharathep Pathumwadee , Rungrotmongkol Thanyada , Decha Panita ...
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (2), pp.162-8PubMed
摘要:In order to understand how rimantadine (RMT) inhibits the proton conductance in the influenza A M2 channel via the recently proposed "allosteric mechanism", molecular dynamics simulations were applied to the M2-tetrameric protein with four RMTs bound outside the channel at the th...
作者:Ali Mohamed Ashraf , Manogaran Elumalai , Govindasamy Jeyabalan ...
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (1), pp.149-53PubMed
摘要:A series of bis dihydropyrimidine compounds were synthesised by reacting dapsone with acetylacetoacetate to produce N1-4-[4-(2-oxopropylcarboxamido) phenylsulphonyl] phenyl-3-oxobutanamide, then treated with guanidine hydrochloride and an appropriate aldehyde with a catalyti...
作者:Amir Mohammad , Saifullah Khalid , Akhter Wasim
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (1), pp.141-8PubMed
摘要:A series of substituted azole derivatives (3a-e, 4a-e and 5a-e) were synthesised by the cyclisation of N(1)(diphenylethanoyl)-N(4)-substituted phenyl thiosemicarbazides under various reaction conditions. These compounds were tested in vivo for their anti-inflammatory activity. Th...
作者:Kotthaus Joscha , Steinmetzer Torsten , van de Locht Andreas ...
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (1), pp.115-22PubMed
摘要:The development of serine protease inhibitors often results in the discovery of new lead compounds containing strong basic amidine functions that usually suffer from poor absorption from the intestine. In order to improve oral bioavailability of these drugs, prodrug principles su...
作者:Kharb Rajeev , Sharma Prabodh Chander , Yar Mohammed Shahar
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (1), pp.1-21PubMed
摘要:The triazole nucleus is one of the most important and well known heterocycles which is a common and integral feature of a variety of natural products and medicinal agents. Triazole nucleus is present as a core structural component in an array of drug categories such as antimicrob...
作者:Choudhary M Iqbal , Abbas Ghulam , Ali Saqib ...
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (1), pp.98-103PubMed
摘要:A feature of diabetes is that the rate of protein glycation and the formation of advanced glycation endproducts (AGEs) increases spontaneously due to the abnormally elevated levels of sugar in the blood. The glycation of proteins is associated with a large number of late diabetic...
作者:Kanagarajan V , Thanusu J , Gopalakrishnan M
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (1), pp.67-77PubMed
摘要:A series of novel hybrid heterocyclic compounds, 3-(3-alkyl-2,6-diarylpiperin-4-ylidene)-2-thioxoimidazolidin-4-ones were synthesised and a comparative study was also carried out under microwave irradiation. The synthesised compounds were characterised by their melting points, el...
作者:Pecic Stevan , McAnuff Marie A , Harding Wayne W
来源:[J].Journal of Enzyme Inhibition and Medicinal Chemistry, 2010, Vol.26 (1), pp.46-55PubMed
摘要:Nantenine, as well as a number of flexible analogs, were evaluated for acetylcholinesterase (AChE) inhibitory activity in microplate spectrophotometric assays based on Ellman's method. It was found that the rigid aporphine core of nantenine is an important structural require...

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