Loading...
  • potent
  • 1981). In addition they have potent antimalarial activity (Yeats et at. (biomedsearch.com)
  • Following the discovery of its activity as a potent negative allosteric modulator of mGluR5, fenobam has been re-investigated for many applications, with its profile of combined antidepressant, anxiolytic, analgesic and anti-addictive effects potentially useful given the common co-morbidity of these symptoms. (wikipedia.org)
  • Yuehchukene possesses a potent anti-fertility activity, with the (R)-(+)-enantiomer having been identified as the active form. (wikipedia.org)
  • molecular
  • The underlying problem is therefore how to define a small difference on a molecular level, since each kind of activity, e.g. reaction ability, biotransformation ability, solubility, target activity, and so on, might depend on another difference. (wikipedia.org)
  • On the one hand, these models allow for the indication of the most important descriptors (molecular properties) responsible for the antiplasmodial activity. (mdpi.com)
  • Ernst Späth subsequently showed that these alkaloids were identical and proposed the correct molecular structure for this substance, for which the name "hordenine" was ultimately retained. (wikipedia.org)
  • receptor
  • Also, the clinical candidates from Janssen, Abott and Merck pharmaceuticals (fig. 8c) having a 5-aminoisoquinoline group as a common feature suggesting that there is a key interaction of this group at the receptor site for TRPV1 antagonist activity. (wikipedia.org)
  • vitro
  • Approach: The compounds evaluated for their in vitro antiviral activities against the viruses: HIV-1, Bovin viral Diarrhea, Yellow Fever, Reovirus 1, Herpesvirus 1, Vaccinia, Vescular Stomatitis, Coxackie virus B2, Poliovirus 1 and Respiratory Syncytial viruses by using Microculture Tetrazolium assay (MTT) method. (biomedsearch.com)
  • Conclusion: The in vitro antiviral activities of the tested dihydropyridones can be enhanced by increasing chain length of the substituent on the nitrogen atom. (biomedsearch.com)
  • 2008). These compounds as well as curcumin were evaluated for preliminary estimation of the in vitro tumor inhibiting activity against a variety of viruses included: HIV-1, Bovin Viral Diarrhea (BVDV), Yellow Fever (YFV), Reovirus 1 (Reo), Herpesvirus 1 (HSV-1), Vaccinia VV), Vescular Stomatitis (VSV), Coxackie virus B2 CVB-2), Poliovirus 1 (Sb-1) and Respiratory Syncytial (RSV) viruses, using microculture assay (MTT) method (Tang et at. (biomedsearch.com)
  • In vitro antiplasmodial activity was shown before for several compounds belonging to this class, and in this paper the antiplasmodial and cytotoxic activities of ten more cyclopeptide alkaloids are reported. (mdpi.com)
  • SARs
  • Many of these methods are not generally applicable or reduce the activity space to scalar summary statistics before establishing SARs. (broadinstitute.org)
  • derivatives
  • An example of such compounds is hydroxycinnamic acids ( p -coumaric, caffeic, ferulic, and sinapic) and their derivatives (esters, amides, and glycosides) which possess a pool of biological activities, including and antidiabetic effects [ 28 - 32 ]. (hindawi.com)
  • In this paper, an overview of the structure-activity relationship (SAR) profiles of promising nonxanthine pyrazolo derivatives is reported and discussed. (hindawi.com)
  • substituents
  • It was observed that replacement of either of these hydrogens at N1 or N3 by substituents increases the activity significantly. (biomedsearch.com)
  • It is also apparent that electronic factors (which reflect changes in the dissociation constants) and the position of electron-withdrawing substituents on aromatic groups variously influences the ulcerogenic activity in different groups of NSAI drugs. (springer.com)
  • proton
  • Fenobam is known to exist in five crystalline forms, all of them exhibiting a tautomeric structure with the proton attached to the five membered ring nitrogen. (wikipedia.org)
  • moiety
  • Furthermore, the presence of a β-hydroxy proline moiety could correlate with higher antiplasmodial activity, and methoxylation (or, to a lesser extent, hydroxylation) of the styrylamine moiety could be important for displaying antiplasmodial activity. (mdpi.com)
  • nitrogen
  • Activity was found to be abolished by nitrogen substitution, 2, 5 and 5'-position substitution, hydroxylation of the benzene ring, hydroxylation of C9-C10 double bond and deletion of 7,7-dimethyl group. (wikipedia.org)
  • effects
  • tested DMDA for effects in unilaterally-caudectomized mice (dose ≤ 120 mg/kg, i.p.), nigral-lesioned rats (dose = 10 mg/kg, i.p.), and on adenylate cyclase activity in homogenized mouse caudate nuclei (concentration = 10μM/L). DMDA showed no effects in any of these assay systems. (wikipedia.org)
  • Yuehchukene has not been developed as a pharmaceutical drug due to the effects of this estrogenic activity. (wikipedia.org)
  • potential
  • I. M. Cestari, S. J. Sarti, C. M. Waib, and A. C. Branco Jr., "Evaluation of the potential insecticide activity of Tagetes minuta (Asteraceae) essential oil against the head lice Pediculus humanus capitis (Phthiraptera: Pediculidae)," Neotropical Entomology , vol. 33, no. 6, pp. 805-807, 2004. (hindawi.com)
  • Hyperpolarization, on the other hand, is employed to reduce neuronal activity by establishing a high threshold potential for firing across an action potential. (wikipedia.org)
  • selective
  • Anoxic depolarization is induced by the loss of neuronal selective membrane permeability and the ion gradients across the membrane that are needed to support neuronal activity. (wikipedia.org)
  • various
  • Gram-negative bacteria can develop resistance to polymyxins through various modifications of the LPS structure that inhibit the binding of polymyxins to LPS. (wikipedia.org)
  • whose
  • MRP2/ABCC2 is a member of the integral membrane protein family whose high-resolution crystal structure has not been described. (springer.com)
  • Effect
  • K.D. Rainsford and M.W. Whitehouse , Gastric Irritancy of Aspirin and its Congeners: Anti-Inflammatory Activity Without this Side-Effect , J. Pharm. (springer.com)