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  • 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)
  • receptors
  • Despite their structural differences, psychoactive synthetic cannabinoids bind with high affinity to CB1 receptors in the brain and, when tested, have been shown to activate these receptors and to produce a characteristic profile of effects, including suppression of locomotor activity, antinociception, hypothermia, and catalepsy, as well as Δ9-tetrahydrocannabinol (THC)-like discriminative stimulus effects in mice. (rti.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)
  • drugs
  • Structure-activity relationships of non-steroid anti-inflammatory drugs 1. (springer.com)
  • Lipid solubility was also found to influence the gastric ulcerogenic activity of other NSAI drugs in different ways. (springer.com)
  • K.D. Rainsford , The Comparative Gastric Ulcerogenic Activities of Non-Steroid Anti-Inflammatory Drugs , Agents and Actions 7 , 573-577 (1977). (springer.com)
  • Other successful strategies are to combine existing antibacterial agents with other drugs as well as the development of improved diagnostic procedures that may lead to rapid identification of the causative pathogen and permit the use of antibacterial agents with a narrow spectrum of activity. (wiley.com)
  • Some macrolides have antibiotic or antifungal activity and are used as pharmaceutical drugs. (wikipedia.org)
  • 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)
  • 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)
  • 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)
  • 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)
  • reduce
  • 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)