• 1981). In addition they have potent antimalarial activity (Yeats et at. (biomedsearch.com)
  • A number of aminomethylcyclines with potent in vitro activity (MIC range of ≤0.06 to 2.0 μg/ml) were identified. (asm.org)
  • This study identified the AMCs as a novel class of antibiotics evolved from tetracycline that exhibit potent activity in vitro against tetracycline-resistant Gram-positive bacteria, including pathogenic strains of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant enterococci (VRE). (asm.org)
  • The most potent compound, compound 23, showed potent growth inhibitory activities on both prostate and breast cancer lines with IC(50) values in sub-micromolar range, fifty times more potent than curcumin. (semanticscholar.org)
  • Of these new carbapenems, (1R,5S,6S)-2-[(3S,5S)-5-sulfamoylaminomethyl pyrrolidin-3-ylthio]-6-[(1R)-1-hydroxyethyl]-1-methylcarb apen- 2-em-3-carboxyli c acid (S-4661) showed the most potent and well balanced activity and was selected as a candidate for further evaluation. (nih.gov)
  • Structure based design led to aminopyridine (R)-21, a potent and selective inhibitor able to modulate Nek2 activity in cells. (le.ac.uk)
  • and ( c ) poor correlations in some instances must be anticipated between in vivo tumorigenicity and activity in in vitro short-term tests as well as among different short-term tests. (aacrjournals.org)
  • However, we have been able to demonstrate that, for a series of non-steroidal anti-inflammatory drugs that are or were in clinical use, the incorporation of two simple physicochemical properties results in excellent correlations between human and rodent potencies for anti-inflammatory, analgesic and anti-pyretic activities. (openrepository.com)
  • 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)
  • Figure 2 shows the core structure and different substituents in general terms. (pubmedcentralcanada.ca)
  • The three nitrogen atoms of a guanidine moiety, which make it possible to bind to various substituents, as a result of a guanidine derivative show a diverse range of biochemical behavior that can be attributed to their flexible structure . (deepdyve.com)
  • the dipole moment μ and the charge of the ligand in the complex Q l , are the explanatory and predictive quantum descriptors correlated with the values of the anti-cancer activity of the studied complexes. (scirp.org)
  • The biological activities of ruthenium complexes are strongly influenced by the ligand structure. (scirp.org)
  • A comparison of this solution structure to the crystal structure reveals a general conservation of the DHFR fold and cofactor interactions as well as differences in the location of an active site helix and specific ligand interactions. (pubmedcentralcanada.ca)
  • In general, the solution structures are similar to the related X-ray crystal structures and yield additional details regarding the cooperativity of cofactor and ligand binding. (pubmedcentralcanada.ca)
  • Structureâ activity Relationships for the Interactions of 2â ²- and 3â ²-(O)-(N-methyl)anthraniloyl-substituted Purine and Pyrimidine Nucleotides with Mammalian Adenylyl Cyclases. (ku.edu)
  • Structural characteristics of anabolic androgenic steroids contributing to binding to the androgen receptor and to their anabolic and androgenic activities. (wikipedia.org)
  • An extended or bulkier group at the C17α position reduces AR agonist activity or changes the steroid into an antiandrogen . (wikipedia.org)
  • An ethynyl group (e.g., ethisterone , norethisterone ), allyl group (e.g., allylestrenol ), or vinyl group (e.g., norvinisterone ) all dramatically reduce AR agonist activity. (wikipedia.org)
  • Introduction of a double bond between the C4 and C5 positions in testosterone, otherwise known as 5α-reduction, confers several-fold increased AR agonist activity to testosterone. (wikipedia.org)
  • A hydroxyl group (instead of a ketone ) at the C3 position and/or a ketone (instead of a hydroxyl group) at the C17β can dramatically decrease AR agonist activity but render the steroid into an androgen prohormone . (wikipedia.org)
  • Originally developed as research tools for use in structure-activity relationship studies, synthetic cannabinoids contributed to significant scientific advances in the cannabinoid field. (rti.org)
  • Attachment of esters at the C3 and/or C17β hydroxyl groups confers increased lipophilicity and hence depot activity when administered in oil via intramuscular injection . (wikipedia.org)
  • Therefore it was discovered that the activities of the adjacent hydroxyl groups in scavenging free radical were increased. (cnki.com.cn)
  • The dynamics of catalytic structures are particularly vivid in selective oxidation catalysis where the lattice of a given catalytic solid partakes as a whole, not only its surface, in the redox processes of the reaction. (foyles.co.uk)
  • However, not only in selective redox catalysis does structure play an important role, its importance is also well documented, among others, in shape selective zeolite catalysis, enantioselective hydrogenation and hydrodesulfurization. (foyles.co.uk)
  • iii) Lipophilicity is a necessary but apparently not sufficient characteristic for BA cytocidal activity to which it appears to be indirectly related. (tcd.ie)