scholarly journals Thalidomide-type teratogenicity: structure–activity relationships for congeners

2018 ◽  
Vol 7 (6) ◽  
pp. 1036-1047 ◽  
Author(s):  
R. L. Smith ◽  
S. C. Mitchell
Keyword(s):  
Molecular Basis ◽  
Mature Animal ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Low Toxicity ◽  
Species Specific

Unravelling the molecular basis of thalidomide embryotoxicity, which is remarkably species-specific, is challenging in view of its low toxicity in the mature animal.

scholarly journals Species-Specific Differences and Structure−Activity Relationships in the Debromination of PBDE Congeners in Three Fish Species

2011 ◽  
Vol 45 (5) ◽  
pp. 1999-2005 ◽  
Author(s):  
Simon C. Roberts ◽  
Pamela D. Noyes ◽  
Evan P. Gallagher ◽  
Heather M. Stapleton
Keyword(s):  
Fish Species ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Species Specific

scholarly journals Antimicrobial Properties of Volatile Phenylpropanes

2010 ◽  
Vol 5 (9) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Alexander Pauli ◽  
Karl-Heinz Kubeczka
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Properties ◽  
Substitution Pattern ◽  
Structure Activity Relationships ◽  
Specific Effects ◽  
Structure Activity ◽  
Microbial Characteristics ◽  
Cis And Trans Isomers ◽  
Species Specific ◽  
Cis And Trans

The examination of antimicrobial structure-activity relationships of 93 volatile phenylpropanes (VPs) and 21 related aromatic compounds revealed a dependence of antimicrobial activity from the kind and number of substituents on the aromatic ring, their substitution pattern and microbial characteristics, such as Gram coloring and strain specific factors. Eugenol isomers were predominantly inhibitory in a concentration range from 25 to 2000 mg/L against all microorganisms tested, which were three strains of Escherichia Coli and Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, Listeria monocytogenes, and Candida albicans. Etherified VPs were either less active or inactive depending on the type of side chain and/or substitution pattern. Differences in the antimicrobial activity of cis- and trans-isomers were observed. Species specific structure-activity relationships exist as was demonstrated with the Gram-negative bacteria (inactivity of E-ortho-eugenol) C. albicans (activity of di- and threefold methoxylated 1-propenylbenzenes), S. aureus and B. subtilis (activity of di-ortho methoxylated phenolic allylbenzenes and hydroquinone derivatives). With regard to the variety of observed specific effects and natural variation of susceptibility towards VPs according to literature reference data, the chances for successful prediction by computational analysis (QSAR) appear to be limited.

Molecular Basis of Structure–Activity Relationships between Salphen Metal Complexes and Human Telomeric DNA Quadruplexes

2011 ◽  
Vol 55 (1) ◽  
pp. 209-222 ◽  
Author(s):  
Nancy H. Campbell ◽  
Nurul H. Abd Karim ◽  
Gary N. Parkinson ◽  
Mekala Gunaratnam ◽  
Vanessa Petrucci ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Molecular Basis ◽  
Telomeric Dna ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Dna Quadruplexes

scholarly journals Structure–activity relationships of guanylated antimicrobial polymethacrylates

2014 ◽  
Vol 86 (8) ◽  
pp. 1281-1291 ◽  
Author(s):  
Katherine E.S. Locock ◽  
Thomas D. Michl ◽  
Hans J. Griesser ◽  
Matthias Haeussler ◽  
Laurence Meagher
Keyword(s):  
Bacterial Resistance ◽  
Biological Activities ◽  
Antimicrobial Polymers ◽  
Practical Applications ◽  
Structure Activity Relationships ◽  
New Class ◽  
Human Red Blood Cells ◽  
Structure Activity ◽  
Ideal Composition ◽  
Low Toxicity

AbstractHost-defense antimicrobial peptides (AMPs) are a promising lead in the search for novel antibiotics. Many of these peptides exhibit broad-spectrum antibacterial ability, low toxicity toward human cells, and little susceptibility to induction of bacterial resistance. Our research focuses on the development of synthetic polymers that are able to mimic the amphiphilic and cation-rich characteristics of AMPs. This derives bioactive polymers that retain the activity profile of AMPs while utilizing a construct that is less expensive and easier to produce and manipulate chemically. This review details structure–activity relationships (SARs) of a new class of arginine-rich, synthetic AMP mimicking polymers (SAMPs), the guanylated polymethacrylates. These are contrasted with those of amine-based polymers that are mimics of lysine-rich AMPs. The ideal composition for candidates for practical applications was identified as those containing guanidines as a cation source, having a low molecular weight and a low level of lipophilicity. This gave polymers with high potency against Gram-positive strains of bacteria (e.g., Staphylococcus epidermidis MIC = 10 μg/mL) and low toxicity towards human red blood cells (<4% hemolysis at given MIC). This work emphasizes the need to rationalize observed biological activities based not purely on the global lipophilic and cationic character of polymers but rather to consider the profound effect that specific pendant functional groups may have on the potency, selectivity, and mechanisms behind the action of antimicrobial polymers.

Structure-activity relationships in the acronycine and benzo[b]acronycine series: Role of the pyran ring

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
Q Do ◽  
H Doan Thi Mai ◽  
T Gaslonde ◽  
B Pfeiffer ◽  
S Léonce ◽  
...  
Keyword(s):  
Pyran Ring ◽  
Structure Activity Relationships ◽  
Structure Activity

Structure activity-relationships of P-Glycoprotein modulation using a small library of macrocyclic lathyrane diterpenes

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
M Reis ◽  
RJ Ferreira ◽  
MMM Santos ◽  
DJVA dos Santos ◽  
J Molnár ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structure Activity ◽  
P Glycoprotein
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