scholarly journals Establishment of a Phenotypic-based Sand Dollar Fellaster zelandiae Embryo Development Assay and its Application in Defining the Structure-Activity Relationship of Discorhabdin Alkaloids

2013 ◽  
Vol 8 (6) ◽  
pp. 1934578X1300800
Author(s):  
Tanja Grkovic ◽  
Brent R. Copp
Keyword(s):  
Natural Products ◽  
New Zealand ◽  
Embryo Development ◽  
Structure Activity Relationship ◽  
Structural Features ◽  
Activity Relationship ◽  
Sand Dollar ◽  
Structure Activity ◽  
The Common ◽  
Relationship Of

An embryo development assay using the common New Zealand intertidal species Fellaster zelandiae (sand dollar) is presented. The assay was validated by comparing activity profiles of a range of discorhabdin alkaloids, natural products sourced from Latrunculia spp. sponges containing a core pyrido[2,3- h]pyrrolo[4,3,2- de]quinoline tetracyclic skeleton bound to various spiro-substituents at the C-6 position. Structural features on the discorhabdin molecule that correlated to the greatest degree of F. zelandiae embryo developmental inhibition were the presence of a spiro-dienone moiety and a C-2 bromine substituent. Based on the sand dollar embryo development assay results, a mechanism for the activity of the discorhabdin alkaloids is proposed.

scholarly journals Synthesis and Antibacterial Analysis of Analogues of the Marine Alkaloid Pseudoceratidine

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2713
Author(s):  
David Barker ◽  
Stephanie Lee ◽  
Kyriakos G. Varnava ◽  
Kevin Sparrow ◽  
Michelle van Rensburg ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Structural Features ◽  
Secondary Amines ◽  
Activity Relationship ◽  
Gram Positive ◽  
Gram Negative ◽  
Structure Activity ◽  
Escherichia Coli Bacteria ◽  
Anti Fungal ◽  
Relationship Of

In an effort to gain more understanding on the structure activity relationship of pseudoceratidine 1, a di-bromo pyrrole spermidine alkaloid derived from the marine sponge Pseudoceratina purpurea that has been shown to exhibit potent biofouling, anti-fungal, antibacterial, and anti-malarial activities, a large series of 65 compounds that incorporated several aspects of structural variation has been synthesised through an efficient, divergent method that allowed for a number of analogues to be generated from common precursors. Subsequently, all analogues were assessed for their antibacterial activity against both Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria. Overall, several compounds exhibited comparable or better activity than that of pseudoceratidine 1, and it was found that this class of compounds is generally more effective against Gram-positive than Gram-negative bacteria. Furthermore, altering several structural features allowed for the establishment of a comprehensive structure activity relationship (SAR), where it was concluded that several structural features are critical for potent anti-bacterial activity, including di-halogenation (preferable bromine, but chlorine is also effective) on the pyrrole ring, two pyrrolic units in the structure and with one or more secondary amines in the chain adjoining these units, with longer chains giving rise to better activities.

scholarly journals Structure–Activity Relationship of Cytotoxic Natural Products from Indonesian Marine Sponges

2022 ◽  
Author(s):  
Jonathan A. Panggabean ◽  
Sya’ban P. Adiguna ◽  
Tutik Murniasih ◽  
Siti I. Rahmawati ◽  
Asep Bayu ◽  
...  
Keyword(s):  
Natural Products ◽  
Structure Activity Relationship ◽  
Marine Sponges ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of

Chemistry and Structure−Activity Relationship of HIV-1 Integrase Inhibitor Integracide B and Related Natural Products

2003 ◽  
Vol 66 (10) ◽  
pp. 1338-1344 ◽  
Author(s):  
Sheo B. Singh ◽  
John G. Ondeyka ◽  
William A. Schleif ◽  
Peter Felock ◽  
Daria J. Hazuda
Keyword(s):  
Natural Products ◽  
Integrase Inhibitor ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of ◽  
Hiv 1

scholarly journals Study "structure-anti-arrhythmic activity" relationship of n-phenil acetamide derivatives and amides of aromatic carbonic acids

2010 ◽  
Vol 56 (4) ◽  
pp. 471-479 ◽  
Author(s):  
V.R. Khairullina ◽  
G.P. Tarasov ◽  
A.Ja. Gerchikov ◽  
F.S. Zarydiy ◽  
L.A. Tjurina
Keyword(s):  
Computer System ◽  
Structural Parameters ◽  
Pharmaceutical Preparations ◽  
Structure Activity Relationship ◽  
Structural Features ◽  
Activity Relationship ◽  
Structure Activity ◽  
Highly Effective ◽  
Carbonic Acids ◽  
Relationship Of

Using the computer system SARD-21 (Structure Activity Relationship & Design) structural features of high- and low-effective anti-arrhythmic agents have been recognized and the influence of these features on the anti-arrhythmic properties has been evaluated. This information has been used for generation of the model for prediction of anti-arrhythmic effectiveness of pharmaceutical preparations with the 82%-level of recognition by two methods. The recognized structural parameters may be successfully used for design of new highly effective anti-arrhythmic drugs, and also for modification of structures of known anti-arrhythmic drugs for the increase of effectiveness of their anti-arrhythmic action.

Structure-activity relationship of (-) mammea A/BB derivatives against Leishmania amazonensis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
MA Brenzan ◽  
CV Nakamura ◽  
BPD Filho ◽  
T Ueda-Nakamura ◽  
MCM Young ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Leishmania Amazonensis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of
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