scholarly journals An organometallic structure-activity relationship study reveals the essential role of a Re(CO)3moiety in the activity against gram-positive pathogens including MRSA

2015 ◽  
Vol 6 (1) ◽  
pp. 214-224 ◽  
Author(s):  
Malay Patra ◽  
Michaela Wenzel ◽  
Pascal Prochnow ◽  
Vanessa Pierroz ◽  
Gilles Gasser ◽  
...  
Keyword(s):  
Essential Role ◽  
Antibacterial Agents ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Gram Positive ◽  
Structural Class ◽  
Structure Activity ◽  
Systematic Structure ◽  
Relationship Study

A systematic structure activity relationship reveals the contribution of individual organometallic moieties to the potency of a new structural class of hetero-trimetallic antibacterial agents.

Structure–activity relationship study of half-sandwich metal complexes in aqueous transfer hydrogenation catalysis

2020 ◽  
Vol 7 (3) ◽  
pp. 583-591 ◽  
Author(s):  
Anh H. Ngo ◽  
Loi H. Do
Keyword(s):  
Metal Complexes ◽  
Structure Activity Relationship ◽  
Transfer Hydrogenation ◽  
Activity Relationship ◽  
Structure Activity ◽  
Systematic Structure ◽  
Relationship Study ◽  
Hydrogenation Catalysis ◽  
Half Sandwich

A systematic structure–activity relationship study was performed to identify the factors that are important to enhancing the transfer hydrogenation efficiency of half-sandwich metal complexes.

scholarly journals Structure–Activity Relationships (SARs) of α-Ketothioamides as Inhibitors of Phosphoglycerate Dehydrogenase (PHGDH)

2020 ◽  
Vol 13 (2) ◽  
pp. 20
Author(s):  
Quentin Spillier ◽  
Séverine Ravez ◽  
Judith Unterlass ◽  
Cyril Corbet ◽  
Charline Degavre ◽  
...  
Keyword(s):  
Cancer Progression ◽  
Structure Activity Relationship ◽  
Therapeutic Agents ◽  
Activity Relationship ◽  
Cancer Treatments ◽  
Promising Strategy ◽  
Structure Activity ◽  
Phosphoglycerate Dehydrogenase ◽  
Relationship Study

For many years now, targeting deregulation within cancer cells’ metabolism has appeared as a promising strategy for the development of more specific and efficient cancer treatments. Recently, numerous reports highlighted the crucial role of the serine synthetic pathway, and particularly of the phosphoglycerate dehydrogenase (PHGDH), the first enzyme of the pathway, to sustain cancer progression. Yet, because of very weak potencies usually in cell-based settings, the inhibitors reported so far failed to lay ground on the potential of this approach. In this paper, we report a structure–activity relationship study of a series of α-ketothioamides that we have recently identified. Interestingly, this study led to a deeper understanding of the structure–activity relationship (SAR) in this series and to the identification of new PHGDH inhibitors. The activity of the more potent compounds was confirmed by cellular thermal shift assays and in cell-based experiments. We hope that this research will eventually provide a new entry point, based on this promising chemical scaffold, for the development of therapeutic agents targeting PHGDH.

scholarly journals Aromatic Hydroxyl Group Plays a Critical Role in Antibacterial Activity of the Curcumin Analogues

2012 ◽  
Vol 7 (1) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Mi Kyoung Kim ◽  
Jun Cheol Park ◽  
Youhoon Chong
Keyword(s):  
Antibacterial Activity ◽  
Critical Role ◽  
Antibacterial Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hydroxyl Group ◽  
Curcumin Analogues ◽  
Structure Activity ◽  
Relationship Study

The aim of this study was to investigate the role of the aromatic substituents of the curcumin scaffold on the antibacterial activity of the resulting curcumin analogues. Six curcumin analogues with different aromatic substituents were prepared and their antibacterial activities were evaluated against two Gram-positive and four Gram-negative bacteria. The structure-activity relationship study demonstrated that antibacterial activity of the curcumin analogues was critically dependent upon the aromatic hydroxyl group. Thus, hydroxycurcumin with an additional aromatic hydroxyl group on the curcumin scaffold showed antibacterial activity against all six pathogens tested and it remained effective even against ampicillin-resistant Enterobacter cloacae. Along with the previously reported antioxidative effect, the broad-spectrum antibacterial activity of the hydroxycurcumin warrants further investigation of its biological activity as well as extensive structure-activity relationship study of the curcumin analogues with various aromatic substituents.

scholarly journals Investigation of 5’-Norcarbocyclic Nucleoside Analogues as Antiprotozoal and Antibacterial Agents

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3433 ◽  
Author(s):  
Anastasia Khandazhinskaya ◽  
Elena Matyugina ◽  
Pavel Solyev ◽  
Maggie Wilkinson ◽  
Karen Buckheit ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Biological Activity ◽  
Antibacterial Agents ◽  
Structure Activity Relationship ◽  
Nucleoside Analogues ◽  
Activity Relationship ◽  
Carbocyclic Nucleosides ◽  
Structure Activity ◽  
Small Structure ◽  
Relationship Study

Carbocyclic nucleosides have long played a role in antiviral, antiparasitic, and antibacterial therapies. Recent results from our laboratories from two structurally related scaffolds have shown promising activity against both Mycobacterium tuberculosis and several parasitic strains. As a result, a small structure activity relationship study was designed to further probe their activity and potential. Their synthesis and the results of the subsequent biological activity are reported herein.

Total synthesis and a systematic structure-activity relationship study of WAP-8294A2

2020 ◽  
Vol 28 (18) ◽  
pp. 115677
Author(s):  
Delin Chen ◽  
Liwen Tian ◽  
Kathy Hiu Laam Po ◽  
Sheng Chen ◽  
Xuechen Li
Keyword(s):  
Total Synthesis ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Systematic Structure ◽  
Relationship Study

scholarly journals Structure–activity relationship study of cationic carbosilane dendritic systems as antibacterial agents

RSC Advances ◽  
2016 ◽  
Vol 6 (9) ◽  
pp. 7022-7033 ◽  
Author(s):  
Elena Fuentes-Paniagua ◽  
Javier Sánchez-Nieves ◽  
José M. Hernández-Ros ◽  
Alba Fernández-Ezequiel ◽  
Juan Soliveri ◽  
...  
Keyword(s):  
Sulfur Atom ◽  
Bactericidal Activity ◽  
Antibacterial Agents ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structural Balance ◽  
Structure Activity ◽  
Relationship Study

The bactericidal activity of a library of cationic dendritic systems depends on the hydrophilic/hydrophobic structural balance, being the presence of a sulfur atom proximal to the peripheral ammonium functions of relevance.

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