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.

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 synthetic hydrazines as ecdysone agonists in the control of spruce budworm (Choristoneurafumiferana)

1995 ◽  
Vol 73 (4) ◽  
pp. 550-557 ◽  
Author(s):  
Anmar K. Mohammed-Ali ◽  
Tak-Hang Chan ◽  
Anthony W. Thomas ◽  
George M. Strunz ◽  
Brent Jewett
Keyword(s):  
Biological Activity ◽  
Spruce Budworm ◽  
Quantitative Structure Activity Relationship ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Quantitative Structure ◽  
Molecular Mechanics Calculations ◽  
Structure Activity ◽  
Relationship Study ◽  
Ecdysone Agonist

A quantitative structure–activity relationship study was performed for a number of aroylhydrazine compounds with respect to their biological activity against spruce budworm. It was found that the biological activity can be modulated by substituents on the aromatic rings. Substituents with high π value and small L value lead to increase in biological activity. Molecular mechanics calculations were used to explain how the active compounds may mimic the strong-binding Y region of ecdysone. Keywords: spruce budworm, ecdysone, agonist, hydrazines, quantitative structure–activity relationship.

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.

Biological Activity of Trans-Membrane Anion Carriers

2018 ◽  
Vol 25 (30) ◽  
pp. 3560-3576 ◽  
Author(s):  
Massimo Tosolini ◽  
Paolo Pengo ◽  
Paolo Tecilla
Keyword(s):  
Biological Activity ◽  
Membrane Transport ◽  
Anticancer Agents ◽  
Biological Effects ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Anion Channels ◽  
Cellular Homeostasis ◽  
Structure Activity

Natural and synthetic anionophores promote the trans-membrane transport of anions such as chloride and bicarbonate. This process may alter cellular homeostasis with possible effects on internal ions concentration and pH levels triggering several and diverse biological effects. In this article, an overview of the recent results on the study of aniontransporters, mainly acting with a carrier-type mechanism, is given with emphasis on the structure/activity relationship and on their biological activity as antibiotic and anticancer agents and in the development of new drugs for treating conditions derived from dysregulation of natural anion channels.

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