scholarly journals Synthesis and SAR of the antistaphylococcal natural product nematophin from Xenorhabdus nematophila

2019 ◽  
Vol 15 ◽  
pp. 535-541
Author(s):  
Frank Wesche ◽  
Hélène Adihou ◽  
Thomas A Wichelhaus ◽  
Helge B Bode
Keyword(s):  
Natural Product ◽  
Activity Relationship ◽  
Xenorhabdus Nematophila ◽  
Structure Activity ◽  
Multiresistant Bacteria ◽  
Improper Use ◽  
Relationship Of ◽  
First Time ◽  
Synthetic Derivatives ◽  
Fluorescent Derivatives

The repeated and improper use of antibiotics had led to an increased number of multiresistant bacteria. Therefore, new lead structures are needed. Here, the synthesis and an expanded structure–activity relationship of the simple and antistaphylococcal amide nematophin from Xenorhabdus nematophila and synthetic derivatives are described. Moreover, the synthesis of intrinsic fluorescent derivatives, incorporating azaindole moieties was achieved for the first time.

Variability of the antibacterial potential among analogue diterpenes against Gram-positive bacteria: considerations on the structure–activity relationship

2019 ◽  
Vol 97 (7) ◽  
pp. 568-575 ◽  
Author(s):  
Ana Carolina Ferreira Soares ◽  
Priscilla Mendonça Matos ◽  
Herbert Júnior Dias ◽  
Gabriela de Paula Aguiar ◽  
Eliene Silvério dos Santos ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Public Health Problem ◽  
Antibacterial Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Gram Positive ◽  
Structure Activity ◽  
Esterification Reactions ◽  
Relationship Of ◽  
Synthetic Derivatives

The search for new antibacterial agents and a better comprehension of substances with antimicrobial behavior is mandatory nowadays due to the serious public health problem of infection diseases. In the present work, 30 diterpenes were studied, with 2 natural derivatives, named ent-16-kauren-19-oic acid and ent-pimara-8(14),15-dien-19-oic acid, and 28 semi-synthetic derivatives. The natural diterpenes were isolated from Mikania glomerata and Viguiera arenaria, respectively. All diterpenes were submitted to antimicrobial assays against six different Gram-positive microorganisms to better understand the structure–activity relationship of antimicrobial diterpenes. The semi-synthetic derivatives were all obtained from the two natural derivatives by structural modifications, mainly esterification reactions. Both natural derivatives, together with the derivative ent-8(14)-pimaren-19-oic acid, displayed the most relevant antibacterial activities, with minimal inhibitory concentration (MIC) values that were less than 10 μg mL–1 for most pathogens; thus, they were considered promising antimicrobial agents. Moreover, in light of the hypothesis of Urzúa and colleagues, several considerations about the structure–activity relationship of antimicrobial diterpenes could be stated.

Research Progress on the Natural Product Aloperine and Its Derivatives

2021 ◽  
Vol 21 ◽  
Author(s):  
Yu Cheng ◽  
Abdur Rauf ◽  
Xiandao Pan
Keyword(s):  
Natural Product ◽  
Recent Progress ◽  
Molecular Mechanisms ◽  
Structure Activity Relationship ◽  
Research Progress ◽  
Activity Relationship ◽  
Pharmacological Effects ◽  
Structure Activity ◽  
Relationship Of

: In this review, an effort towards the presentation of an all-around account of the recent progress on the natural product, aloperine is made, and the antivirus structure-activity relationship of its derivatives is also summarized comprehensively. In addition, the principal pharmacological effects and corresponding molecular mechanisms of aloperine are discussed. Some new modification directions of aloperine are given in the end, which might be brief guidance for further investigations on the natural product aloperine.

scholarly journals On peroxide antimalarials

2007 ◽  
Vol 72 (12) ◽  
pp. 1181-1190 ◽  
Author(s):  
Igor Opsenica ◽  
Dejan Opsenica ◽  
Milka Jadranin ◽  
Kirsten Smith ◽  
Wilbur Milhous ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Natural Product ◽  
Antimalarial Activity ◽  
Multidrug Resistant ◽  
Activity Relationship ◽  
Similar Activity ◽  
Structure Activity ◽  
Relationship Of ◽  
Insight Into ◽  
Better Than

Several dicyclohexylidene tetraoxanes were prepared in order to gain a further insight into structure-activity relationship of this kind of antimalarials. The tetraoxanes 2-5, obtained as a cis/trans mixture, showed pronounced antimalarial activity against Plasmodium falciparum chloroquine susceptible D6, chloroquine resistant W2 and multidrug-resistant TM91C235 (Thailand) strains. They have better than or similar activity to the corresponding desmethyl dicyclohexylidene derivatives. Two chimeric endoperoxides with superior antimalarial activity to the natural product ascaridole were also synthesized.

scholarly journals Cellular Analysis of Disorazole C1 and Structure-Activity Relationship of Analogs of the Natural Product

2006 ◽  
Vol 67 (1) ◽  
pp. 66-73 ◽  
Author(s):  
Peter Wipf ◽  
Thomas H. Graham ◽  
Andreas Vogt ◽  
Rachel P. Sikorski ◽  
Alexander P. Ducruet ◽  
...  
Keyword(s):  
Natural Product ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Cellular Analysis ◽  
Structure Activity ◽  
Relationship Of ◽  
Disorazole C1

scholarly journals Investigating the Structure–Activity Relationship of the Insecticidal Natural Product Rocaglamide

2017 ◽  
Vol 71 (12) ◽  
pp. 845-850
Author(s):  
Roger G. Hall ◽  
Ian Bruce ◽  
Nigel G. Cooke ◽  
Louis J. Diorazio ◽  
Fredrik Cederbaum ◽  
...  
Keyword(s):  
Natural Product ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of

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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