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 A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5847
Author(s):  
Satheesh Gujarathi ◽  
Maroof Khan Zafar ◽  
Xingui Liu ◽  
Robert L. Eoff ◽  
Guangrong Zheng
Keyword(s):  
Natural Product ◽  
Dna Polymerase ◽  
Activity Relationship ◽  
Synthetic Method ◽  
Valuable Insight ◽  
Dna Polymerase Β ◽  
Sar Studies ◽  
Human Dna ◽  
Structure Activity ◽  
Insight Into

Garcinoic acid has been identified as an inhibitor of DNA polymerase β (pol β). However, no structure-activity relationship (SAR) studies of garcinoic acid as a pol β inhibitor have been conducted, in part due to the lack of an efficient synthetic method for this natural product and its analogs. We developed an efficient semi-synthetic method for garcinoic acid and its analogs by starting from natural product δ-tocotrienol. Our preliminary SAR studies provided a valuable insight into future discovery of garcinoic acid-based pol β inhibitors.

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.

Synthesis, Antimalarial Activity, and Structure–Activity Relationship of 7-(2-Phenoxyethoxy)-4(1H)-quinolones

2011 ◽  
Vol 54 (24) ◽  
pp. 8321-8327 ◽  
Author(s):  
R. Matthew Cross ◽  
Niranjan K. Namelikonda ◽  
Tina S. Mutka ◽  
Lisa Luong ◽  
Dennis E. Kyle ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of

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.

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