Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Malaria01:29

Malaria

Malaria pathogenesis in humans reflects a delicate interplay between parasite biology and host response. Clinical illness reflects a host’s immune response to the parasite’s asexual replication cycle, which is often asymptomatic in individuals with partial immunity. From the parasite's perspective, transmission between mosquito and human with minimal host pathology is evolutionarily advantageous. Among the six Plasmodium species infecting humans, P. falciparum and P. vivax dominate in global...
Antifungal Agents01:15

Antifungal Agents

Amphotericin B is a broad-spectrum antifungal agent that exploits structural differences between fungal and mammalian cell membranes. Its amphipathic structure—featuring a hydrophobic polyene-lactone ring and a hydrophilic region containing mycosamine and carboxylic acid groups—enables selective binding to ergosterol, a sterol predominantly found in fungal plasma membranes. This selective interaction underlies the drug’s antifungal activity, although weak binding to cholesterol contributes to...
Anthelminthic Agents01:15

Anthelminthic Agents

Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...
Antiprotozoal Agents01:21

Antiprotozoal Agents

Leishmaniasis is a widespread parasitic disease caused by several Leishmania species. It affects millions of people each year and remains a major public health problem in endemic regions. First-line treatment relies on pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate. Even so, how these drugs work has not been fully clear, especially their interaction with parasite-specific biochemical pathways. One key target is trypanothione reductase (TR), an enzyme that...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

5‑Nitrofuran-Semicarbazone Hybrids as Antitrypanosomal Agents: Structure-Activity Relationship and Nitroreductase Activation.

ACS medicinal chemistry letters·2026
Same author

Synthesis of Methoxylated Benzoxanthones as Drug Metabolites of Antischistosomal Schistodiones-A Limited Environmental Risk.

Molecules (Basel, Switzerland)·2026
Same author

A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 3: from lead towards a drug development candidate.

The Journal of antimicrobial chemotherapy·2026
Same author

A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 1: setting the stage.

The Journal of antimicrobial chemotherapy·2026
Same author

A Systematic Benchmark Study of Free Energy Methods for Quantifying Light-Responsive Binding Affinities of Photoswitchable Antagonists of Beta-Adrenergic Receptors.

Journal of medicinal chemistry·2026
Same author

A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 2: from molecule to confirmed hit.

The Journal of antimicrobial chemotherapy·2026

Related Experiment Video

Updated: Jun 16, 2026

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
08:48

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation

Published on: January 26, 2016

11.9K

Structural Optimization of BIPPO Analogs as Potent Antimalarials.

Yang Zheng1, An Matheeussen2, Louis Maes2

  • 1Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems, Faculty of Science, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.

Molecules (Basel, Switzerland)
|July 14, 2023
PubMed
Summary

Researchers enhanced antimalarial drug discovery by modifying the BIPPO compound. A new analog, NPD-3547, showed significantly improved potency against Plasmodium falciparum, offering a promising lead for future malaria treatments.

Keywords:
BIPPO analogsantimalarialstructural optimization

More Related Videos

An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity
12:02

An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity

Published on: November 2, 2016

12.1K
Author Spotlight: Identifying Compensatory Pathways in Malaria Parasites Containing Hypomorphic Allele of Essential Protein Kinases
09:13

Author Spotlight: Identifying Compensatory Pathways in Malaria Parasites Containing Hypomorphic Allele of Essential Protein Kinases

Published on: November 22, 2024

1.4K

Related Experiment Videos

Last Updated: Jun 16, 2026

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
08:48

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation

Published on: January 26, 2016

11.9K
An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity
12:02

An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity

Published on: November 2, 2016

12.1K
Author Spotlight: Identifying Compensatory Pathways in Malaria Parasites Containing Hypomorphic Allele of Essential Protein Kinases
09:13

Author Spotlight: Identifying Compensatory Pathways in Malaria Parasites Containing Hypomorphic Allele of Essential Protein Kinases

Published on: November 22, 2024

1.4K

Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Malaria remains a critical global health challenge, exacerbated by limited treatment options and increasing drug resistance.
  • Existing antimalarial therapies face challenges due to resistance and availability issues.

Purpose of the Study:

  • To improve the antimalarial efficacy of the lead compound BIPPO.
  • To identify novel pyrazolopyrimidinone analogs with enhanced activity against Plasmodium falciparum.

Main Methods:

  • Systematic chemical modification of the pyrazolopyrimidinone scaffold.
  • In vitro potency testing against Plasmodium falciparum.
  • Assessment of metabolic stability using mouse liver microsomes.

Main Results:

  • A novel analog, NPD-3547 (compound 30), demonstrated a one log unit increase in antimalarial potency (pIC50 6.8) compared to BIPPO (pIC50 5.9).
  • Several other analogs (compounds 23, 28, 29, 47a) displayed potent antimalarial activity (pIC50 > 6.0) and good metabolic stability.
  • Identified compounds serve as valuable starting points for further antimalarial drug development.

Conclusions:

  • The study successfully identified potent antimalarial pyrazolopyrimidinone analogs with improved properties.
  • NPD-3547 and related compounds represent promising leads for developing new therapeutic strategies against malaria.
  • Further optimization of these analogs could yield novel drug candidates for combating malaria.