Evidence map›Paper›PMID 39425665›Full record

ArticleJournal of medicinal chemistry2024

Optimization of B-Ring-Functionalized Antimalarial Tambjamines and Prodiginines.

Amrendra Kumar, Sivanna Chithanna, Yuexin Li, Xiaowei Zhang, Rozalia A Dodean, Diana Caridha, Michael S Madejczyk, Patricia J Lee, Xiannu Jin, Ravi Chetree and 11 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

6 citing papers in PubMed.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

21 authors.

Amrendra KumarDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.
Sivanna ChithannaDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.
Yuexin LiDepartment of Veterans Affairs Medical Center, Portland, Oregon 97239, United States.
Xiaowei ZhangDepartment of Veterans Affairs Medical Center, Portland, Oregon 97239, United States.
Rozalia A DodeanDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0001-5002-4607
Diana CaridhaExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Michael S MadejczykExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Patricia J LeeExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Xiannu JinExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Ravi ChetreeExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Cameron BlountExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
William E DennisExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Jesse DeLucaExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Chau VuongExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Kristina PannoneExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Hieu T DinhExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Susan LeedExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Alison RothExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Kevin A ReynoldsDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0003-0270-9809
Jane X KellyDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0001-8871-0207
Papireddy KancharlaDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0002-6381-1236

Funding

Novel Multiple-Stage Active AntimalarialsR01AI141972 · NIAID · PORTLAND STATE UNIVERSITY · PI JANE X KELLY, Papireddy Kancharla · 2019 to 2026
$4.5M
Natural Product Inspired Novel Antimalarials with Radical Cure PotentialR01AI175444 · NIAID · PORTLAND STATE UNIVERSITY · PI JANE X KELLY, Papireddy Kancharla · 2023 to 2026
$2.5M
NIAID NIH HHS R01 AI141972NIAID NIH HHS R01 AI175444
6 · The paper itself

Abstract

Malaria has been a deadly enemy of mankind throughout history, affecting over 200 million people annually, along with approximately half a million deaths. Resistance to current therapies is of great concern, and there is a dire need for novel and well-tolerated antimalarials that operate by clinically unexploited mechanisms. We have previously reported that both tambjamines and prodiginines are highly potent novel antiplasmodial agents, but they required rigor optimizations to enhance the oral efficacy, safety, and physicochemical properties. Here, we launched a comprehensive structure-activity relationship study for B-ring-functionalized tambjamines and prodiginines with 54 novel analogues systematically designed and synthesized. A number of compounds exhibited remarkable antiplasmodial activities against asexual erythrocytic

Indexed as

AntimalarialsMalariaAnimalsHumansMicePlasmodium bergheiPlasmodium falciparumPlasmodium yoeliiProdigiosinStructure-Activity RelationshipAntimalarialsprodiginineProdigiosin

Identifiers

PMID39425665
PMCPMC11563898

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.