Structure-activity and structure-property relationship studies of spirocyclic chromanes with antimalarial activity

[Display omitted] Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel line of therapy that could overcome, the problem of drug resistance, is imperative. Screening of a set of compounds with dru...

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Published inBioorganic & medicinal chemistry Vol. 57; p. 116629
Main Authors Iyamu, Iredia D., Zhao, Yingzhao, Parvatkar, Prakash T., Roberts, Bracken F., Casandra, Debora R., Wojtas, Lukasz, Kyle, Dennis E., Chakrabarti, Debopam, Manetsch, Roman
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 01.03.2022
Elsevier
Subjects
Antimalarial
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Biochemistry & Molecular Biology
Cell Survival - drug effects
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Chromans - chemical synthesis
Chromans - chemistry
Chromans - pharmacology
Crystallography, X-Ray
Dose-Response Relationship, Drug
Drug resistance
Hep G2 Cells
Humans
Life Sciences & Biomedicine
Malaria - drug therapy
Models, Molecular
Molecular Structure
Natural products
Parasitic Sensitivity Tests
Pharmacology & Pharmacy
Physical Sciences
Plasmodium - drug effects
Science & Technology
Spiro Compounds - chemical synthesis
Spiro Compounds - chemistry
Spiro Compounds - pharmacology
Spirocyclic chromane
Structure-Activity Relationship
Structure-property relationship
Antimalarial
Structure-property relationship
Drug resistance
Natural products
Spirocyclic chromane
Structure-activity relationship
ENANTIOSELECTIVE SYNTHESIS
NATURAL-PRODUCTS
OPTIMIZATION
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Abstract [Display omitted] Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel line of therapy that could overcome, the problem of drug resistance, is imperative. Screening of a set of compounds with drug/natural product-based sub-structural motifs led to the identification of spirocyclic chroman-4-one 1 with promising antimalarial activity against the chloroquine-resistant Dd2 and chloroquine-sensitive 3D7 strains of the parasite. Extensive structure-activity and structure-property relationship studies were conducted to identify the essential features necessary for its activity and properties.
AbstractList Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel line of therapy that could overcome, the problem of drug resistance, is imperative. Screening of a set of compounds with drug/natural product-based sub-structural motifs led to the identification of spirocyclic chroman-4-one 1 with promising antimalarial activity against the chloroquine-resistant Dd2 and chloroquine-sensitive 3D7 strains of the parasite. Extensive structure-activity and structure-property relationship studies were conducted to identify the essential features necessary for its activity and properties.
Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel line of therapy that could overcome, the problem of drug resistance, is imperative. Screening of a set of compounds with drug/natural product-based sub-structural motifs led to the identification of spirocyclic chroman-4-one 1 with promising antimalarial activity against the chloroquine-resistant Dd2 and chloroquine-sensitive 3D7 strains of the parasite. Extensive structure-activity and structure-property relationship studies were conducted to identify the essential features necessary for its activity and properties.
[Display omitted] Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel line of therapy that could overcome, the problem of drug resistance, is imperative. Screening of a set of compounds with drug/natural product-based sub-structural motifs led to the identification of spirocyclic chroman-4-one 1 with promising antimalarial activity against the chloroquine-resistant Dd2 and chloroquine-sensitive 3D7 strains of the parasite. Extensive structure-activity and structure-property relationship studies were conducted to identify the essential features necessary for its activity and properties.
ArticleNumber 116629
Author Wojtas, Lukasz
Parvatkar, Prakash T.
Iyamu, Iredia D.
Roberts, Bracken F.
Kyle, Dennis E.
Manetsch, Roman
Chakrabarti, Debopam
Zhao, Yingzhao
Casandra, Debora R.
AuthorAffiliation Molecular Microbiology Division, Burnett School of Biomedical Science, University of Central Florida, 12722 Research Parkway, Orlando, Florida 32826, USA
Department of Chemistry, University of South Florida, 4202 E. Fowler Ave, Tampa, Florida 33620, USA
ϕ Center for Tropical and Emerging Global Diseases, University of Georgia, Athens, 500 D.W. Brooks Dr, Athens, Georgia 30602, USA
Department of Pharmaceutical Sciences, Bouvé College of Pharmacy, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, USA
Center for Drug Discovery, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, USA
Department of Global Health, College of Public health, University of South Florida, 3720 Spectrum Boulevard, Tampa, Florida 33612, USA
Department of Chemistry and Chemical Biology, College of Science, Northeastern University, 360 Huntington Avenue, Boston, Massachusetts 02115, USA
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Keywords Antimalarial
Structure-property relationship
Drug resistance
Natural products
Spirocyclic chromane
Structure-activity relationship
ENANTIOSELECTIVE SYNTHESIS
NATURAL-PRODUCTS
OPTIMIZATION
Language English
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Snippet [Display omitted] Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the...
Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel...
Source Web of Science
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StartPage 116629
SubjectTerms Antimalarial
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Biochemistry & Molecular Biology
Cell Survival - drug effects
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Chromans - chemical synthesis
Chromans - chemistry
Chromans - pharmacology
Crystallography, X-Ray
Dose-Response Relationship, Drug
Drug resistance
Hep G2 Cells
Humans
Life Sciences & Biomedicine
Malaria - drug therapy
Models, Molecular
Molecular Structure
Natural products
Parasitic Sensitivity Tests
Pharmacology & Pharmacy
Physical Sciences
Plasmodium - drug effects
Science & Technology
Spiro Compounds - chemical synthesis
Spiro Compounds - chemistry
Spiro Compounds - pharmacology
Spirocyclic chromane
Structure-Activity Relationship
Structure-property relationship
Title Structure-activity and structure-property relationship studies of spirocyclic chromanes with antimalarial activity
URI https://dx.doi.org/10.1016/j.bmc.2022.116629
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https://www.ncbi.nlm.nih.gov/pubmed/35091169
https://pubmed.ncbi.nlm.nih.gov/PMC9233738
Volume 57
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