{"doi":"10.1111/cbdd.12914","title":"Design, synthesis and in vitro antiplasmodial activity of some bisquinolines against chloroquine‐resistant strain","abstract":"<jats:p>A series of novel bisquinoline compounds comprising <jats:italic>N</jats:italic><jats:sup>1</jats:sup>‐(7‐chloroquinolin‐4‐yl) ethane‐1,2‐diamine and 7‐chloro‐<jats:italic>N</jats:italic>‐(2‐(piperazin‐1‐yl)ethyl)quinolin‐4‐amine connected with 7‐chloro‐4‐aminoquinoline containing various amino acids is described. We have bio‐evaluated the compounds against both chloroquine‐sensitive (3D7) and chloroquine‐resistant (K1) strains of <jats:italic>Plasmodium falciparum</jats:italic> in vitro. Among the series, compounds <jats:bold>4</jats:bold> and <jats:bold>7</jats:bold> exhibited 1.8‐ and 10.6‐fold superior activity as compared to chloroquine (CQ; IC<jats:sub>50</jats:sub> = 0.255 ± 0.049 μ<jats:sc>m</jats:sc>) against the K1 strain with IC<jats:sub>50</jats:sub> values 0.137 ± 0.014 and 0.026 ± 0.007 μ<jats:sc>m</jats:sc>, respectively. Furthermore, compound <jats:bold>7</jats:bold> also displayed promising activity against the 3D7 strain (IC<jats:sub>50</jats:sub> = 0.024 ± 0.003 μ<jats:sc>m</jats:sc>) of <jats:italic>P. falciparum</jats:italic> when compared to CQ. All the compounds in the series displayed resistance factor between 0.57 and 4.71 as against 51 for CQ. These results suggest that bisquinolines can be explored for further development as new antimalarial agents active against chloroquine‐resistant <jats:italic>P. falciparum</jats:italic>.</jats:p>","journal":"Chemical Biology &amp; Drug Design","year":2017,"id":662016,"datarank":0.4493598410330987,"base_score":2.995732273553991,"endowment":2.995732273553991,"self_citation_contribution":0.4493598410330987,"citation_network_contribution":0.0,"self_endowment_contribution":0.4493598410330987,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":19,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1420655,"name":"Pooja Agarwal","orcid":null,"position":1,"is_corresponding":false},{"id":1728269,"name":"Kumkum Srivastava","orcid":null,"position":2,"is_corresponding":false},{"id":1728270,"name":"Sunil K. Puri","orcid":null,"position":3,"is_corresponding":false},{"id":1728271,"name":"Seturam B. Katti","orcid":null,"position":4,"is_corresponding":false},{"id":1728268,"name":"Srinivasarao Kondaparla","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Design, synthesis and in vitro antiplasmodial activity of some bisquinolines against chloroquine‐resistant strain","abstract":"<jats:p>A series of novel bisquinoline compounds comprising <jats:italic>N</jats:italic><jats:sup>1</jats:sup>‐(7‐chloroquinolin‐4‐yl) ethane‐1,2‐diamine and 7‐chloro‐<jats:italic>N</jats:italic>‐(2‐(piperazin‐1‐yl)ethyl)quinolin‐4‐amine connected with 7‐chloro‐4‐aminoquinoline containing various amino acids is described. We have bio‐evaluated the compounds against both chloroquine‐sensitive (3D7) and chloroquine‐resistant (K1) strains of <jats:italic>Plasmodium falciparum</jats:italic> in vitro. Among the series, compounds <jats:bold>4</jats:bold> and <jats:bold>7</jats:bold> exhibited 1.8‐ and 10.6‐fold superior activity as compared to chloroquine (CQ; IC<jats:sub>50</jats:sub> = 0.255 ± 0.049 μ<jats:sc>m</jats:sc>) against the K1 strain with IC<jats:sub>50</jats:sub> values 0.137 ± 0.014 and 0.026 ± 0.007 μ<jats:sc>m</jats:sc>, respectively. Furthermore, compound <jats:bold>7</jats:bold> also displayed promising activity against the 3D7 strain (IC<jats:sub>50</jats:sub> = 0.024 ± 0.003 μ<jats:sc>m</jats:sc>) of <jats:italic>P. falciparum</jats:italic> when compared to CQ. All the compounds in the series displayed resistance factor between 0.57 and 4.71 as against 51 for CQ. These results suggest that bisquinolines can be explored for further development as new antimalarial agents active against chloroquine‐resistant <jats:italic>P. falciparum</jats:italic>.</jats:p>","is_dataset_classified":null,"base_score":2.995732273553991,"endowment":2.995732273553991,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"27896925","pmcid":null,"openalex_id":"https://openalex.org/W2559445368","authors":[],"funders":[{"funder_name":"Council for Scientific and Industrial Research","grant_id":"","title":null}],"total_grants":1,"fwci":2.1281,"citation_percentile":0.8935425,"influential_citations":0,"citation_trend":[{"year":2017,"count":3},{"year":2018,"count":3},{"year":2019,"count":1},{"year":2020,"count":2},{"year":2021,"count":4},{"year":2023,"count":3},{"year":2025,"count":2},{"year":2026,"count":1}],"oa_status":"closed","license":"http://onlinelibrary.wiley.com/termsAndConditions#vor","oa_locations":[{"url":"https://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1111%2Fcbdd.12914","host_type":"publisher"},{"url":"https://onlinelibrary.wiley.com/doi/pdf/10.1111/cbdd.12914","host_type":"publisher"},{"url":"https://doi.org/10.1111/cbdd.12914","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/27896925","host_type":"repository"}],"fields_of_study":["Malaria Research and Control","Phenothiazines and Benzothiazines Synthesis and Activities","HIV/AIDS drug development and treatment","Animals","Antimalarials","Chloroquine","Drug Design","Drug Resistance","Inhibitory Concentration 50","Molecular Structure","Plasmodium falciparum","Quinolines"],"mesh_terms":["Animals","Antimalarials","Chloroquine","Drug Resistance","Plasmodium falciparum","Quinolines","Drug Design","Molecular Structure","Inhibitory Concentration 50"],"keywords":["Chloroquine","Plasmodium falciparum","IC50","In vitro","Strain (injury)","Antimalarial Agent","Chemistry","Amine gas treating","Stereochemistry","Pharmacology","Biology","Malaria","Biochemistry","Organic chemistry","Immunology","Antiplasmodial Activity","4-Aminoquinoline","Chloroquine-resistant Strain","Chloroquine-sensitive Strain"],"sdg_mappings":[],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-12T12:15:48.496248Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}