biostudies-literatureKumari ADepartment of Pharmaceuticals, Ministry of Chemicals and Fertilizers, India320-326https://www.ebi.ac.uk/biostudies/studies/S-EPMC8942235biostudies-literatureUnknown13(3)2-Arylquinazolines with a range of alkyl polyamines as side chain/ring functional motifs at the 4th-position were considered for antileishmanial study with the rationale that related heterocyclic scaffolds and polyamine functionalities are present in drugs, clinical trial agents, natural products and anti-parasitic/leishmanial agents. Synthesis involves construction of the 2-arylquinazolin-4-one ring and deoxyamination <i>via</i> deoxychlorination followed by S_NAr-based amination or a methodology of S_NAr-deoxyamination driven by BOP-mediated hydroxyl-activation. Various alkyl-polyamines important for activities were incorporated. A total of 26 compounds were prepared and screened against <i>Leishmania donovani</i> (<i>Ld</i>) promastigote cells using the MTT assay. MoRSC medicinal chemistryIdentification of 2-arylquinazolines with alkyl-polyamine motifs as potent antileishmanial agents: synthesis and biological evaluation studies.PMC8942235KA-01Acharya AKumar VKumar GJaiswal TBabu NKHura NKumari AGuchhait SKSingh SRoy PKfalseIdentification of 2-arylquinazolines with alkyl-polyamine motifs as potent antileishmanial agents: synthesis and biological evaluation studies.2-Arylquinazolines with a range of alkyl polyamines as side chain/ring functional motifs at the 4th-position were considered for antileishmanial study with the rationale that related heterocyclic scaffolds and polyamine functionalities are present in drugs, clinical trial agents, natural products and anti-parasitic/leishmanial agents. Synthesis involves construction of the 2-arylquinazolin-4-one ring and deoxyamination <i>via</i> deoxychlorination followed by S_NAr-based amination or a methodology of S_NAr-deoxyamination driven by BOP-mediated hydroxyl-activation. Various alkyl-polyamines important for activities were incorporated. A total of 26 compounds were prepared and screened against <i>Leishmania donovani</i> (<i>Ld</i>) promastigote cells using the MTT assay. Mo2022-01-01T00:00:00Z2022 Mar2025-04-22T04:27:01.579Z2025-04-05T21:00:31.312ZS-EPMC89422353543463110.1039/d1md00336d