title: 4-Aminoquinoline-β-lactam conjugates: synthesis, antimalarial, and antitubercular evaluation.
abstract: A library of quinoline-β-lactam-based hybrids was synthesized and tested for their antimalarial and antitubercular activities. The present antimalarial data showed the dependence of activity on the nature of linker, N-1 substituent of the β-lactam ring as well as the length of alkyl chain. Most of the compounds are not as efficient as chloroquine in inhibiting the culture growth of Plasmodium falciparum W2 strain. Nevertheless, the synthesized hybrids showed better antitubercular activities (up to five times) compared with cephalexin (up to three times) and ethionamide.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar, 143005, India.
authors.forename: Raghu
authors.initials: R
authors.lastname: Raj
authors.forename: Christophe
authors.initials: C
authors.lastname: Biot
authors.forename: Séverine
authors.initials: S
authors.lastname: Carrère-Kremer
authors.forename: Laurent
authors.initials: L
authors.lastname: Kremer
authors.forename: Yann
authors.initials: Y
authors.lastname: Guérardel
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rosenthal
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology; D000962:Antimalarials / Q000138:chemical synthesis / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship; D047090:beta-Lactams / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D000995:Antitubercular Agents; D047090:beta-Lactams; C001920:4-aminoquinoline
keywords: 4-aminoquinoline-β-lactam conjugates; antimalarial evaluation; antitubercular evaluation; molecular hybridization; structure-activity relationship