title: Synthesis and biological evaluation of a new class of 4-aminoquinoline-rhodanine hybrid as potent anti-infective agents.
abstract: Synthesis of novel 4-aminoquinoline-rhodanine hybrid using inexpensive starting materials via easy to operate methodology, and their biological activity is reported. All the compounds were screened for their in vitro antimalarial activity against chloroquine-resistant (K1) and chloroquine-sensitive (3D7) strains of Plasmodium falciparum, and their cytotoxicity toward VERO cell line. Compounds 9, 19, 21 and 23 exhibited excellent antimalarial activity with IC50 value ranging from 13.2 to 45.5 nM against chloroquine-resistant (K1) strain. Biochemical studies revealed that inhibition of hemozoin formation is the primary mechanism of action of these analogs for their antimalarial activity. Additionally, some derivatives (14, 18 and 26) of this series also exhibited the antimycobacterial activity against H37Rv strain of Mycobacterium tuberculosis with MIC value of 6.25 μM.
authors: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226001, India.
authors: Kuldeep
authors: K
authors: Chauhan
authors: Moni
authors: M
authors: Sharma
authors: Juhi
authors: J
authors: Saxena
authors: Shiv Vardan
authors: SV
authors: Singh
authors: Priyanka
authors: P
authors: Trivedi
authors: Kumkum
authors: K
authors: Srivastava
authors: Sunil K
authors: SK
authors: Puri
authors: J K
authors: JK
authors: Saxena
authors: Vinita
authors: V
authors: Chaturvedi
authors: Prem M S
authors: PM
authors: Chauhan
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry*; D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D012236:Rhodanine / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000634:Aminoquinolines; D000890:Anti-Infective Agents; D012236:Rhodanine; C001920:4-aminoquinoline