title: Synthesis, identification and in vitro biological evaluation of some novel quinoline incorporated 1,3-thiazinan-4-one derivatives.
abstract: The present study describes the synthesis of two new series of 3-hydroxy-N-(4-oxo-2-phenyl-1,3-thiazinan-3-yl)-8-(trifluoromethyl)quinoline-2-carboxamide derivatives (4a-j) and 3-((7-chloroquinolin-4-ylamino)methyl)-2-phenyl-1,3-thiazinan-4-one derivatives (5a-7j). All the compounds were synthesized in moderate to good yield by one-pot three component cyclo-condensation reaction. The newly synthesized compounds were characterized by FT-IR,1H,13C NMR and elemental analysis. The compounds were screened for their in vitro antibacterial activity against a panel of pathogenic bacterial strains, antitubercular activity against Mycobacterium tuberculosis H37Rv and also for their in vitro antimalarial activity against Plasmodium falciparum. Among the synthesized compounds two of them (4f and 5f) showed excellent antibacterial activity against C. tetani at 15.6μg/mL. Some of them exhibited excellent antitubercular (4f &5f) and good antimalarial (4f, 5f &6f) activity compared with the first line drugs.
authors.affiliation: Department of Chemistry, Govt. Arts College, Tiruchirappalli, Tamil Nadu 620022, India.
authors.forename: S
authors.initials: S
authors.lastname: Umamatheswari
authors.affiliation: Department of Chemistry, TRP Engineering College, Irungalur, Tiruchirappalli, Tamil Nadu 621 105, India. Electronic address: sankschem@gmail.com.
authors.forename: C
authors.initials: C
authors.lastname: Sankar
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003017:Clostridium tetani / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D000962:Antimalarials; D000995:Antitubercular Agents; D011804:Quinolines; D013843:Thiazines
keywords: Antimalarial; Quinoline; Thiazinan-4-one; Tuberculosis