title: Synthesis and discovery of new bisadducts derived from heterocyclic aldehydes and active methylene compounds as potent antitubercular agents.
abstract: A series of some new bisadducts possessing five, six membered and coumarin subunits were synthesized by the condensation of heterocyclic aldehydes with active methylene compounds and characterized by IR, NMR and X-ray crystallographic studies and were assayed as antitubercular agents. Among the bisadducts, 4-hydroxy-3-[(4-hydroxy-2-oxo-2H-3-chromenyl)(3-thienyl)methyl]-2H-2-chromenone 3a was found to be the most promising compound, active against Mycobacterium tuberculosis (Mtb) H37Rv and isoniazid resistant Mycobacterium tuberculosis (INHR-Mtb) with minimum inhibitory concentration 5.22 and 8.34 microM, respectively.
authors.affiliation: School of Chemical Sciences, University Sains Malaysia, Minden 11800, Penang, Malaysia.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Asad
authors.forename: Chuan-Wei
authors.initials: CW
authors.lastname: Oo
authors.forename: Raju Suresh
authors.initials: RS
authors.lastname: Kumar
authors.forename: Hasnah
authors.initials: H
authors.lastname: Osman
authors.forename: Mohamed Ashraf
authors.initials: MA
authors.lastname: Ali
mesh_terms: D000447:Aldehydes / Q000138:chemical synthesis* / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D055808:Drug Discovery; D024881:Drug Resistance, Bacterial; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000235:genetics / Q000254:growth & development; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship
chemical_list: D000447:Aldehydes; D000995:Antitubercular Agents; D003374:Coumarins