title: Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
abstract: Synthesis of a series of novel and functionalized benzimidazole derivatives by the condensation of OPDA with 4-bromobenzoic acid and subsequent reactions of the product obtained with phenylacetylene and 6-ethynyl-4,4-dimethylthiochroman utilising Sonogashira coupling has been reported. The Sonogashira coupling products were then alkylated at the benzimidazole -NH with different electrophilic reagents leading to functionalized derivatives. All the compounds synthesized were screened for their potential anti-bacterial, anti-asthmatic and anti-diabetic properties, which exhibited moderate activities in screening studies in vitro.
authors.affiliation: Glenmark Research Center, Plot No. A-607, T.T.C. Industrial Area, M.I.D.C. Mahape, Navi Mumbai 400 709, India. rvinodk@yahoo.com
authors.forename: Ramanatham
authors.initials: R
authors.lastname: Vinodkumar
authors.forename: Sanjay Dashrath
authors.initials: SD
authors.lastname: Vaidya
authors.forename: Bobba Venkata
authors.initials: BV
authors.lastname: Siva Kumar
authors.forename: Umesh Nanasaheb
authors.initials: UN
authors.lastname: Bhise
authors.forename: Shekhar Bhaskar
authors.initials: SB
authors.lastname: Bhirud
authors.forename: Uday Chandrakant
authors.initials: UC
authors.lastname: Mashelkar
mesh_terms: D000480:Alkynes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018927:Anti-Asthmatic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D054873:Dipeptidyl-Peptidase IV Inhibitors; D006574:Heterocyclic Compounds, 2-Ring / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D058988:Phosphodiesterase 4 Inhibitors; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship