Design, synthesis and antitubercular activity of diarylmethylnaphthol derivatives

• Published in: Bioorganic & medicinal chemistry letters Vol. 17; no. 20; pp. 5586 - 5589
• Main Authors: Das, Sajal Kumar, Panda, Gautam, Chaturvedi, Vinita, Manju, Y.S., Gaikwad, Anil K., Sinha, Sudhir
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 15.10.2007; Elsevier
• Subjects: Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antitubercular; Antitubercular Agents - chemical synthesis; Antitubercular Agents - chemistry; Antitubercular Agents - pharmacology; Biological and medical sciences; Diarylmethylnaphthol derivatives; Drug Design; Fridel-Crafts; Medical sciences; Methylation; Molecular Structure; Mycobacterium tuberculosis - drug effects; Naphthols - chemical synthesis; Naphthols - chemistry; Naphthols - pharmacology; Pharmacology. Drug treatments; Structure-Activity Relationship; Antitubercular; Fridel-Crafts; Diarylmethylnaphthol derivatives; Benzene derivatives; Aminoether; Condensed benzenic compound; In vitro; Mycobacterium tuberculosis; Structure activity relation; Mycobacteriales; Chlorine Organic compounds; Mycobacteriaceae; Tertiary amine; Bicyclic compound; Bacteria; Actinomycetes; Antituberculous agent; Fluorine Organic compounds; Antibacterial agent; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2007.07.089

A new series of diarylmethylnapthyloxy ethylamines were synthesized by aminoalkylation of diarylmethylnaphthols which were obtained by Friedel–Crafts alkylation on 1- and 2-naphthols using diarylcarbinols as the alkylating agents. The title compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis H 37 R v in vitro and showed MIC in the range of 3.12–25 μg/ml.