z-logo
Premium
Ultrasound assisted, synthesis of N ‐(7‐(R)‐2‐oxa‐8‐azabicyclo[4.2.0]octan‐8‐yl)isonicotinamide derivatives and their biological evaluation
Author(s) -
Chavan Pravin,
Salve Amol,
Jadhav Shivaji,
Pansare Dattatraya,
Rai Megha
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3860
Subject(s) - azetidine , chemistry , dihydropyran , antibacterial activity , catalysis , cycloaddition , proton nmr , antimicrobial , staphylococcus aureus , stereochemistry , combinatorial chemistry , organic chemistry , bacteria , biology , genetics
In this study, new series of azetidine derivatives were synthesized ( 4a‐n ) from isoniazide ( 1 ), Aromatic aldehydes ( 2a‐n ), dihydropyran ( 3 ) using SnCl 2 catalyst, via one pot multicomponent reaction/cycloaddition reaction. The synthesized azetidine derivatives were characterized by IR, 1 H NMR and 13 C NMR and have been screened for antimicrobial, antituberculosis and anti‐inflammatory activities. In relation to Staphylococcus aureus (ATCC 25923) promising antibacterial activity was shown, compounds 4e and 4k , followed by compounds 4h , 4n , 4f , 4g and 4l . The synthesized azetidine derivatives, 4a , 4e , 4j and 4m (with zone 12 mm) displayed antituberculosis activity. But its lower potential than, the standard streptomycin (with zone 18 mm). Further 4d compound alone displayed similar activity.

This content is not available in your region!

Continue researching here.

Having issues? You can contact us here