Abstract:
:α-Santonin derived new series of 1,2,3-triazoles synthesized through Azide-Alkyne Huisgen 1,3-dipolar cycloaddition reaction between substituted aryl azide and a propargylated α-desmotrosantonin were bio-evaluated for their diminutive effect on ConA induced T-cell and LPS induced B-cell proliferation. Interestingly, most of the synthesized compounds showed better immunosuppressant activity than α-santonin. Triazole derivatives 9, 10, 17, 18, 29, and 30 displayed significant diminutive effect on cell proliferation. Compounds 12 and 13 were found selective against ConA T-cell proliferation exhibiting >90% inhibition at 1 × 10(-6) M concentration. The present study resulted in identification of several triazole derivatives as effective immunosuppressive agents.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Chinthakindi PK,Sangwan PL,Farooq S,Aleti RR,Kaul A,Saxena AK,Murthy YL,Vishwakarma RA,Koul Sdoi
10.1016/j.ejmech.2012.12.018subject
Has Abstractpub_date
2013-02-01 00:00:00pages
365-75eissn
0223-5234issn
1768-3254pii
S0223-5234(12)00740-4journal_volume
60pub_type
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