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Synthesis and Biological Evaluation of a Series of Substituted Pyrazolo[3,4‐ d ]‐1,2,3‐triazoles and Pyrazolo[3,4‐ d ]oxazoles
Author(s) -
Vicentini Chiara B.,
Manfredini Stefano,
Manfrini Maurizio,
Bazzanini Rita,
Musiu Chiara,
Putzolu Monica,
Perra Graziella,
Marongiu Maria E.
Publication year - 1998
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/(sici)1521-4184(19989)331:9<269::aid-ardp269>3.0.co;2-7
Subject(s) - series (stratigraphy) , stereochemistry , chemistry , combinatorial chemistry , biology , paleontology
In view of the biological relevance of triazole‐based heterocyclic structures as antifungal, antiviral, and antitumor agents, we have synthesized a series of substituted pyrazolo[3,4‐ d ]‐1,2,3‐triazoles ( 2e–h, 2j, 4b ) which we evaluated for their cytostatic and antiviral (HIV‐1 included) activity and for their capability to inhibit the multiplication of various human pathogenic fungi and bacteria. Moreover, the biological activities of a few compounds, namely pyrazolo[3,4‐ d ]oxazoles ( 3a–e ) and pyrazolo[3,4‐ d ]‐1,2,3‐triazoles ( 2a–d, 4a, 5 ), previously obtained by us but not investigated for their biological activity, were also studied. Only compounds 3a–e were endowed with a significative antiproliferative activity on the human lymphoblastoid cell line MT‐4 cells. All pyrazole derivatives proved ineffective in protecting cell cultures against the HIV‐1‐induced cytopathogenicity, and none of the compounds was active against the bacteria and fungi tested.