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Synthesis of Sydnone Substituted Biginelli Derivatives as Hyaluronidase Inhibitors
Author(s) -
Gireesh Tegginamath,
Kamble Ravindra R.,
Kattimani Pramod P.,
Dorababu Atukuri,
Manikantha Maraswamy,
Hoskeri Joy H.
Publication year - 2013
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/ardp.201300118
Subject(s) - hyaluronidase , biginelli reaction , chemistry , docking (animal) , ramachandran plot , stereochemistry , in vitro , enzyme , sydnone , biochemistry , organic chemistry , protein structure , urea , medicine , ring (chemistry) , nursing
A novel series of Biginelli 2 – 3 ( a and b ) and Biginelli‐like compounds 4 – 7 ( a and b ) were synthesized from 3‐aryl‐4‐formylsydnone 1 ( a and b ). Since the crystal structure of hyaluronidase was unavailable, the human hyaluronidase protein structure was used as template and homology modeling was performed, validated by Ramachandran plots and subjected to docking studies along with in vitro anti‐inflammatory activity assessment against hyaluronidase. Compounds 2 – 3 ( a and b ) exhibited potent enzyme inhibition.