title: Synthesis of sydnone substituted Biginelli derivatives as hyaluronidase inhibitors.
abstract: 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.
authors.affiliation: Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad, India.
authors.forename: Tegginamath
authors.initials: T
authors.lastname: Gireesh
authors.forename: Ravindra R
authors.initials: RR
authors.lastname: Kamble
authors.forename: Pramod P
authors.initials: PP
authors.lastname: Kattimani
authors.forename: Atukuri
authors.initials: A
authors.lastname: Dorababu
authors.forename: Maraswamy
authors.initials: M
authors.lastname: Manikantha
authors.forename: Joy H
authors.initials: JH
authors.lastname: Hoskeri
mesh_terms: D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D006821:Hyaluronoglucosaminidase / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D062105:Molecular Docking Simulation; D010078:Oxazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013558:Sydnones / Q000737:chemistry
chemical_list: D000893:Anti-Inflammatory Agents; D004791:Enzyme Inhibitors; D010078:Oxazines; D011743:Pyrimidines; D013558:Sydnones; D006821:Hyaluronoglucosaminidase
keywords: Anti-inflammatory activity; Dihydropyrimidine; Hyaluronidase; Molecular docking; Sydnone