The present work deals with the synthesis and evaluation of biological activities of 4-aminoantipyrine derivatives derived from a three-component Betti reaction. The synthesis was initiated by the condensation of aromatic aldehyde, 4-aminoantipyrine, and 8-hydroxyquinoline in presence of fluorite as catalyst in a simple one-step protocol. The reactions were stirred at room temperature for 10–15？min achieving 92–95% yield. The structures of synthesized derivatives were established on the basis of spectroscopic and elemental analysis. All derivatives 4(a–h) were screened in vivo and in vitro for anti-inflammatory and anthelmintic activity against a reference drug, Diclofenac and Albendazole, respectively. The screening results show that compounds 4c, 4d, 4f, and 4h were found to possess potential anti-inflammatory activity while compounds 4a, 4b, 4e, and 4g are potent anthelmintic agents when compared with reference drugs, respectively. The bioactivity of these derivatives has also been evaluated with respect to Lipinski’s rule of five using molinspiration cheminformatics software. 1. Introduction Multicomponent reactions (MCRs) have appeared as an imperative means for the construction of diverse and complex organic molecules [1]. They have intrinsic advantages over two component reactions in several aspects including the simplicity of a one-pot procedures and possible structural variation. The synthetic competence comes from several tandem bond formation reactions in MCRs, which save time, energy, and raw material. Betti reaction is a modified type of Mannich reaction [2] which has subsequently become vital in synthetic chemistry because of C–C bond formation under mild experimental conditions. Interest in the chemistry of Betti reaction derivatives was also strengthened as it was found to possess various catalytic and biological applications [3–5]. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most clinically important medicine used for the treatment of inflammation-related diseases like arthritis, asthma, and cardiovascular diseases [6]. However, the long-term administration of NSAID may induce gastrointestinal ulcers, bleeding, and renal disorders due to their nonselective inhibition of both constitutive (COX-1) and inducible (COX-2) isoforms of the cyclooxygenase enzymes [7–9]. Therefore, new anti-inflammatory drugs lacking those effects are being searched all over the world as alternatives to NSAIDs [10]. Due to the emerging need of improved and highly selective inhibitors of COX-2, various heterocyclic compounds are synthesized amongst
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