Synthesis and Evaluation of Anticonvulsant and Antimicrobial Activities of 3‐Hydroxy‐6‐methyl‐2‐substituted 4H‐Pyran‐4‐one Derivatives.

Abstract

are prepared by Mannich reaction of allomaltol with substituted piperazine derivatives. Their anticonvulsant activities are determined in vivo by maximal electroshock (MES), subcutaneous Metrazo (scMet), and rotorod toxicity tests for neurological deficits. The antimicrobial activities of the new compounds are investigated in vitro against some bacteria and fungi using the microdilution broth method. -(AYTEMIR*, M. D.; CALIS, U.; OEZALP, M.; Arch. Pharm. (Weinheim, Ger.) 337 (2004) 5, 281-288; Dep. Pharm. Chem., Fac. Pharm., Hacettepe Univ., TR-06100 Ankara, Turk.; Eng.) -H. Haber 36-223

Synthesis and biological activities of new Mannich bases of chlorokojic acid derivatives

“…They are good ligands for the nucleophilic and electrophilic substitution reactions (Ichimoto and Tatsumi, 1965;Uher et al, 2000). Therefore, many researchers used them for starting or intermediate material for preparation of new compounds (O'brien et al, 1960;Ichimoto and Tatsumi, 1965;Ellis et al, 1996;Aytemir et al, 2003Aytemir et al, , 2004Dehkordi et al, 2008). In this study, chlorokojic acid was used as the starting material.…”

“…It was synthesized from commercially available kojic acid in one-step reaction according to literature. Chlorination of 2-hydroxymethyl moiety of kojic acid using clean thionyl chloride at room temperature afforded chlorokojic acid (Ellis et al, 1996;Aytemir et al, 2003Aytemir et al, , 2004.…”

“…Previous antimicrobial activity studies showed that kojic acid and its derivatives have antibacterial activity (Kotani et al, 1975;Pirselova et al, 1996;Aytemir et al, 2003;Bentley, 2006;Fassihi et al, 2009). Moreover, 2-chloromethyl-5-hydroxy-4H-pyran-4-one (chlorokojic acid) inhibited Aeromonas aerogenes, Micrococcus pyogenes var.…”

“…Also, their copper(II) salts' complex derivatives were prepared and found to be more active than chlorokojic acid (Brtko et al, 2004). It was shown that kojic acid derivatives were determined as having significant antifungal effects against different Candida species and Pythium graminicola by the different researchers (Kayahara et al, 1990;Aytemir et al, 2003Aytemir et al, , 2004Fassihi et al, 2009). According to its antibacterial and fungicidal properties, kojic acid is used as a food additive to prevent browning (Burdock et al, 2001;Brtko et al, 2004;Bentley, 2006).…”

“…According to its antibacterial and fungicidal properties, kojic acid is used as a food additive to prevent browning (Burdock et al, 2001;Brtko et al, 2004;Bentley, 2006). Moreover, kojic acid derivatives exhibit a number of interesting bioactivities including herbicidal (Veverka and Kralovicova, 1990), anti-speck (Uchino et al, 1988), pesticide and insecticide (Alverson, 2003), antitumor activity (Higa et al, 2007), anti-diabetic (Xiong and Pirrung, 2008), antiepileptic (Aytemir et al, 2004(Aytemir et al, , 2010, modest anti-inflammatory effect (Brtko et al, 2004), and as a skin-whitening product in cosmetic (Burdock et al, 2001;Bentley, 2006).…”