Synthesis and Anticandidal Activity of Azole‐Containing Sulfonamides

Abstract

Twenty five benzenesulfonamides containing one imidazole or triazole ring, or two imidazole or triazole rings have been synthesized and evaluated as anticandidal agents. The most active compounds were 5c, 6b, 6c, 6e, and 17b, which exhibited MIC values of 4.55-24.39 mM depending on the clinical isolate. Comparing imidazole to triazole derivatives did not show a clear effect on activity. Compounds containing a N-benzyl group also showed no clear evidence on activity given the fact that they have an extra aromatic ring. Secondary sulfonamides, 5l, 5m, and 5n showed activities that were proportional to their lipophilicity. The activities of N-aryl-substituted derivatives 5j, 5k, 5l, 5m, 5n, and 6j were also proportional to their lipophilicity. Halogenation enhanced the activity as a result of improvement of lipophilicity. The presence of two imidazole or triazole rings in the same compound did not show a clear enhancement of activity.

Synthesis and evaluation of α-Ag2WO4 as novel antifungal agent

“…To the best of our knowledge, the antifungal properties of a-Ag 2 WO 4 microcrystals have never been evaluated to date. Recently, there has been a dramatic increase in the frequency of systemic fungal infection, and in particular, Candida albicans (CA) is a major human pathogen that causes local and life-threatening systemic infections [16]. Therefore, the discovery of new antifungal materials with greater potency against CA is becoming not only a hot research subject but also a compelling challenge.…”

Synthesis and Spectroscopic Analysis of Novel 1H-Benzo[d]imidazoles Phenyl Sulfonylpiperazines

“…The benzimidazole 1 was then chlorosulfonated selectively at the para -position of the anisyl moiety and the resultant sulfonyl chloride was extensively washed with water and used in the next step without further purification. To obtain the final compounds, the sulfonyl chloride, dissolved in dichloromethane, was coupled to 1-methylpiperazine, N -ethylpiperazine and piperazine dihydrochloride in the presence of excess amounts of triethylamine [24,25]. The resultant amines were then converted to the hydrochloride salts and purified by crystallization from methanol/ethyl acetate to afford compounds 2, 3 and 4 in good yields.…”

Synthesis and Evaluation of Prodrugs of Ketoprofen with Antioxidants as Gastroprotective NSAIDs

“…These natural phytophenols/alcohol have shown not only the antioxidant properties, but also antimutagenic, anticarcinogenic, anti-inflammatory properties [14,15]. Thus ketoprofen-phytophenols/alcohol mutual prodrugs were prepared with the objective to get not only the complementary/additional [16,17] and synergistic pharmacological actions [18], but also the reduced gastrointestinal side effects. These naturally occurring compounds have been traditionally in use as a food additive and have well documented safety profile [19].…”