Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents

New sulfone and sulfanyl derivatives with antifungal activity

“…Many of these derivatives, particularly compounds: 6 and 9 showed goood antifungal actitivy against C. albicans. In line with previous studies (6,17), performed structure-activity analysis revealed that the presence of the electron-withdrawing groups such as -CF 3 and/ or halogens: -F, -Br, -Cl, and -I, generally enhanced the antifungal potential of the tested derivatives. On the contrary to results obtained by Zhao et al 17, we found that electrondonating groups, such as -CH 3 also contribute to increased antifungal potential.…”

“…The present study was focused on the investigation of a series of new 17 synthesized sulfanyl and sulfone derivatives for their anti-Candida activity. Benozothiazole, benzoxazole, nitrobenzene or benzimidazole rings were chosen as scaffolds for the synthesis of sulfur-organic derivatives based on their antifungal potential (6,17). Many of these derivatives, particularly compounds: 6 and 9 showed goood antifungal actitivy against C. albicans.…”

Novel 1,2,3-triazolium-functionalized starch derivatives: Synthesis, characterization, and evaluation of antifungal property

“…The results indicate that increasing the length of the alkyl chain on the 1,2,3-triazolium rings results in a decrease in antifungal activity of starch derivatives (P < 0.05) against all the targeted microorganisms and the antifungal activity increases in the order of 2a > 2b > 2c > 2d > 1a ∼ 1d > starch. It was in accordance with the conclusions of Chandrika et al (2016), Garudachari, Isloor, Satyanarayana, Fun, and Hegde (2014); Yao et al, 2012; while some studies had shown that an increase in chain length of alkyl substituted groups corresponded with an increase in antifungal activity (Zhao et al, 2016). The reasonable interpretation was that the longer alkyl groups had the stronger electron-donating ability and tended to donate more electrons to 1,2,3-triazolium moieties accordingly, which inevitably caused the decrease in the positive charge density of 1,2,3-triazolium moieties and eventually led to reducing in antifungal property (Guo et al, 2007).…”

Synthesis and biological activity of novel benzoazoles, benzoazines and other analogs functionalized by 2,4-dihydroxyphenyl moiety

“…Recently, there have been various approaches to study the role of the benzothiazole moiety as antimicrobial [20][21][22][23], anticancer [24][25][26][27] and antifungal agents [22,[28][29][30]. It has been shown that some benzothiazole dimers were free from irritation, teratogenicity and sensitivity properties compared to monomers and that the increase in the hydrogen donor count is conductive for cytotoxic activity of derivatives against the HL-60 cell lines [31].…”