Antimicrobial activity of ortho-aminomethylphenols and their derivatives

Molodykh, Zh. V.; Kudryavtseva, L. A.; Shagidullina, R. A.; Shtanova, L. V.; Teitel'baum, A. B.; Zotova, A. M.; Рыжкина, И. С.; Kudrina, M. A.; Anisimova, N. N.; Ivanov, B. E.

doi:10.1007/bf00765108

Cited by 2 publications

(2 citation statements)

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“…Recently, 4-hydroxychalcones have demonstrated their effectiveness as cytotoxic [8,9], antitumor [10,11] antioxidative [10], antibacterial [12], antifungal [13], antileishmanial [14], and antinociceptive [15] agents. Antimicrobial [16] and mosquito repellent [17] activities of orthoaminomethyl phenol derivatives (Mannich phenols) are also noteworthy.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 4′‐Hydroxy‐3′‐piperidinomethylchalcone Derivatives and Their Cytotoxicity Against PC‐3 Cell Lines

Gül¹,

Yerdelen

Gül

et al. 2007

Archiv der Pharmazie

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A new series of mono Mannich bases of 4'-hydroxychalcones 2a-e carrying a variety of aryl groups was synthesized and the in vitro cytotoxic activities of the new compounds were screened against PC-3 cell lines. Bioactivities of 2a-e, which are reported for the first time in this study, were compared against their precursor 4'-hydroxychalcones 1a-e. Compound 2b was found to be the most potent (IC(50 )= 3.7 microM) among the compounds synthesized. In addition, the compounds 1a-c and 2d showed moderate cytotoxicity. Incorporation of the 3'-piperidinomethyl group in 1b and 1d raised the potency by 1.68 and 2.19 times respectively and, therefore, seemed to be a noteworthy molecular modification. Correlations were noted between cytotoxicity and one or more physiochemical constants of the aryl ring as well as log P values for the compounds 2a-e. The significant improvement of cytotoxicity of 2b, 2d, and 2e against PC-3 cell lines compared with their chalcone precursors suggests that the incorporation of a piperidinomethyl group is a useful molecular modification and further development of these compounds as candidate cytotoxic agents may be warranted.

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Section: Introductionmentioning

confidence: 99%

Synthesis of 4′‐Hydroxy‐3′‐piperidinomethylchalcone Derivatives and Their Cytotoxicity Against PC‐3 Cell Lines

Gül¹,

Yerdelen

Gül

et al. 2007

Archiv der Pharmazie

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show abstract

“…4-Hydroxychalcones have demonstrated their effectiveness as cytotoxic 7,8 , antitumour 9 , antioxidant 9 agents. The antimicrobial 10 and mosquito repellent 11 activities of o-aminomethyl phenol derivatives (Mannich phenols) are also noteworthy. In view of potential cytotoxicity associated with 4′-hydroxychalcones and Mannich ketones, we were interested in preparing a novel series of Mannich chalcones (2a-f, 4a-e Scheme 1) in order to explore their effectiveness as potent cytotoxic agents.…”

Section: Introductionmentioning

confidence: 99%