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Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies.

ABSTRACT: 4-Chloro-3-nitrophenylthioureas 1?30 were synthesized and tested for their antimicrobial and cytotoxic activities. Compounds exhibited high to moderate antistaphylococcal activity against both standard and clinical strains (MIC values 2?64 ?g/mL). Among them derivatives with electron-donating alkyl substituents at the phenyl ring were the most promising. Moreover, compounds 1?6 and 8?19 were cytotoxic against MT-4 cells and various other cell lines derived from human hematological tumors (CC₅₀ ? 10 ?M). The influence of derivatives 11, 13 and 25 on viability, mortality and the growth rate of immortalized human keratinocytes (HaCaT) was observed.

SUBMITTER: Bielenica A

PROVIDER: S-EPMC6222614 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature

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Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies.

Bielenica Anna A Sanna Giuseppina G Madeddu Silvia S Giliberti Gabriele G Stefańska Joanna J Kozioł Anna E AE Savchenko Oleksandra O Strzyga-Łach Paulina P Chrzanowska Alicja A Kubiak-Tomaszewska Grażyna G Struga Marta M

Molecules (Basel, Switzerland) 20180921 10

4-Chloro-3-nitrophenylthioureas 1⁻30 were synthesized and tested for their antimicrobial and cytotoxic activities. Compounds exhibited high to moderate antistaphylococcal activity against both standard and clinical strains (MIC values 2⁻64 μg/mL). Among them derivatives with electron-donating alkyl substituents at the phenyl ring were the most promising. Moreover, compounds 1⁻6 and 8⁻19 were cytotoxic against MT-4 cells and various other cell lines deriv ...[more]

PMID: 30248936

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