Study of Biological Activities and ADMET-Related Properties of Novel Chlorinated
antimicrobial activity
cinnamamides
cytotoxicity
lipophilicity
structure-activity relationships
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
15 Mar 2022
15 Mar 2022
Historique:
received:
26
02
2022
revised:
11
03
2022
accepted:
13
03
2022
entrez:
25
3
2022
pubmed:
26
3
2022
medline:
9
4
2022
Statut:
epublish
Résumé
A series of eighteen 4-chlorocinnamanilides and eighteen 3,4-dichlorocinnamanilides were designed, prepared and characterized. All compounds were evaluated for their activity against gram-positive bacteria and against two mycobacterial strains. Viability on both cancer and primary mammalian cell lines was also assessed. The lipophilicity of the compounds was experimentally determined and correlated together with other physicochemical properties of the prepared derivatives with biological activity. 3,4-Dichlorocinnamanilides showed a broader spectrum of action and higher antibacterial efficacy than 4-chlorocinnamanilides; however, all compounds were more effective or comparable to clinically used drugs (ampicillin, isoniazid, rifampicin). Of the thirty-six compounds, six derivatives showed submicromolar activity against
Identifiants
pubmed: 35328580
pii: ijms23063159
doi: 10.3390/ijms23063159
pmc: PMC8951032
pii:
doi:
Substances chimiques
Anti-Bacterial Agents
0
Ampicillin
7C782967RD
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Slovak Research and Development Agency
ID : APVV-17-0373
Organisme : VEGA
ID : VEGA 1/0116/22
Organisme : CzeCOS
ID : LM2018123
Organisme : SustES
ID : CZ.02.1.01/0.0/0.0/16_019/0000797
Organisme : FIT
ID : CZ.02.1.01/0.0/0.0/15_003/0000495
Organisme : Czech Ministry of Agriculture
ID : RO0518
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