PMID- 33023084 OWN - NLM STAT- MEDLINE DCOM- 20210318 LR - 20210318 IS - 1420-3049 (Electronic) IS - 1420-3049 (Linking) VI - 25 IP - 19 DP - 2020 Oct 2 TI - Design of Organoiron Dendrimers Containing Paracetamol for Enhanced Antibacterial Efficacy. LID - 10.3390/molecules25194514 [doi] LID - 4514 AB - Paracetamol (acetaminophen) is a common painkiller and antipyretic drug used globally. Attachment of paracetamol to a series of organoiron dendrimers was successfully synthesized. The aim of this study is to combine the benefits of the presence of these redox-active organoiron dendrimers, their antimicrobial activities against some human pathogenic Gram-positive, and the therapeutic characteristics of paracetamol. The antimicrobial activity of these dendrimers was investigated and tested with a minimum inhibitory concentration and this has been reported. Some of these newly synthesized dendrimers exhibited the highest inhibitory activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium (VRE), and Staphylococcus warneri compared to reference drugs. The results of this study indicate that the antimicrobial efficacy of the dendrimers is dependent on the size of the redox-active organoiron dendrimer and its terminal functionalities. The best result has been recorded for the fourth-generation dendrimer 11, which attached to 48 paracetamol end groups and has 90 units composed of the eta(6)-aryl-eta(5)-cyclopentadienyliron (II) complex. This dendrimer presented inhibition of 50% of the growth (IC(50)) of 0.52 muM for MRSA, 1.02 muM for VRE, and 0.73 muM for Staphylococcus warneri. The structures of the dendrimers were characterized by elemental analysis, Fourier transform infrared (FT-IR), nuclear magnetic resonance ((1)H-NMR), and (13)C-NMR spectroscopic techniques. In addition, all synthesized dendrimers displayed good thermal stability in the range of 300-350 degrees C following the degradation of the cationic iron moieties which occurred around 200 degrees C. FAU - Abd-El-Aziz, Alaa S AU - Abd-El-Aziz AS AD - Department of Chemistry, University of Prince Edward Island, 550 University Avenue, Charlottetown, PE C1A 4P3, Canada. FAU - El-Ghezlani, Ebtehal G AU - El-Ghezlani EG AD - Department of Chemistry, University of Prince Edward Island, 550 University Avenue, Charlottetown, PE C1A 4P3, Canada. FAU - Abdelghani, Amani A AU - Abdelghani AA AD - Department of Chemistry, University of Prince Edward Island, 550 University Avenue, Charlottetown, PE C1A 4P3, Canada. LA - eng PT - Journal Article DEP - 20201002 PL - Switzerland TA - Molecules JT - Molecules (Basel, Switzerland) JID - 100964009 RN - 0 (Anti-Bacterial Agents) RN - 0 (Dendrimers) RN - 362O9ITL9D (Acetaminophen) SB - IM MH - Acetaminophen/*pharmacology MH - Anti-Bacterial Agents/*pharmacology MH - Bacteria/drug effects MH - Dendrimers/*chemical synthesis/chemistry MH - Electrochemistry MH - Inhibitory Concentration 50 MH - Microbial Sensitivity Tests MH - Oxidation-Reduction MH - Thermogravimetry PMC - PMC7583835 OTO - NOTNLM OT - MRSA OT - SEM OT - VRE OT - dendrimer OT - organoiron OT - paracetamol OT - redox-active OT - staphylococcus warneri COIS- The authors declare no conflict of interest. EDAT- 2020/10/08 06:00 MHDA- 2021/03/19 06:00 PMCR- 2020/10/02 CRDT- 2020/10/07 01:01 PHST- 2020/09/08 00:00 [received] PHST- 2020/09/28 00:00 [revised] PHST- 2020/09/28 00:00 [accepted] PHST- 2020/10/07 01:01 [entrez] PHST- 2020/10/08 06:00 [pubmed] PHST- 2021/03/19 06:00 [medline] PHST- 2020/10/02 00:00 [pmc-release] AID - molecules25194514 [pii] AID - molecules-25-04514 [pii] AID - 10.3390/molecules25194514 [doi] PST - epublish SO - Molecules. 2020 Oct 2;25(19):4514. doi: 10.3390/molecules25194514.