title: Design, synthesis and antistaphylococcal activity of marine pyrrole alkaloid derivatives.
abstract: A novel set of 16 hybrids of bromopyrrole alkaloids with aroyl hydrazone were designed, synthesized and evaluated for antibacterial and antibiofilm activities against methicillin-resistant Staphylococcus aureus (MRSA; ATCC 43866), methicillin-susceptible Staphylococcus aureus (MSSA; ATCC 35556) and Staphylococcus epidermidis (SE, S. epidermidis ATCC 35984). Of the 16 tested hybrids, 14 exhibited equal or superior antibiofilm activity against MSSA and MRSA relative to standard vancomycin. Compound 4m showed highest potency with antibiofilm activity of 0.39 µg/mL and 0.78 µg/mL against MSSA and MRSA, respectively. Thus, this compound could act as a potential lead for further development of new antistaphylococcal drugs.
authors.affiliation: S. P. P. School of Pharmacy and Technology Management, NMIMS university , Mumbai , India.
authors.forename: Rajesh A
authors.initials: RA
authors.lastname: Rane
authors.forename: Niteshkumar U
authors.initials: NU
authors.lastname: Sahu
authors.forename: Chetan P
authors.initials: CP
authors.lastname: Shah
authors.forename: Nishant K
authors.initials: NK
authors.lastname: Shah
mesh_terms: D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018441:Biofilms / Q000187:drug effects* / Q000254:growth & development; D015195:Drug Design; D024881:Drug Resistance, Bacterial; D006835:Hydrazones / Q000737:chemistry; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects* / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D050296:Microbial Viability / Q000187:drug effects; D011161:Porifera / Q000737:chemistry; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013212:Staphylococcus epidermidis / Q000187:drug effects* / Q000254:growth & development; D053778:Thiazolidines / Q000737:chemistry; D014640:Vancomycin / Q000494:pharmacology
chemical_list: D000470:Alkaloids; D000900:Anti-Bacterial Agents; D006835:Hydrazones; D011758:Pyrroles; D053778:Thiazolidines; D014640:Vancomycin
keywords: Antistaphylococcal activity; bromopyrrole alkaloids; hydrazide derivatives