title: Novel synthetic organic compounds inspired from antifeedant marine alkaloids as potent bacterial biofilm inhibitors.
abstract: In this paper, we have reported seventeen novel synthetic organic compounds derived from marine bromopyrrole alkaloids, exhibiting potential inhibition of biofilm produced by Gram-positive bacteria. Compound 5f with minimumbiofilm inhibitory concentration(MBIC) of 0.39, 0.78 and 3.125 μg/mL against MSSA, MRSA and SE respectively, emerged as promising anti-biofilm lead compounds. In addition, compounds 5b, 5c, 5d, 5e, 5f, 5h, 5i and 5j revealed equal potency as that of the standard drug Vancomycin (MBIC = 3.125 μg/mL) against Streptococcus epidermidis. Notably, most of the synthesized compounds displayed better potency than Vancomycin indicating their potential as inhibitors of bacterial biofilm. The cell viability assay for the most active hybrid confirms its anti-virulence properties which need to be further researched.
authors.affiliation: Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa.
authors.forename: Rajesh A
authors.initials: RA
authors.lastname: Rane
authors.affiliation: Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa. Electronic address: karpoormath@ukzn.ac.za.
authors.forename: Rajshekhar
authors.initials: R
authors.lastname: Karpoormath
authors.affiliation: Government College of Amravati, Maharashtra 444601, India.
authors.forename: Shital S
authors.initials: SS
authors.lastname: Naphade
authors.affiliation: SPP School of Pharmacy and Technology Management, Vile Parle, Mumbai 400056, India.
authors.forename: Pavankumar
authors.initials: P
authors.lastname: Bangalore
authors.affiliation: Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa.
authors.forename: Mahamadhanif
authors.initials: M
authors.lastname: Shaikh
authors.affiliation: Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa.
authors.forename: Girish
authors.initials: G
authors.lastname: Hampannavar
mesh_terms: D000470:Alkaloids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D059001:Aquatic Organisms / Q000737:chemistry / Q000378:metabolism; D018441:Biofilms / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000502:physiology*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D053038:Quorum Sensing / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects / Q000502:physiology; D013291:Streptococcus / Q000187:drug effects; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000470:Alkaloids; D000900:Anti-Bacterial Agents
keywords: 1,3,4-Oxadiazoles; Biofilm inhibitors; Bromopyrrole; Marine alkaloids