title: Syntheses and Antibiotic Evaluation of 2-{[(2R,4R)-4-Carboxy-2-hydroxypyrrolidin-1-yl]carbonyl}benzene-1,5-dicarboxylic Acids and 2-Carbamoylbenzene-1,5-dicarboxylic Acid Analogues.
abstract: Our search for new antibiotics led to the syntheses and biological evaluation of new classes of dicarboxylic acid analogues. The syntheses involve nucleophilic addition of different substituted benzylamine, aniline, alkylamine, and 4-hydroxyl-L-proline with carbamoylbenzoic acid. The results of the antimicrobial activity as indicated by the zone of inhibition (ZOI) showed that Z 10 is the most active against Pseudomonas aeruginosa (32 mm) and least active against Candida stellatoidea (27 mm) and Vancomycin Resistant Enterococci (VRE) (27 mm), while Z 7 shows the least zone of inhibition (22 mm) against Methicillin Resistant Staphylococcus aureus (MRSA). The minimum inhibition concentration (MIC) determination reveals that Z 10 inhibits the growth of tested microbes at a low concentration of 6.25 μg/mL, while Z 9 and Z 12 inhibits the growth of most microbes at a concentration of 12.5 μg/mL, recording the least MIC. The Minimum Bactericidal/Fungicidal Concentration (MBC/MFC) results revealed that Z 10 has the highest bactericidal/fungicidal effect on the test microbes, at a concentration of 12.5 μg/mL, with the exception of Candida stellatoidea and Vancomycin Resistant Enterococci (VRE) with MBC/MFC of 25 μg/mL. The result of this investigation reveals the potential of the target compounds (Z 1-3,5,7-12 ) in the search for new antimicrobial agents.
authors.affiliation: Department of Chemistry, Ahmadu Bello University, Zaria 810001, Nigeria.
authors.forename: Abdulrazaq
authors.identifier: 0000-0002-1140-8453
authors.initials: A
authors.lastname: Tukur
authors.affiliation: Department of Chemistry, Ahmadu Bello University, Zaria 810001, Nigeria.
authors.forename: Isaac Asusheyi
authors.identifier: 0000-0001-8135-4692
authors.initials: IA
authors.lastname: Bello
authors.affiliation: School of Chemistry and Physics, University of KwaZulu-Natal, Private Bag X 54001, Durban 4000, South Africa.
authors.forename: Neil Anthony
authors.identifier: 0000-0002-6214-4021
authors.initials: NA
authors.lastname: Koorbanally
authors.affiliation: Department of Chemistry, Ahmadu Bello University, Zaria 810001, Nigeria.
authors.forename: James Dama
authors.identifier: 0000-0003-3518-5271
authors.initials: JD
authors.lastname: Habila