title: Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans.
abstract: We herein report the synthesis and in vitro antimicrobial evaluation of twenty five novel hybrid derivatives of imidazo [2,1-b]-1,3,4-thiadiazole containing chalcones (5a-o) and Schiff bases (6a-j) against three fungal strains (Candida albicans, Cryptococcus neoformans and Aspergillus niger). Most of the tested compounds displayed substantial anti-fungal activity with MICs ranging between 1.56 and 100 μg/mL. Compounds 5a, 5b and 5n exhibited promising activity against C. neoformans at a MIC 1.56 μg/mL. In addition, compound 5n also demonstrated significant antifungal activity against the clinical isolates of C. neoformans at MIC 3.125 μg/mL. However, moderate activity was observed for these compounds against four bacterial strains (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) and Mycobacterium tuberculosis (H37Rv).
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
authors.forename: Wesam S
authors.initials: WS
authors.lastname: Alwan
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa. Electronic address: karpoormath@ukzn.ac.za.
authors.forename: Rajshekhar
authors.initials: R
authors.lastname: Karpoormath
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
authors.forename: Mahesh B
authors.initials: MB
authors.lastname: Palkar
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
authors.forename: Harun M
authors.initials: HM
authors.lastname: Patel
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
authors.forename: Rajesh A
authors.initials: RA
authors.lastname: Rane
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
authors.forename: Mahamadhanif S
authors.initials: MS
authors.lastname: Shaikh
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
authors.forename: Afsana
authors.initials: A
authors.lastname: Kajee
authors.affiliation: Department of Microbiology, National Health Laboratory Services (NHLS), Inkosi Albert Luthuli Central Hospital, Durban, South Africa.
authors.forename: Koleka P
authors.initials: KP
authors.lastname: Mlisana
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002599:Chalcone / Q000737:chemistry; D003455:Cryptococcus neoformans / Q000187:drug effects* / Q000302:isolation & purification; D015195:Drug Design; D006801:Humans; D008826:Microbial Sensitivity Tests; D012545:Schiff Bases / Q000737:chemistry; D013830:Thiadiazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D012545:Schiff Bases; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole; D002599:Chalcone
keywords: Antifungal activity; Chalcones; Cryptococcosis; Cryptococcus neoformans; Imdazo [2,1-b]-1,3,4-thiadiazole; Schiff bases