Synthesis and antimicrobial activity of novel 5-aminoimidazole-4-carboxamidrazones

• Type: Article in International Scientific Journal
• Date: 2014

Authors

Ana I Ribeiro (Author) Other; Carla Gabriel (Author) Other; Fatima Cerqueira (Author) Other; Marta Maia (Author) Other; Eugenia Pinto (Author) FFUP; Joao Carlos Sousa (Author) Other; Rui Medeiros (Author) Other; Fernanda Proenca, MF (Author) Other; Alice M Dias (Author) Other

Journal

Title: Bioorganic and Medicinal Chemistry Letters

Vol. 24

Pages: 4699-4702

ISSN: 0960-894X

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 21 Citations

Scopus - 22 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: P-009-TAT

DOI: 10.1016/j.bmcl.2014.08.025

Abstract (EN): A mild and simple method was developed to prepare a series of fifteen 5-aminoimidazole 4-carboxamidrazones, starting from the easily accessible 5-amino-4-cyanoformimidoyl imidazoles. The antimicrobial activity of these novel amidrazones was screened against Gram positive (Staphylococcus aureus) and Gram negative (Escherichia coli, Pseudomonas aeruginosa) bacteria and Candida sp. (Candida albicans, Candida krusei, Candida parapsilosis). Only a subset of compounds displayed fair-moderate activity against S. aureus and E. coli but all exhibited activity against Candida sp. The three most potent antifungal compounds were further tested against Cryptococcus neoformans, Aspergillus fumigatus and three dermatophytes (Trichophyton rubrum, Trichophyton mentagrophytes, Microsporum gypseum). These three hit compounds strongly inhibited C. krusei and C. neoformans growth, although their activity on filamentous fungi was very weak when compared to the activity on yeasts.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 4