Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents.
A series of novel 2,5-bis(guanidino-aryl)-1-methyl-1H-pyrroles 9a-h has been synthesized starting from 1-methyl-1H-pyrrole. The antifungal activities of compounds were evaluated by in vitro agar diffusion and broth dilution assay against Candida spp. and Aspergillus spp. Compound 9c from this series was found to be equipotent or more potent than fluconazole, whereas compound 9d was comparable to fluconazole against most of the tested strains.
Medicinal Chemistry Division, New Chemical Entity Research, Lupin Research Park, 46/47A Village Nande, Taluka Mulshi, Pune 411 042, Maharashtra, India.
Gour Hari
GH
Jana
Sanjay
S
Jain
Sudershan K
SK
Arora
Neelima
N
Sinha
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001230:Aspergillus / Q000187:drug effects* / Q000254:growth & development; D002175:Candida / Q000187:drug effects* / Q000254:growth & development; D004352:Drug Resistance, Microbial; D015725:Fluconazole / Q000494:pharmacology; D019791:Guanidine / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D011758:Pyrroles; D015725:Fluconazole; D019791:Guanidine