title: Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation.
abstract: Known morpholine class antifungals (fenpropimorph, fenpropidin, and amorolfine) were synthetically modified through silicon incorporation to have 15 sila-analogues. Twelve sila-analogues exhibited potent antifungal activity against different human fungal pathogens such as Candida albicans, Candida glabrata, Candida tropicalis, Cryptococcus neoformans, and Aspergillus niger. Sila-analogue 24 (fenpropimorph analogue) was the best in our hands, which showed superior fungicidal potential than fenpropidin, fenpropimorph, and amorolfine. The mode of action of sila-analogues was similar to morpholines, i.e., inhibition of sterol reductase and sterol isomerase enzymes of ergosterol synthesis pathway.
authors.affiliation: Division of Organic Chemistry and Biochemical Sciences Division, CSIR-National Chemical Laboratory , Dr. Homi Bhabha Road, Pune-411008, India.
authors.forename: Gorakhnath R
authors.initials: GR
authors.lastname: Jachak
authors.affiliation: Division of Organic Chemistry and Biochemical Sciences Division, CSIR-National Chemical Laboratory , Dr. Homi Bhabha Road, Pune-411008, India.
authors.forename: Remya
authors.initials: R
authors.lastname: Ramesh
authors.affiliation: Division of Organic Chemistry and Biochemical Sciences Division, CSIR-National Chemical Laboratory , Dr. Homi Bhabha Road, Pune-411008, India.
authors.forename: Duhita G
authors.initials: DG
authors.lastname: Sant
authors.affiliation: Division of Organic Chemistry and Biochemical Sciences Division, CSIR-National Chemical Laboratory , Dr. Homi Bhabha Road, Pune-411008, India.
authors.forename: Shweta U
authors.initials: SU
authors.lastname: Jorwekar
authors.affiliation: National Research Centre for Grapes , Manjri, Solapur Road, Pune-412307, India.
authors.forename: Manjusha R
authors.initials: MR
authors.lastname: Jadhav
authors.affiliation: Division of Organic Chemistry and Biochemical Sciences Division, CSIR-National Chemical Laboratory , Dr. Homi Bhabha Road, Pune-411008, India.
authors.forename: Santosh G
authors.initials: SG
authors.lastname: Tupe
authors.affiliation: Division of Organic Chemistry and Biochemical Sciences Division, CSIR-National Chemical Laboratory , Dr. Homi Bhabha Road, Pune-411008, India.
authors.forename: Mukund V
authors.initials: MV
authors.lastname: Deshpande
authors.affiliation: Division of Organic Chemistry and Biochemical Sciences Division, CSIR-National Chemical Laboratory , Dr. Homi Bhabha Road, Pune-411008, India.
authors.forename: D Srinivasa
authors.initials: DS
authors.lastname: Reddy
keywords: Antifungal drugs; Candida albicans; ergosterol biosynthesis; morpholines; sila-analogues