Silicon incorporated morpholine antifungals: Design, synthesis, and biological evaluation
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 g...
| Asıl Yazarlar: | , , , , , , , |
|---|---|
| Materyal Türü: | Journal article |
| Dil: | English |
| Baskı/Yayın Bilgisi: |
American Chemical Society
2015
|
| _version_ | 1826308419480453120 |
|---|---|
| author | Jachak, GR Ramesh, R Sant, DG Jorwekar, SU Jadhav, MR Tupe, SG Deshpande, MV Reddy, DS |
| author_facet | Jachak, GR Ramesh, R Sant, DG Jorwekar, SU Jadhav, MR Tupe, SG Deshpande, MV Reddy, DS |
| author_sort | Jachak, GR |
| collection | OXFORD |
| description | 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. |
| first_indexed | 2024-03-07T07:19:12Z |
| format | Journal article |
| id | oxford-uuid:010409cb-a241-4727-9b51-4ccf25f3994a |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-07T07:19:12Z |
| publishDate | 2015 |
| publisher | American Chemical Society |
| record_format | dspace |
| spelling | oxford-uuid:010409cb-a241-4727-9b51-4ccf25f3994a2022-09-15T15:37:49ZSilicon incorporated morpholine antifungals: Design, synthesis, and biological evaluationJournal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:010409cb-a241-4727-9b51-4ccf25f3994aEnglishSymplectic ElementsAmerican Chemical Society2015Jachak, GRRamesh, RSant, DGJorwekar, SUJadhav, MRTupe, SGDeshpande, MVReddy, DSKnown 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. |
| spellingShingle | Jachak, GR Ramesh, R Sant, DG Jorwekar, SU Jadhav, MR Tupe, SG Deshpande, MV Reddy, DS Silicon incorporated morpholine antifungals: Design, synthesis, and biological evaluation |
| title | Silicon incorporated morpholine antifungals: Design, synthesis, and biological evaluation |
| title_full | Silicon incorporated morpholine antifungals: Design, synthesis, and biological evaluation |
| title_fullStr | Silicon incorporated morpholine antifungals: Design, synthesis, and biological evaluation |
| title_full_unstemmed | Silicon incorporated morpholine antifungals: Design, synthesis, and biological evaluation |
| title_short | Silicon incorporated morpholine antifungals: Design, synthesis, and biological evaluation |
| title_sort | silicon incorporated morpholine antifungals design synthesis and biological evaluation |
| work_keys_str_mv | AT jachakgr siliconincorporatedmorpholineantifungalsdesignsynthesisandbiologicalevaluation AT rameshr siliconincorporatedmorpholineantifungalsdesignsynthesisandbiologicalevaluation AT santdg siliconincorporatedmorpholineantifungalsdesignsynthesisandbiologicalevaluation AT jorwekarsu siliconincorporatedmorpholineantifungalsdesignsynthesisandbiologicalevaluation AT jadhavmr siliconincorporatedmorpholineantifungalsdesignsynthesisandbiologicalevaluation AT tupesg siliconincorporatedmorpholineantifungalsdesignsynthesisandbiologicalevaluation AT deshpandemv siliconincorporatedmorpholineantifungalsdesignsynthesisandbiologicalevaluation AT reddyds siliconincorporatedmorpholineantifungalsdesignsynthesisandbiologicalevaluation |