Solid supported microwave induced synthesis of imidazole–pyrimidine hybrids: Antimicrobial evaluation and docking study as 14DM-CPY51 inhibitors
As part of our exploration for new antifungal agents, substituted 4,5-diphenyl imidazolyl pyrimidine hybrids were synthesized. A series of substituted ethyl 1,2,3,6-tetrahydro-4-methyl-2-oxo/thioxo-6-phenyl-1-(4,5-diphenyl-1-H-imidazol-2-yl) pyrimidine-5-carboxylates have been studied for their bind...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2016-09-01
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| Series: | Arabian Journal of Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1878535211000670 |
| _version_ | 1819171368192704512 |
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| author | Naziyanaz B. Pathan Anjali M. Rahatgaonkar |
| author_facet | Naziyanaz B. Pathan Anjali M. Rahatgaonkar |
| author_sort | Naziyanaz B. Pathan |
| collection | DOAJ |
| description | As part of our exploration for new antifungal agents, substituted 4,5-diphenyl imidazolyl pyrimidine hybrids were synthesized. A series of substituted ethyl 1,2,3,6-tetrahydro-4-methyl-2-oxo/thioxo-6-phenyl-1-(4,5-diphenyl-1-H-imidazol-2-yl) pyrimidine-5-carboxylates have been studied for their binding active sites of cytochrome P450 14α-sterol demethylase CPY51 enzyme. For comparison, the binding behavior of known 14DM selective (Fluconazole) and non-selective (Clotrimazole, Miconazole, Griesofulvin) drugs has also been studied. Synthesized compounds were screened for their in vitro antibacterial activity against Staphylococcus aureus, Salmonella typhi, Pseudomonas aurogenosa and Klebsiella pneumonae and also antifungal activity against the opportunistic pathogens Candida albicans. |
| first_indexed | 2024-12-22T19:50:10Z |
| format | Article |
| id | doaj.art-27d65d99bbf4487cb9df43a58994d25d |
| institution | Directory Open Access Journal |
| issn | 1878-5352 |
| language | English |
| last_indexed | 2024-12-22T19:50:10Z |
| publishDate | 2016-09-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Arabian Journal of Chemistry |
| spelling | doaj.art-27d65d99bbf4487cb9df43a58994d25d2022-12-21T18:14:35ZengElsevierArabian Journal of Chemistry1878-53522016-09-019S1S100S10810.1016/j.arabjc.2011.02.013Solid supported microwave induced synthesis of imidazole–pyrimidine hybrids: Antimicrobial evaluation and docking study as 14DM-CPY51 inhibitorsNaziyanaz B. PathanAnjali M. RahatgaonkarAs part of our exploration for new antifungal agents, substituted 4,5-diphenyl imidazolyl pyrimidine hybrids were synthesized. A series of substituted ethyl 1,2,3,6-tetrahydro-4-methyl-2-oxo/thioxo-6-phenyl-1-(4,5-diphenyl-1-H-imidazol-2-yl) pyrimidine-5-carboxylates have been studied for their binding active sites of cytochrome P450 14α-sterol demethylase CPY51 enzyme. For comparison, the binding behavior of known 14DM selective (Fluconazole) and non-selective (Clotrimazole, Miconazole, Griesofulvin) drugs has also been studied. Synthesized compounds were screened for their in vitro antibacterial activity against Staphylococcus aureus, Salmonella typhi, Pseudomonas aurogenosa and Klebsiella pneumonae and also antifungal activity against the opportunistic pathogens Candida albicans.http://www.sciencedirect.com/science/article/pii/S1878535211000670Cytochrome P450 (14DM) CPY51DiphenylimidazolylpyrimidineSingle crystal XRDAntifungal activity |
| spellingShingle | Naziyanaz B. Pathan Anjali M. Rahatgaonkar Solid supported microwave induced synthesis of imidazole–pyrimidine hybrids: Antimicrobial evaluation and docking study as 14DM-CPY51 inhibitors Arabian Journal of Chemistry Cytochrome P450 (14DM) CPY51 Diphenylimidazolylpyrimidine Single crystal XRD Antifungal activity |
| title | Solid supported microwave induced synthesis of imidazole–pyrimidine hybrids: Antimicrobial evaluation and docking study as 14DM-CPY51 inhibitors |
| title_full | Solid supported microwave induced synthesis of imidazole–pyrimidine hybrids: Antimicrobial evaluation and docking study as 14DM-CPY51 inhibitors |
| title_fullStr | Solid supported microwave induced synthesis of imidazole–pyrimidine hybrids: Antimicrobial evaluation and docking study as 14DM-CPY51 inhibitors |
| title_full_unstemmed | Solid supported microwave induced synthesis of imidazole–pyrimidine hybrids: Antimicrobial evaluation and docking study as 14DM-CPY51 inhibitors |
| title_short | Solid supported microwave induced synthesis of imidazole–pyrimidine hybrids: Antimicrobial evaluation and docking study as 14DM-CPY51 inhibitors |
| title_sort | solid supported microwave induced synthesis of imidazole pyrimidine hybrids antimicrobial evaluation and docking study as 14dm cpy51 inhibitors |
| topic | Cytochrome P450 (14DM) CPY51 Diphenylimidazolylpyrimidine Single crystal XRD Antifungal activity |
| url | http://www.sciencedirect.com/science/article/pii/S1878535211000670 |
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