Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studies
A wide range of 4-chloro-3,4-dihydroquinazolines hybrid isoniazid derivatives were synthesised efficiently via reaction of 4-chloro-3,4-dihydroquinazolines with isoniazid in the presence of catalytic amount of N,N-diisopropylethylamine (DIPEA) under refluxing methanol. All the title molecules were c...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2020-01-01
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| Series: | Arabian Journal of Chemistry |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S187853521830056X |
| _version_ | 1828378168329764864 |
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| author | Kinjal D. Patel Rajesh H. Vekariya Neelam P. Prajapati Dhaval B. Patel Hitesh D. Patel Tauhid Shaikh Dhanji P. Rajani Smita Rajani Naumita S. Shah Devendrasinh Jhala |
| author_facet | Kinjal D. Patel Rajesh H. Vekariya Neelam P. Prajapati Dhaval B. Patel Hitesh D. Patel Tauhid Shaikh Dhanji P. Rajani Smita Rajani Naumita S. Shah Devendrasinh Jhala |
| author_sort | Kinjal D. Patel |
| collection | DOAJ |
| description | A wide range of 4-chloro-3,4-dihydroquinazolines hybrid isoniazid derivatives were synthesised efficiently via reaction of 4-chloro-3,4-dihydroquinazolines with isoniazid in the presence of catalytic amount of N,N-diisopropylethylamine (DIPEA) under refluxing methanol. All the title molecules were characterized by 13C NMR, 1H NMR, Mass and IR spectroscopy. All the compounds were tested for anti-malarial, anti-microbial and anti-tuberculosis activities. They were further tested for the cytotoxic feature. In-silico molecular docking study and ADME properties were also studied for the title molecules. Keywords: Molecular hybridization, Anti-malarial, Anti-microbial, Anti-tuberculosis, MTT assay, Docking, ADME |
| first_indexed | 2024-04-14T08:22:47Z |
| format | Article |
| id | doaj.art-159e7501c1fd4b49a6cd932ba631b830 |
| institution | Directory Open Access Journal |
| issn | 1878-5352 |
| language | English |
| last_indexed | 2024-04-14T08:22:47Z |
| publishDate | 2020-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Arabian Journal of Chemistry |
| spelling | doaj.art-159e7501c1fd4b49a6cd932ba631b8302022-12-22T02:04:10ZengElsevierArabian Journal of Chemistry1878-53522020-01-0113119862000Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studiesKinjal D. Patel0Rajesh H. Vekariya1Neelam P. Prajapati2Dhaval B. Patel3Hitesh D. Patel4Tauhid Shaikh5Dhanji P. Rajani6Smita Rajani7Naumita S. Shah8Devendrasinh Jhala9Department of Chemistry, School of Sciences, Gujarat University, Navarangpura, Ahmedabad, Gujarat, IndiaDepartment of Chemistry, School of Sciences, Gujarat University, Navarangpura, Ahmedabad, Gujarat, IndiaDepartment of Chemistry, School of Sciences, Gujarat University, Navarangpura, Ahmedabad, Gujarat, IndiaDepartment of Chemistry, School of Sciences, Gujarat University, Navarangpura, Ahmedabad, Gujarat, IndiaDepartment of Chemistry, School of Sciences, Gujarat University, Navarangpura, Ahmedabad, Gujarat, India; Corresponding author.Department of Chemistry, School of Sciences, Gujarat University, Navarangpura, Ahmedabad, Gujarat, IndiaMicrocare Laboratory and TRC, Surat, IndiaMicrocare Laboratory and TRC, Surat, IndiaDepartment of Zoology, School of Sciences, Gujarat University, Navarangpura, Ahmedabad, Gujarat, IndiaDepartment of Zoology, School of Sciences, Gujarat University, Navarangpura, Ahmedabad, Gujarat, IndiaA wide range of 4-chloro-3,4-dihydroquinazolines hybrid isoniazid derivatives were synthesised efficiently via reaction of 4-chloro-3,4-dihydroquinazolines with isoniazid in the presence of catalytic amount of N,N-diisopropylethylamine (DIPEA) under refluxing methanol. All the title molecules were characterized by 13C NMR, 1H NMR, Mass and IR spectroscopy. All the compounds were tested for anti-malarial, anti-microbial and anti-tuberculosis activities. They were further tested for the cytotoxic feature. In-silico molecular docking study and ADME properties were also studied for the title molecules. Keywords: Molecular hybridization, Anti-malarial, Anti-microbial, Anti-tuberculosis, MTT assay, Docking, ADMEhttp://www.sciencedirect.com/science/article/pii/S187853521830056X |
| spellingShingle | Kinjal D. Patel Rajesh H. Vekariya Neelam P. Prajapati Dhaval B. Patel Hitesh D. Patel Tauhid Shaikh Dhanji P. Rajani Smita Rajani Naumita S. Shah Devendrasinh Jhala Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studies Arabian Journal of Chemistry |
| title | Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studies |
| title_full | Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studies |
| title_fullStr | Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studies |
| title_full_unstemmed | Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studies |
| title_short | Synthesis of N'-(Quinazolin-4-yl)isonicotinohydrazides and their biological screening, docking and ADME studies |
| title_sort | synthesis of n quinazolin 4 yl isonicotinohydrazides and their biological screening docking and adme studies |
| url | http://www.sciencedirect.com/science/article/pii/S187853521830056X |
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