Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors
Thirty N-arylidenequinoline-3-carbohydrazides (1–30) have been synthesized and evaluated against β-glucuronidase inhibitory potential. Twenty four analogs showed outstanding β-glucuronidase activity having IC50values ranging between 2.11 ± 0.05 and 46.14 ± 0.95 than standard D-saccharic acid 1,4 lac...
| Published in: | Bioorganic and Medicinal Chemistry |
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| Format: | Article |
| Language: | English |
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Elsevier Ltd
2016
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84978286017&doi=10.1016%2fj.bmc.2016.06.008&partnerID=40&md5=03ca04d172bfd0b30ab2122b709d35e2 |
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2-s2.0-84978286017 Taha M.; Sultan S.; Nuzar H.A.; Rahim F.; Imran S.; Ismail N.H.; Naz H.; Ullah H. Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors 2016 Bioorganic and Medicinal Chemistry 24 16 10.1016/j.bmc.2016.06.008 https://www.scopus.com/inward/record.uri?eid=2-s2.0-84978286017&doi=10.1016%2fj.bmc.2016.06.008&partnerID=40&md5=03ca04d172bfd0b30ab2122b709d35e2 Thirty N-arylidenequinoline-3-carbohydrazides (1–30) have been synthesized and evaluated against β-glucuronidase inhibitory potential. Twenty four analogs showed outstanding β-glucuronidase activity having IC50values ranging between 2.11 ± 0.05 and 46.14 ± 0.95 than standard D-saccharic acid 1,4 lactone (IC50 = 48.4 ± 1.25 μM). Six analogs showed good β-glucuronidase activity having IC50values ranging between 49.38 ± 0.90 and 80.10 ± 1.80. Structure activity relationship and the interaction of the active compounds and enzyme active site with the help of docking studies were established. Our study identifies novel series of potent β-glucuronidase inhibitors for further investigation. © 2016 Elsevier Ltd Elsevier Ltd 9680896 English Article |
| author |
Taha M.; Sultan S.; Nuzar H.A.; Rahim F.; Imran S.; Ismail N.H.; Naz H.; Ullah H. |
| spellingShingle |
Taha M.; Sultan S.; Nuzar H.A.; Rahim F.; Imran S.; Ismail N.H.; Naz H.; Ullah H. Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors |
| author_facet |
Taha M.; Sultan S.; Nuzar H.A.; Rahim F.; Imran S.; Ismail N.H.; Naz H.; Ullah H. |
| author_sort |
Taha M.; Sultan S.; Nuzar H.A.; Rahim F.; Imran S.; Ismail N.H.; Naz H.; Ullah H. |
| title |
Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors |
| title_short |
Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors |
| title_full |
Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors |
| title_fullStr |
Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors |
| title_full_unstemmed |
Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors |
| title_sort |
Synthesis and biological evaluation of novel N-arylidenequinoline-3-carbohydrazides as potent β-glucuronidase inhibitors |
| publishDate |
2016 |
| container_title |
Bioorganic and Medicinal Chemistry |
| container_volume |
24 |
| container_issue |
16 |
| doi_str_mv |
10.1016/j.bmc.2016.06.008 |
| url |
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84978286017&doi=10.1016%2fj.bmc.2016.06.008&partnerID=40&md5=03ca04d172bfd0b30ab2122b709d35e2 |
| description |
Thirty N-arylidenequinoline-3-carbohydrazides (1–30) have been synthesized and evaluated against β-glucuronidase inhibitory potential. Twenty four analogs showed outstanding β-glucuronidase activity having IC50values ranging between 2.11 ± 0.05 and 46.14 ± 0.95 than standard D-saccharic acid 1,4 lactone (IC50 = 48.4 ± 1.25 μM). Six analogs showed good β-glucuronidase activity having IC50values ranging between 49.38 ± 0.90 and 80.10 ± 1.80. Structure activity relationship and the interaction of the active compounds and enzyme active site with the help of docking studies were established. Our study identifies novel series of potent β-glucuronidase inhibitors for further investigation. © 2016 Elsevier Ltd |
| publisher |
Elsevier Ltd |
| issn |
9680896 |
| language |
English |
| format |
Article |
| accesstype |
|
| record_format |
scopus |
| collection |
Scopus |
| _version_ |
1809678487064150016 |