Bioorganic Chemistry p. 163 - 177 (2019)
Update date:2022-08-05
Topics: Kinetic studies Synthesis of Benzohydrazide Derivatives In Vitro Urease Inhibitory Activity In Silico Studies
Abbas, Azhar
Ali, Basharat
Kanwal
Khan, Khalid Mohammed
Iqbal, Jamshed
ur Rahman, Shafiq
Zaib, Sumera
Perveen, Shahnaz
Benzohydrazide derivatives 1–43 were synthesized via “one-pot” reaction and structural characterization of these synthetic derivatives was carried out by different spectroscopic techniques such as 1H NMR and EI-MS. The synthetic molecules were evaluated for their in vitro urease inhibitory activity. All synthetic derivatives showed good inhibitory activities in the range of (IC50 = 0.87 ± 0.31–19.0 ± 0.25 μM) as compared to the standard thiourea (IC50 = 21.25 ± 0.15 μM), except seven compounds 17, 18, 23, 24, 29, 30, and 41 which were found to be inactive. The most active compound of the series was compound 36 (IC50 = 0.87 ± 0.31 μM) having two chloro groups at meta positions of ring A and methoxy group at para position of ring B. The structure–activity relationship (SAR) of the active compounds was established on the basis of different substituents and their positions in the molecules. Kinetic studies of the active compounds revealed that compounds can inhibit enzyme via competitive and noncompetitive modes. In silico study was also performed to understand the binding interactions of the molecules (ligand) with the active site of enzyme.
View MoreContact:86-25-84683399
Address:605, Phoenix Herui Plaza, No.389, South Taiping Road, Nanjing, China 210002
SHANGHAI RC CHEMICALS CO.,LTD.
website:http://www.rcc.net.cn
Contact:+86-21-50322175
Address:Rm1415 Yinqiao Masion No.58 Jinxin Road Pudong Shanghai China
Tianjin Te-An Chemtech Co., Ltd.
Contact:+86-22-65378638
Address:A5-8, No.80 Haiyun Street, TEDA
Taixing Shenfeng Chemical Co., Ltd.
Contact:+86-523-87117033, 87117666
Address:4# Yinsanlu, Huangqiao town, Taixing, Jiangsu, China.
Feis International Trade Co,. Ltd
Contact:13961823444-18235944442
Address:Wuxi jiangsu
Doi:10.1038/205262a0
(1965)Doi:10.1039/b005068g
(2000)Doi:10.1021/ic000529x
(2000)Doi:10.1016/S0040-4039(00)01453-2
(2000)Doi:10.1002/jps.2600591230
(1970)Doi:10.1021/jo005593a
(2000)