Medicinal Chemistry Research p. 3606 - 3620 (2013)
Update date:2022-08-02
Topics:
Shaukat, Awais
Mirza, Hira M.
Ansari, Amna H.
Yasinzai, Masoom
Zaidi, Sohail Z.
Dilshad, Sana
Ansari, Farzana L.
Leishmanolysin GP63 is a zinc metalloprotease, expressed at the surface of Leishmania promastigotes. Studies on this protein are hindered as only a limited number of effective non-toxic inhibitors of this drug target are known. Present study describes the identification of a variety of 2-aryl- and 5-nitro-2-arylbenzimidazoles as new GP63 inhibitors. All the compounds were tested for in vitro activity against the promastigote form of Leishmania major and showed very good activity. 2-(Thiophen-2-yl)-1H-benzimidazole (19) and 2-(1H-indol-3-yl)-5-nitro-1H-benzimidazole (34) with IC50 value of 0.62 μg/mL were identified as lead of this library. Molecular docking studies were performed on binding site of GP63 to study the binding mode of compounds. The results of both in vitro and in silico studies clearly indicated that benzimidazoles may serve as new drug candidates in the combat against leishmaniasis.
View MoreNantong LiKai Chemical Co.,Ltd
Contact:+86-513-89068669
Address:Jincheng Science Park
Zibo Ocean International Trade Co.,Ltd(expird)
Contact:+86 533 5160706
Address:1117, Hongtai Bld., Songling rd, Zichuan,Zibo,Shandong,China
Jurong Huaheng Natural Biological Products Factory
website:http://www.risebiochem.com
Contact:+86-13921007726
Address:Chuncheng town,Jurong city,Jiangsu province,China
KAIYUAN CHEMICAL COMPANY LIMITED.
website:http://www.kaiyuanchem.com
Contact:+86-22-59891255/66/77
Address:B-2205, Kuangshi International Building, Yingbin Road, XiangLuo Bay Business District, Binhai New area, Tianjin, China.
Nanjing Norris Pharm Technology Co., Ltd.
Contact:+86-13901585132
Address:2 Qiande Road, Jiangning sciencepark Hi-Tech Zone, Nanjing, P.R.China
Doi:10.1016/j.bmcl.2012.10.141
(2013)Doi:10.1002/anie.201104769
(2011)Doi:10.1016/S0040-4020(97)00933-2
(1997)Doi:10.1021/om300997s
(2013)Doi:10.1021/acs.joc.0c02251
(2021)Doi:10.1021/acs.oprd.8b00402
(2019)