Abstract：
:In search of better α-glucosidase inhibitors, a series of bis-indolylmethane sulfonohydrazides derivatives (1-14) were synthesized and evaluated for their α-glucosidase inhibitory potential. All derivatives exhibited outstanding α-glucosidase inhibition with IC50 values ranging between 0.10 ± 0.05 to 5.1 ± 0.05 μM when compared with standard drug acarbose having IC50 value 856.28 ± 3.15 μM. Among the series, analog 7 (0.10 ± 0.05 μM) with tri-chloro substitution on phenyl ring was identified as the most potent inhibitor of α-glucosidase (∼ 8500 times). The structure activity relationship has been also established. Molecular docking studies were also performed to help understand the binding interaction of the most active analogs with receptors. From the docking studies, it was observed that all the active bis-indolylmethane sulfonohydrazides derivatives showed considerable binding interactions within the active site (acarbose inhibition site) of α-glucosidase. We also evaluated toxicity of all derivatives and found none of them are toxic.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Gollapalli M,Taha M,Ullah H,Nawaz M,AlMuqarrabun LMR,Rahim F,Qureshi F,Mosaddik A,Ahmat N,Khan KMdoi
10.1016/j.bioorg.2018.06.001subject
Has Abstractpub_date
2018-10-01 00:00:00pages
112-120eissn
0045-2068issn
1090-2120pii
S0045-2068(18)30060-9journal_volume
80pub_type
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