Literature DB >> 28585419

Synthesis and biological evaluation of 2-acylbenzofuranes as novel α-glucosidase inhibitors with hypoglycemic activity.

Alexander A Spasov1, Denis A Babkov1, Tatyana Yu Prokhorova1, Ekaterina A Sturova1, Diana R Muleeva1, Maxim R Demidov2, Dmitry V Osipov2, Vitaly A Osyanin2, Yuri N Klimochkin2.   

Abstract

A series of benzofuran derivatives was synthesized as analogues of known natural α-glucosidase inhibitors. Their activity was evaluated in enzymatic assay and in rat model of diabetes mellitus. Newly identified inhibitors demonstrate significant potency with IC50 values ranging from 6.50 to 722.2 μm, as well as hypoglycemic activity exceeding the reference drug acarbose. Docking simulations provided insight into structure-activity relationships to direct further development of these novel hypoglycemic agents.
© 2017 John Wiley & Sons A/S.

Entities:  

Keywords:  benzofurans; diabetes; α-glucosidase

Mesh：

Substances：

Year:  2017        PMID： 28585419     DOI： 10.1111/cbdd.13038

Source DB:  PubMed          Journal:  Chem Biol Drug Des        ISSN： 1747-0277            Impact factor:   2.817


  6 in total

1.  Triterpenic Acids as Non-Competitive α-Glucosidase Inhibitors from Boswellia elongata with Structure-Activity Relationship: In Vitro and In Silico Studies.

Authors:  Najeeb Ur Rehman; Sobia Ahsan Halim; Mohammed Al-Azri; Majid Khan; Ajmal Khan; Kashif Rafiq; Ahmed Al-Rawahi; Rene Csuk; Ahmed Al-Harrasi
Journal:  Biomolecules       Date:  2020-05-12

2.  Triazoloquinazolines as a new class of potent α-glucosidase inhibitors: in vitro evaluation and docking study.

Authors:  Hatem A Abuelizz; El Hassane Anouar; Rohaya Ahmad; Nor Izzati Iwana Nor Azman; Mohamed Marzouk; Rashad Al-Salahi
Journal:  PLoS One       Date:  2019-08-14       Impact factor: 3.240

3.  Design, synthesis, biological evaluation, and molecular modeling studies of pyrazole-benzofuran hybrids as new α-glucosidase inhibitor.

Authors:  Fateme Azimi; Homa Azizian; Mohammad Najafi; Ghadamali Khodarahmi; Lotfollah Saghaei; Motahareh Hassanzadeh; Jahan B Ghasemi; Mohammad Ali Faramarzi; Bagher Larijani; Farshid Hassanzadeh; Mohammad Mahdavi
Journal:  Sci Rep       Date:  2021-10-21       Impact factor: 4.379

Review 4.  Dihydronaphthofurans: synthetic strategies and applications.

Authors:  Abolfazl Olyaei; Mahdieh Sadeghpour
Journal:  RSC Adv       Date:  2020-02-05       Impact factor: 4.036

5.  Synthesis, In Vitro Evaluation and Molecular Docking of the 5-Acetyl-2-aryl-6-hydroxybenzo[b]furans against Multiple Targets Linked to Type 2 Diabetes.

Authors:  Malose J Mphahlele; Yee Siew Choong; Marole M Maluleka; Samantha Gildenhuys
Journal:  Biomolecules       Date:  2020-03-07

6.  GC-MS Analysis and Biomedical Therapy of Oil from n-Hexane Fraction of Scutellaria edelbergii Rech. f.: In Vitro, In Vivo, and In Silico Approach.

Authors:  Muddaser Shah; Waheed Murad; Najeeb Ur Rehman; Sidra Mubin; Jamal Nasser Al-Sabahi; Manzoor Ahmad; Muhammad Zahoor; Obaid Ullah; Muhammad Waqas; Saeed Ullah; Zul Kamal; Rafa Almeer; Simona G Bungau; Ahmed Al-Harrasi
Journal:  Molecules       Date:  2021-12-18       Impact factor: 4.411
  6 in total

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