Twenty eight xanthone derivatives were designed and docked into the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM) by considering miglitol as standard drug. Most of the molecules showed excellent docking scores and docking interaction as compared to the binding cavity of the standard molecule. The five best scoring ligands were synthesized and characterized by a number of analytical and spectroscopic techniques. The molecules were screened for the in vivo anti-diabetic activity in streptozotocin-induced diabetic animal model in Wistar rats. Compound P4 showed the most prominent inhibition among others. The synthesized compounds reported significant (p<0.01) effect in lowering blood glucose levels compared to miglitol as a standard alpha-glucosidase inhibitor.
机构:
Wuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Wuyi Univ, Guangdong Prov Key Lab Large Anim Models Biomed, Jiangmen 529020, Peoples R ChinaWuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Feng, Mei
Liang, Bingwen
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Wuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Wuyi Univ, Guangdong Prov Key Lab Large Anim Models Biomed, Jiangmen 529020, Peoples R ChinaWuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Liang, Bingwen
Sun, Jinping
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Wuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Wuyi Univ, Guangdong Prov Key Lab Large Anim Models Biomed, Jiangmen 529020, Peoples R ChinaWuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Sun, Jinping
Min, Xiaofeng
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Wuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Wuyi Univ, Guangdong Prov Key Lab Large Anim Models Biomed, Jiangmen 529020, Peoples R ChinaWuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Min, Xiaofeng
Wang, Shao-Hua
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Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China
Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China
Lanzhou Univ, Collaborat Innovat Ctr Northwestern Chinese Med, Lanzhou 730000, Peoples R ChinaWuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Wang, Shao-Hua
Lu, Yujing
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Guangdoong Univ Technol, Sch Biomed & Pharmaceut Sci, Guangzhou 510006, Peoples R ChinaWuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Lu, Yujing
Xu, Xuetao
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Wuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
Wuyi Univ, Guangdong Prov Key Lab Large Anim Models Biomed, Jiangmen 529020, Peoples R ChinaWuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
机构:
Al Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Cairo 11884, EgyptAl Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Cairo 11884, Egypt
Ibrahim, Albaraa
Sakr, Helmy M.
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Al Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Cairo 11884, EgyptAl Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Cairo 11884, Egypt
Sakr, Helmy M.
Ayyad, Rezk R.
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Al Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Cairo 11884, EgyptAl Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Cairo 11884, Egypt
Ayyad, Rezk R.
Khalifa, Mohamed M.
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Al Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Cairo 11884, EgyptAl Azhar Univ, Fac Pharm Boys, Pharmaceut Med Chem & Drug Design Dept, Cairo 11884, Egypt
机构:
Univ Tehran Med Sci, Fac Pharm, Dept Pharmaceut Biotechnol, Tehran, Iran
Univ Tehran Med Sci, Biotechnol Res Ctr, Tehran, IranUniv Tehran, Coll Sci, Sch Chem, Tehran, Iran
Imanparast, Somaye
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Faramarzi, Mohammad Ali
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Ranjbar, Parviz Rashidi
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Mahdavi, Mohammad
Larijani, Bagher
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Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Clin Sci Inst, Tehran, IranUniv Tehran, Coll Sci, Sch Chem, Tehran, Iran
机构:
Glenmark Res Ctr, Div Med Chem, Mahape 400709, Navi Mumbai, IndiaAndhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, India
Lakshminarayana, N.
Prasad, Y. Rajendra
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Andhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, IndiaAndhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, India
Prasad, Y. Rajendra
Gharat, Laxmikant
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Glenmark Res Ctr, Div Med Chem, Mahape 400709, Navi Mumbai, IndiaAndhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, India
Gharat, Laxmikant
Thomas, Abraham
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Glenmark Res Ctr, Div Med Chem, Mahape 400709, Navi Mumbai, IndiaAndhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, India
Thomas, Abraham
Ravikumar, P.
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机构:
Andhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, IndiaAndhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, India
Ravikumar, P.
Narayanan, Shridhar
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Glenmark Res Ctr, Div Med Chem, Mahape 400709, Navi Mumbai, IndiaAndhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, India
Narayanan, Shridhar
Srinivasan, C. V.
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Glenmark Res Ctr, Div Med Chem, Mahape 400709, Navi Mumbai, IndiaAndhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, India
Srinivasan, C. V.
Gopalan, Balasubramanian
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Glenmark Res Ctr, Div Med Chem, Mahape 400709, Navi Mumbai, IndiaAndhra Univ, AU Coll Pharmaceut Sci, Pharmaceut Chem Div, Visakhapatnam 530003, Andhra Pradesh, India
机构:
Jagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, PolandJagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, Poland
Waszkielewicz, Anna M.
Sloczynska, Karolina
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Jagiellonian Univ Med Coll, Fac Pharm, Dept Pharmaceut Biochem, Krakow, PolandJagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, Poland
Sloczynska, Karolina
Pekala, Elzbieta
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Jagiellonian Univ Med Coll, Fac Pharm, Dept Pharmaceut Biochem, Krakow, PolandJagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, Poland
Pekala, Elzbieta
Zmudzki, Pawel
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Jagiellonian Univ Med Coll, Fac Pharm, Dept Pharmaceut Chem, Krakow, PolandJagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, Poland
Zmudzki, Pawel
Siwek, Agata
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Jagiellonian Univ Med Coll, Fac Pharm, Dept Pharmacobiol, Krakow, PolandJagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, Poland
Siwek, Agata
Grybos, Anna
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Jagiellonian Univ Med Coll, Fac Pharm, Dept Pharmacobiol, Krakow, PolandJagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, Poland
Grybos, Anna
Marona, Henryk
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Jagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, PolandJagiellonian Univ Med Coll, Fac Pharm, Dept Bioorgan Chem, Chair Organ Chem, Krakow, Poland
机构:
Karpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Tamil Nadu Dr MGR Med Univ, Chennai, Tamil Nadu, IndiaKarpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Sasikala, M.
Mohan, S.
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机构:
Karpagam Coll Pharm, Dept Pharmaceut, Coimbatore, Tamil Nadu, India
Tamil Nadu Dr MGR Med Univ, Chennai, Tamil Nadu, IndiaKarpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Mohan, S.
Geetha, M.
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机构:
Karpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Tamil Nadu Dr MGR Med Univ, Chennai, Tamil Nadu, IndiaKarpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Geetha, M.
Nisha, E.
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机构:
Karpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Tamil Nadu Dr MGR Med Univ, Chennai, Tamil Nadu, IndiaKarpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Nisha, E.
Narmadha, N.
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机构:
Karpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Tamil Nadu Dr MGR Med Univ, Chennai, Tamil Nadu, IndiaKarpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India
Narmadha, N.
Nagarajan, A.
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机构:
Karpagam Coll Pharm, Dept Pharmaceut Chem, Coimbatore, Tamil Nadu, India
Tamil Nadu Dr MGR Med Univ, Chennai, Tamil Nadu, IndiaKarpagam Coll Pharm, Dept Pharmaceut Anal, Coimbatore, Tamil Nadu, India