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Novel C-2 Symmetric...
Novel C-2 Symmetric Molecules as -Glucosidase and -Amylase Inhibitors : Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics
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- Shahzad, Danish (author)
- Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
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- Saeed, Aamer (author)
- Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
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- Larik, Fayaz Ali (author)
- Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
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- Channar, Pervaiz Ali (author)
- Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
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- Abbas, Qamar (author)
- Univ Sindh, Dept Physiol, Jamshoro 76080, Pakistan
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- Alajmi, Mohamed F. (author)
- King Saud Univ, Dept Pharmacognosy, Coll Pharm, Riyadh 11451, Saudi Arabia
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- Arshad, M. Ifzan (author)
- Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
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- Erben, Mauricio F. (author)
- UNLP, CONICET, CEQUINOR, Dept Quim,Fac Ciencias Exactas,CCT La Plata, Blvd 120 E-60 & 64 1465, RA-1900 La Plata, Argentina
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- Hassan, Mubashir (author)
- Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, 56 Gongjudehak Ro, Gongju 32588, Chungnam, South Korea
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- Raza, Hussain (author)
- Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, 56 Gongjudehak Ro, Gongju 32588, Chungnam, South Korea
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- Seo, Sung-Yum (author)
- Kongju Natl Univ, Coll Nat Sci, Dept Biol Sci, 56 Gongjudehak Ro, Gongju 32588, Chungnam, South Korea
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- El-Seedi, Hesham (author)
- Uppsala universitet,Farmakognosi
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(creator_code:org_t)
- 2019-04-17
- 2019
- English.
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In: Molecules. - : MDPI. - 1431-5157 .- 1420-3049. ; 24:8
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Abstract
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- A series of symmetrical salicylaldehyde-bishydrazine azo molecules, 5a-5h, have been synthesized, characterized by H-1-NMR and C-13-NMR, and evaluated for their in vitro -glucosidase and -amylase inhibitory activities. All the synthesized compounds efficiently inhibited both enzymes. Compound 5g was the most potent derivative in the series, and powerfully inhibited both -glucosidase and -amylase. The IC50 of 5g against -glucosidase was 0.35917 +/- 0.0189 mu M (standard acarbose IC50 = 6.109 +/- 0.329 mu M), and the IC50 value of 5g against -amylase was 0.4379 +/- 0.0423 mu M (standard acarbose IC50 = 33.178 +/- 2.392 mu M). The Lineweaver-Burk plot indicated that compound 5g is a competitive inhibitor of -glucosidase. The binding interactions of the most active analogues were confirmed through molecular docking studies. Docking studies showed that 5g interacts with the residues Trp690, Asp548, Arg425, and Glu426, which form hydrogen bonds to 5g with distances of 2.05, 2.20, 2.10 and 2.18 angstrom, respectively. All compounds showed high mutagenic and tumorigenic behaviors, and only 5e showed irritant properties. In addition, all the derivatives showed good antioxidant activities. The pharmacokinetic evaluation also revealed promising results
Subject headings
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
Keyword
- bis-azo Schiff bases
- dual inhibitor
- -glucosidase inhibitor
- -amylase
- antioxidant
- SAR
- chemo-informatics
- kinetic mechanism
- molecular docking
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- ref (subject category)
- art (subject category)
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- By the author/editor
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Shahzad, Danish
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Saeed, Aamer
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Larik, Fayaz Ali
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Channar, Pervaiz ...
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Abbas, Qamar
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Alajmi, Mohamed ...
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show more...
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Arshad, M. Ifzan
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Erben, Mauricio ...
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Hassan, Mubashir
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Raza, Hussain
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Seo, Sung-Yum
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El-Seedi, Hesham
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show less...
- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Chemical Science ...
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and Organic Chemistr ...
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Molecules
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Uppsala University