Synthesis and Evaluation of NewBis-1,3,4,2-triazaphospholino-alkane Derivatives as In Vitro alpha-Amylase and Lipase Inhibitors

A series of new 1,-bis-(5-alkyl-2-oxide-3-tosyl-1,3,4,2-triazaphospholino)alkanes 2 and 3 were prepared in good yields by the treatment of 1,-bis-(1-tosylamidrazone)alkanes 1 with two molar equivalents of phosphoryl trichloride and phenylphosphonic dichloride, respectively. All the newly synthesized...

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Published inArchiv der Pharmazie (Weinheim) Vol. 348; no. 3; pp. 188 - 193
Main Authors Hamzaoui, Salwa, Ben Salah, Bochra, Hamden, Khaled, Rekik, Awatef, Kossentini, Mohamed
Format Journal Article
LanguageEnglish
Published WEINHEIM Wiley 01.03.2015
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Multidisciplinary
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
Obesity
KEY ENZYMES
Bis-triazaphospholinoalkanes
BIOLOGICAL-ACTIVITY
alpha-Amylase
Diabetes
Lipase
HYPERTENSION
BIS
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Summary:A series of new 1,-bis-(5-alkyl-2-oxide-3-tosyl-1,3,4,2-triazaphospholino)alkanes 2 and 3 were prepared in good yields by the treatment of 1,-bis-(1-tosylamidrazone)alkanes 1 with two molar equivalents of phosphoryl trichloride and phenylphosphonic dichloride, respectively. All the newly synthesized compounds were characterized by IR, H-1 NMR, C-13 NMR, P-31 NMR, and elemental analysis. All the new compounds were screened for their inhibitory effect on the key enzymes related to diabetes and obesity, as -amylase and lipase. The in vitro study revealed that these alkane derivatives exert an inhibitory action against these key enzymes, especially 2b with an IC50 of 16g/mL against -amylase and lipase. Overall, the findings of the current study indicate that 2d exhibits attractive properties and can therefore be considered for future application in the development of antidiabetic and hypolipidemic drugs.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.201400283