Abstract
An ecofriendly effective synthetic reaction pathway has been developed for the synthesis of phosphoramidates under mild reaction conditions. This is a green procedure and can be used in drug discovery for the synthesis of phosphoramidate intermediates used as prodrugs to enhance therapeutic potential properties of the parent drugs. All the title compounds are docked with α-amylase and also tested for in vitro α-amylase activity. All the synthesized compounds (3a–h) have exhibited higher in vitro α-amylase inhibitory activity than the standard acarbose, with 3f, 3g and 3h showing the better activity. The docking results are in good agreement with the in vitro α-amylase inhibitory activity. Interestingly aromatic phosphites have shown good activity when compared with aliphatic phosphites.
Graphical Abstract
Acknowledgments
The authors express thank Prof. C. Devendranath Reddy, Department of Chemistry, Sri Venkateswara University, Tirupati, for his helpful discussions and University Grants Commission (UGC), New Delhi, India, for providing BSR-RFSMS to Mr. Shaik Mahammad Sadik. F.25-1/2014-15 (BSR)/7-187/2007 (BSR) dated 13-03-2015. One of the authors Dr. G Mohan acknowledges DST-PURSE 2nd Phase Programme facilitated at Sri Venkateswara University, Tirupati, India, supported by Department of Science and Technology, New Delhi, India [17118-UGC-III(3)/DST-PURSE 2nd Phase/2017, Dt: 23-08-2018] for instrumental analysis and funding. One of the authors S. Santhisudha expresses her sincere thanks to DST, New Delhi, India, for providing financial support through Woman Scientist Scheme-A (WOS-A) (F. no.: SR/WOS-A/CS-104/2018, Dated: 27-09-2019).