Cilastatin is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Dehydropeptidase is an enzyme found in the kidney and is responsible for degrading the antibiotic imipenem. Cilastatin can therefore be combined intravenously with imipenem in order to protect it from dehydropeptidase and prolong its antibacterial effect. Cilastatin itself does not have antibiotic activity although it has been proved to be active against a zinc-dependent beta-lactamase that usually confer antibiotic resistance to certain bacteria.
Graham, Donald W.; Ashton, Wallace T.; Barash, Louis; Brown, Jeannette E.; Brown, Ronald D.; Canning, Laura F.; Chen, Anna; Springer, James P.; Rogers, Edward F. Inhibition of the mammalian β-lactamase renal dipeptidase (dehydropeptidase-I) by Z-2-(acylamino)-3-substituted-propenoic acids. Journal of Medicinal Chemistry. Volume 30. Issue 6. Pages 1074-90. Journal. (1987).
Vinogradov, M. G.; Kaigorodova, L. N.; Chel'tsova-Bebutova, G. V.; Gorshkova, L. S.; Starostin, E. K.; Nikishin, G. I.; Ignatenko, A. V.; Shapiro, E. A. New approach to the synthesis of cilastatin, the inhibitor of renal dipeptidase. Izvestiya Akademii Nauk, Seriya Khimicheskaya. Issue 1. Pages 171-5. Journal. (1995).
Li, Quanliang; Zhai, Baokang. Process for preparation of cilastatin. Assignee Jiangxi Jindun Flavor Co., Ltd., Peop. Rep. China. CN 102875433. (2013).
Jayachandra, Suresh Babu; Yogesh, Ruchika; Morampudi, Raghuram; Khanduri, Chandra Has. Process for the preparation of cilastatin and its salts. Assignee Ranbaxy Laboratories Limited, India. WO 2011061609. (2011).
