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Simplified captopril analogues as NDM-1 inhibitors

, : Simplified captopril analogues as NDM-1 inhibitors. Bioorganic & Medicinal Chemistry Letters 24(1): 386-389

Captopril is a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 value of 7.9μM. It is composed of two units: a 3-mercapto-2-methylpropanoyl fragment and a proline residue. In this study, we synthesized simple amide derivatives of 3-mercapto-2-methylpropanoic acid, and then tested them as NDM-1 inhibitors in order to identify the pharmacophore for NDM-1 inhibition. We found that the lead compound 22 had an IC50 value of 1.0μM. Further structure simplification provided compounds 31 and 32, which had IC50 values of 15 and 10μM, respectively. As compound 32 is a clinically used antidote for metal poisoning, it has great potential to be repurposed to treat bacterial infections.


PMID: 24269122

DOI: 10.1016/j.bmcl.2013.10.068

Other references

Skuditskiĭ, A.E., 1987: A rare case of maternal alloimmunization by fetal antigen M. Gematologiia i Transfuziologiia 32(12): 41-42

Anonymous, 2006: Opportunities. NlmCategory="UNASSIGNED">qualifications represent advanced practice. Operating department practitioners and allied health professionals would stay with the Health Professions Council.

Peethambaran, C.K., 1996: Cashew in Kenya. The history of cashew production in Kenya, current production of cashews (including marketing and processing) and reasons for the decline in cashew production (including the mismanagement of cooperatives set up to buy cashews which caused poor ret...

Lindsley, K.; Pamidimukkala, J.; Lubahn, D.; Hay, M., 2001: Baroreflex heart rate responses in estrogen receptor-alpha knockout mice. Estrogens are known to not only play an important role in reproductive behaviour and physiology but also effect the cardiovascular system. The role of the estrogen receptor-alpha (ERalpha) in mediating the classical effects of estrogens on the dev...

Fremuth, J., 1981: Barypeithes Exomias paratenex spec nov aus Mittelewopa Coleoptera, Curculionidae. Entomologische Blaetter fuer Biologie und Systematik der Kaefer. 1980 ; 762-3: 70-72

Holtenius, P.; Traven, M., 1990: Impaired glucose tolerance and heterogeneity of insulin responses in cows with abomasal displacement. Injections of glucagon in dairy cows resulted in a rapid and marked increase in serum insulin and also in plasma glucose. Glucagon injection appears to be a simple and useful method for testing insulin secretion and glucose release. There was a so...

Paterson, M.J.; Rudd, J.W.M.; Louis, V.S., 1998: Increases in total and methylmercury in zooplankton following flooding of a peatland reservoir. Fish from new reservoirs often have elevated concentrations of methylmercury (MeHg) that they primarily accumulate from food such as zooplankton. The objectives of this research were (i) to determine the effect of reservoir creation on total mercu...

Pacsu, E., 2010: Carbohydrate orthoesters. Advances in Carbohydrate Chemistry 1: 77-127

Daly K.L.; Macaulay M.C., 1991: Influence of physical and biological mesoscale dynamics on the seasonal distribution and behavior of euphausia superba in the antarctic marginal ice zone. The influence of day length, currents, sea ice presence, seawater temperature and salinity, chlorophyll a, particulate organic carbon, and predators was investigated in relation to the distribution and behavior of life history stages of Euphausia...

Bardzilauskene, A.; Morkunas, B.; Velikis, A.; Mil'ner, E.; Orinene, A., 1988: Identification of conditionally pathogenic Enterobacteriaceae isolated from the environment and the use of the results in epidemiologic practice. Gigiena i Sanitariia: 65-67