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Article

Synthesis and Elastase Inhibitory Evaluation of Phosphate Esters and Mixed Phosphate Anhydride of Penam Sulfones

Instituto de Química Orgánica de Síntesis (IQUIOS-UNR), Casilla de Correo 991, 2000 Rosario, Argentina
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Author to whom correspondence should be addressed.
Molecules 2000, 5(4), 655-656; https://doi.org/10.3390/50400655
Submission received: 1 April 2000 / Accepted: 3 April 2000 / Published: 5 April 2000

Abstract

:
The evaluation of human leucocite elastase inhibition by phosphate esters (1-2) and phosphate mixed anhydride (3) of penicillin sulfones and their precursor sulfides is described.

Introduction

Human Leukocyte Elastase [1] (HLE, EC 3.4.21.37) is a serine proteinase found in the azurophilic granules of polymorphonuclear leukocytes. This enzyme has been the subject of extensive studies, both in terms of its biological role in numerous diseases [2] and in the development of suitable inhibitors to be used as potential therapeutic agents. This interest has led over the past fifteen years to the synthesis of a wide variety of inhibitors based on the β-lactam nucleus.

Results and Discussion

We have recently reported the structure-activity relationship (S.A.R) of several benzyl and methyl 6-α-substituted penicillanate sulfones [3]. In this communication we describe the synthesis and our initial structure-activity relationship study of a series of phosphate triesters (1-2) and phosphatecarboxylate mixed anhydride (3) of penicillin sulfones. These new penicillin derivatives were evaluated as elastase inhibitors using H.L.E.
Molecules 05 00655 i001

Acknowledgements

UNR, CONICET, Agencia Nacional de Promoción Científica.

References and Notes

  1. a) Edwards, P.D.; Bernstein, P.R. Med. Res. Rev. 1994, 14, 127. b) Hlasta, D.J.; Pagani, E.D. Ann. Rep. Med. Chem. 1994, 29, 195. c) Durette, P.L.; Chabin, R.M. Bioorg. Med. Chem. Lett. 1995, 5, 271.
  2. Weinbaum, G.; Giles, R.E.; Krell, R.D. Ann. N.Y. Acad. Sci. 1991, 624, 1–370.
  3. Boschetti, C.E.; Mata, E.G.; Mascaretti, O.A.; Cricco, J.A.; Coux, G.; Roveri, O.A. Bioorg. Med. Chem. Lett. 1995, 5, 2033. b) Boschetti, C.E.; Mascaretti, O.A.; Cricco, J.A.; Roveri, O.A. Bioorg. Med. Chem. 1995, 3, 95. c) Boschetti, C.E.; Mata, E.G.; Mascaretti, O.A.; Cricco, J.A.; Coux, G.; Lodeyro, A.; Roveri, O.A. J. Braz. Chem. Soc. 1996, 7, 285.

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MDPI and ACS Style

Laborde, M.A.; Mascaretti, O.A. Synthesis and Elastase Inhibitory Evaluation of Phosphate Esters and Mixed Phosphate Anhydride of Penam Sulfones. Molecules 2000, 5, 655-656. https://doi.org/10.3390/50400655

AMA Style

Laborde MA, Mascaretti OA. Synthesis and Elastase Inhibitory Evaluation of Phosphate Esters and Mixed Phosphate Anhydride of Penam Sulfones. Molecules. 2000; 5(4):655-656. https://doi.org/10.3390/50400655

Chicago/Turabian Style

Laborde, María A., and O. A. Mascaretti. 2000. "Synthesis and Elastase Inhibitory Evaluation of Phosphate Esters and Mixed Phosphate Anhydride of Penam Sulfones" Molecules 5, no. 4: 655-656. https://doi.org/10.3390/50400655

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