LEOCILLIN (BENZYL PENICILLIN‐β‐DIETHYLAMINOETHYLESTER HYDRIODIDE)

Jensen, K. A.; Dragsted, P. J.; Kiær, I.; Nielsen, Erling Juhl; Frederiksen, E

doi:10.1111/j.1699-0463.1951.tb03706.x

Cited by 23 publications

(2 citation statements)

References 5 publications

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“…A proposal for this program described testing of antibiotic-containing substrates on pathogenic bacteria, "that are not satisfactorily treatable with penicillin, streptomycin or sulfonamides and which play an important role in human or veterinary pathology" (Quote from 39). One example was Leocillin (Benzylpenicillin-bdiethylaminoethylester hydriodide) which found application in veterinary practice [39][40][41]. LEO Pharma was also interested in the application of antibiotics for veterinary use, as feed supplements [39].…”

Section: A Concerted Effort From World War I and To The 1980smentioning

confidence: 99%

Veterinary bacteriology in Denmark from the 1880s to 2022

Leisner

Larsen

2023

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This paper gives an account of the history of veterinary bacteriology including clinical veterinary bacteriology as well as the area of veterinary public health in Denmark from the 1880s to 2022. We describe key persons, including B. Bang, C.O. Jensen, K.A. Jensen and others who made important contributions to the development of these areas of microbiological expertise, and we discuss how challenges ranging from bovine tuberculosis to bacterial antimicrobial resistance have been met. Further, we describe progress in research on important bacterial pathogens both with regard to animal clinical aspects and zoonotic food‐related aspects. Finally, we describe current issues in relation to One Health and research organization.

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Section: A Concerted Effort From World War I and To The 1980smentioning

confidence: 99%

Veterinary bacteriology in Denmark from the 1880s to 2022

Leisner

Larsen

2023

APMIS

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“…Fifty different penicillin esters had been tested in collaboration with K. A. Jensen by 1951, increasing to at least 75 different compounds in 1954 ( Table 2 and Figures 2, 3) 23 . One outcome was Leocillin (Benzylpenicillin, β-diethylaminoethyl ester hydrochloride) with a high lung affinity that found application as a veterinary product (Jensen et al, 1951;Schrøder, 2005). This compound was an inspiration to LEO to search for anti-tuberculosis compounds with similar affinities as mentioned previously 24 .…”

Section: The Search For Natural Product Antibiotics At Leo During Thementioning

confidence: 99%

The Diverse Search for Synthetic, Semisynthetic and Natural Product Antibiotics From the 1940s and Up to 1960 Exemplified by a Small Pharmaceutical Player

Leisner

2020

Front. Microbiol.

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The 1940s and 1950s witnessed a diverse search for not just natural product antibiotics but also for synthetic and semisynthetic compounds. This review revisits this epoch, using the research by a Danish pharmaceutical company, LEO Pharma, as an example. LEO adopted a strategy searching for synthetic antibiotics toward specific bacterial pathogens, in particular Mycobacterium tuberculosis, leading to the discovery of a new derivative of a known drug. Work on penicillin during and after WWII lead to the development of associated salts/esters and a search for new natural product antibiotics. This led initially to no new, marketable compounds, but concluded with the serendipitous discovery of fusidic acid, an antibiotic used to treat infections by Staphylococcus aureus, in 1960. The discovery process included contemporary approaches such as open innovation; targeting specific pathogens and/or specific organs in the patient; examining the effects of antimicrobial compounds on bacterial virulence as well as on antibioticresistant variants, and searching for antibiotic producers among microorganisms not previously well explored. These activities were promoted by the collaboration with a renowned Danish clinical microbiologist, K. A. Jensen, as well as company expertise in fermentation technologies, chemical synthesis and purification of bioactive compounds from organic materials.

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Modification de la Fonction Carboxy de la Pénicilline

Claesen¹,

Vanderhaeghe²

1964

Bulletin des Soc Chimique

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La fonction carboxy de la pknicilline V (I, R = C~HBOCHP, X = OH) a ktk transformke en fonction alcool, par rkduction de l'azide avec du LiBH4. L'azide a permis aussi la synthkse du benzylcarbamate. Lors de la rkduction de l'ester de la p6nicilline V, la fonction ester et le carbonyle du ,R-lactam sont reduits par le LiBH4.La fonction carboxy de la penicilline (I, X = OH) semble indispensable a l'activitt antibactkrienne de cet antibiotique. L'estbrification de cette fonction (par ex. I, X = OCHs ou -0CzHs) fait disparaitre l'activitt antimicrobienne (1). Quand on administre ces esters de ptnicilline des animaux, on n'observe pas d'activit6 antibacttrienne dam le sang, sauf chez les rongeurs qui possbdent une esttrase capable d'hydrolyser cette fonction ester. Un ester de ptnicilline (I, R = C~H~C H F , X = OCHz CHzN(CzH5)z-HI) est utilisC en therapeutique humaine mais son emploi est bast sur son hydrolyse spontante a un pH physiologique (293).Nous avons voulu examiner le Emplacement du groupe COOH par une fonction -CHzOH. A cause de l'instabilitk de la p6nicilline en milieu acide et alcalin, seule la reduction d'une forme rdactionelle du carboxyle (4) a Ctt envisagte. La rtduction au LiBH4 du chlorure acide de la -X = CI), dtcrits par Villax (5), a donne avec de mauvais rendements, un mtlange complexe qui contenait, d'aprbs la chromatographie en couche mince le pCnicillano1 (V). pknicilline G (I, R = CsH5CH2, -X = Cl) et V (I, R = CtjH&H@, ( l ) H.T. CLARKE, J.R. JOHNSON et R. ROBINSON, The Chemistry of' penicillin, p. 93 et p. 680, Princeton Univ. Press, 1949.

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LEOCILLIN (BENZYL PENICILLIN‐β‐DIETHYLAMINOETHYLESTER HYDRIODIDE)

Cited by 23 publications

References 5 publications

Veterinary bacteriology in Denmark from the 1880s to 2022

Veterinary bacteriology in Denmark from the 1880s to 2022

The Diverse Search for Synthetic, Semisynthetic and Natural Product Antibiotics From the 1940s and Up to 1960 Exemplified by a Small Pharmaceutical Player

Modification de la Fonction Carboxy de la Pénicilline

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