95672-01-8Relevant academic research and scientific papers
Synthesis and evaluation of new elastase inhibitors. I. 1,1-Dioxocephem-4-thiolesters
Alpegiani,Baici,Bissolino,Carminati,Cassinelli,Del Nero,Franceschi,Orezzi,Perrone,Rizzo,Sacchi
, p. 875 - 890 (2007/10/02)
Several 7α-chloro and 7α-methoxy cephalosporin thiolester sulphones variously substituted at the C-3' position were synthesized from 7-amino-3-deacetoxycephalosporanic acid (7-ADCA). The compounds are time-dependent inhibitors of human leukocyte elastase
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters
Doherty,Ashe,Barker,Blacklock,Butcher,Chandler,Dahlgren,Davies,Dorn Jr.,Finke,Firestone,Hagmann,Halgren,Knight,Maycock,Navia,O'Grady,Pisano,Shah,et al.
, p. 2513 - 2521 (2007/10/02)
Time-dependent inhibitors of the enzyme human leukocyte elastase have been developed based on the cephem nucleus. A series of cephalosporin tert-butyl esters has been examined, and the activity of these compounds has been found to be very sensitive to C-7
A Versatile Synthesis of 1,1-Dioxo 7-Substituted Cephems: Preparation of the Human Leukocyte Elastase (HLE) Inhibitor 1,1-Dioxo-trans-7-methoxycephalosporanic Acid tert-Butyl Ester
Blacklock, Thomas J.,Butcher, John W.,Sohar, Paul,Rothauser Lamanec, Theresa,Grabowski, Edward J. J.
, p. 3907 - 3913 (2007/10/02)
A four-step synthesis of the human leukocyte elastase (HLE) inhibitor 1,1-dioxo-trans-7-methoxycephalosporanic acid tert-butyl ester in 44percent isolated yield from 7-aminocephalosporanic acid (7-ACA) is described.A variety of 7-substituents have been introduced via metal-catalyzed diazo insertion reactions, and the use of a flow reactor for chemodiscriminate control of particularly rapid reactions is presented.A chemoselective oxidation of 7-ACA tert-butyl ester to the corresponding 1,1-dioxide without formal N-protection is introduced.
