1159599-99-1Relevant articles and documents
SUBSTITUTED PHENYLOXAZOLIDINONES FOR ANTIMICROBIAL THERAPY
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Page/Page column 138; 139, (2017/02/09)
The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
Synthesis and Properties of 2-Oxa-6-azaspiro[3.3]heptane Sulfonate Salts
Van Der Haas, Richard N. S.,Dekker, Jeroen A.,Hassfeld, Jorma,Hager, Anastasia,Fey, Peter,Rubenbauer, Philipp,Damen, Eric
, p. 2394 - 2401 (2017/05/22)
An improved synthesis of the bicyclic spiro compound 2-oxa-6-azaspiro[3.3]heptane is presented. While this compound is often isolated as an oxalate salt, its isolation as a sulfonic acid salt yields a more stable and more soluble product. With these improved properties access to a wider range of reaction conditions with the spirobicyclic 2-oxa-6-azaspiro[3.3]heptane has been enabled.
Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents
Gadekar, Pradip K.,Roychowdhury, Abhijit,Kharkar, Prashant S.,Khedkar, Vijay M.,Arkile, Manisha,Manek, Hardik,Sarkar, Dhiman,Sharma, Rajiv,Vijayakumar,Sarveswari
, p. 475 - 487 (2016/07/19)
The design, synthesis and antimicrobial evaluation of a novel series of azaspiro analogues of linezolid (1) have been described. Linezolid comprises of a morpholine ring which is known for its metabolism-related liabilities. Therefore, the key modificatio
The Development of a Manufacturing Route to an MCHr1 Antagonist
Golden, Michael,Legg, Danny,Milne, David,Arun Bharadwaj,Deepthi,Gopal, Madan,Dokka, Nagaraju,Nambiar, Sudhir,Ramachandra, Puranik,Santhosh,Sharma, Parhalad,Sridharan,Sulur, Manjunatha,Linderberg, Mats,Nilsson, Anders,Sohlberg, Roger,Kremers, John,Oliver, Samuel,Patra, Debasis
, p. 675 - 682 (2016/04/01)
Process development work to provide an efficient manufacturing route to a MCHr1 antagonist is presented herewith. Features of this development work include a scalable manufacturing route to the useful 6-oxa-2-azaspiro[3.3]heptane building block and the use of a (soluble) alternative to sodium triacetoxyborohydride.
Design, synthesis and biological evaluation of paclitaxel-mimics possessing only the oxetane D-ring and side chain structures
Chen, Xing-Xiu,Gao, Feng,Wang, Qi,Huang, Xing,Wang, Dan
, p. 111 - 115 (2014/01/06)
Two spiro paclitaxel-mimics consisting only of an oxetane D-ring and a C-13 side chain were designed and synthesized on the basis of analysis of structure-activity relationships (SAR) of paclitaxel. In vitro microtubule-stabilizing and antiproliferative assays indicated a moderate weaker activity of the mimics than paclitaxel, but which still represented the first example of simplified paclitaxel analogues with significant anti-tumor biological activity.