113137-29-4Relevant articles and documents
Discovery of atrop fixed alkoxy-aminobenzhydrol derivatives: Novel, highly potent and orally efficacious squalene synthase inhibitors
Ichikawa, Masanori,Yokomizo, Aki,Itoh, Masao,Haginoya, Noriyasu,Sugita, Kazuyuki,Usui, Hiroyuki,Terayama, Koji,Kanda, Akira
experimental part, p. 5207 - 5224 (2011/10/08)
We have recently reported the discovery of the new benzhydrol template, which has a highly potent inhibitory activity for squalene synthase, as typified by compound 1 (SSI IC50 = 0.85 nM). However, it was composed of a pair of easy rotatable at
Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz
Markwalder, Jay A.,Christ, David D.,Mutlib, Abdul,Cordova, Beverly C.,Klabe, Ronald M.,Seitz, Steven P.
, p. 619 - 622 (2007/10/03)
Studies on the biotransformation of the clinically important non-nucleoside reverse transcriptase inhibitor efavirenz have shown that oxidation and secondary conjugation are important components of the processing of this molecule in vivo. We have synthesized metabolites of efavirenz to confirm their structure and to evaluate their activity as antivirals.
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA(TM)) as HIV-1 reverse transcriptase inhibitors
Patel, Mona,Ko, Soo S.,McHugh Jr., Robert J.,Markwalder, Jay A.,Srivastava, Anurag S.,Cordova, Beverly C.,Klabe, Ronald M.,Erickson-Viitanen, Susan,Trainor, George L.,Seitz, Steven P.
, p. 2805 - 2810 (2007/10/03)
Efavirenz (SUSTIVA(TM)) is a potent non-nucleoside reverse transcriptase inhibitor. Due to the observation of breakthrough mutations of the reverse transcriptase enzyme during Efavirenz therapy, we sought to develop an optimized second generation series. To that end, SAR of the substituents on the aromatic ring was undertaken and the results are summarized here. The 5,6-difluoro (4f) and the 6-methoxy (4m) substituted benzoxazinones were determined to be equipotent, and as a result such substitution patterns will be incorporated in second generation scaffolds.