1580504-38-6Relevant articles and documents
Biarylmethoxy nicotinamides as novel and specific inhibitors of mycobacterium tuberculosis
Kedari, Chaitanya Kumar,Roy Choudhury, Nilanjana,Sharma, Sreevalli,Kaur, Parvinder,Guptha, Supreeth,Panda, Manoranjan,Mukerjee, Kakoli,Ramachandran, Vasanthi,Bandodkar, Balachandra,Ramachandran, Sreekanth,Tantry, Subramanyam J.
, p. 491 - 495 (2014/06/09)
A whole cell based screening effort on a focused library from corporate collection resulted in the identification of biarylmethoxy nicotinamides as novel inhibitors of M. tuberculosis (Mtu) H37Rv. The series exhibited tangible structure-activity relationships, and during hit to lead exploration, a cellular potency of 100 nM was achieved, which is an improvement of >200-fold from the starting point. The series is very specific to Mtu and noncytotoxic up to 250 μM as measured in the mammalian cell line THP-1 based cytotoxicity assay. This compound class retains its potency on several drug sensitive and single drug resistant clinical isolates, which indicate that the compounds could be acting through a novel mode of action.