175152-65-5Relevant academic research and scientific papers
Polymer support assisted selective functionalization of Azoles using a palladium-catalyzed coupling reaction
Kondo, Yoshinori,Komine, Takashi,Sakamoto, Takao
, p. 3111 - 3113 (2000)
(matrix presented) Regioselective palladium-catalyzed monoarylation of azoles was achieved using iodobenzoate immobilized on an insoluble polymer support. The positional selectivity for the coupling reaction was dramatically influenced by the presence of Cul. No diarylation was observed in either case. Unsymmetrical diarylation was also obtained with the polymer support using sequential coupling reactions.
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.
supporting information, 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.
Novel imidazole compounds as a new series of potent, orally active inhibitors of 5-lipoxygenase
Mano, Takashi,Stevens, Rodney W.,Ando, Kazuo,Nakao, Kazunari,Okumura, Yoshiyuki,Sakakibara, Minoru,Okumura, Takako,Tamura, Tetsuya,Miyamoto, Kimitaka
, p. 3879 - 3887 (2007/10/03)
Replacement of the dihydroquinolinone pharmacophore of Zeneca's ZD2138 by ionizable imidazolylphenyl moiety has lead to the discovery of a novel series of potent and orally active 5-lipoxygenase (5-LO) inhibitors. The synthesis and structure-activity relationship (SAR) of this series of compounds are described herein.
Benzoheterocyclic derivatives
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Page column 90, (2010/01/21)
A benzoheterocyclic derivative of the following formula [1]: and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist, vasopressin agonist or oxytocin antagonist.
