270260-56-5Relevant academic research and scientific papers
Small-Molecule Inhibitors Targeting Sterol 14α-Demethylase (CYP51): Synthesis, Molecular Modelling and Evaluation Against Candida albicans
Binjubair, Faizah A.,Braidley, Peter J.,Kelly, Diane E.,Kelly, Steven L.,Parker, Josie E.,Puri, Kalika,Simons, Claire,Tatar, Esra,Warrilow, Andrew G.
supporting information, (2020/07/04)
Fungal infections are a global issue affecting over 150 million people worldwide annually, with 750 000 of these caused by invasive Candida infections. Azole drugs are the frontline treatment against fungal infections; however, resistance to current azole
ADENINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Page/Page column 131; 132, (2017/12/14)
The present invention relates to a compound suitable for use as a kinase inhibitor according to general formula (I) [compound (C), herein after], or the N- oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or stereoisomer thereof, formula (I) wherein A, R1, R2, R3, R3', R4, R4', X, Y, Z, T are as defined in the claims. The invention further relates to an in vitro method of inhibiting protein kinase activity which comprises contacting a protein kinase with a compound of formula (I), or the N-oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or stereoisomer thereof. The invention further relates to the compounds of formula (I) per se, as well as to their use as a medicament, and for use or in a method of treatment of a disease mediated by a protein kinase selected from cancer, inflammatory disorders, cardiovascular diseases, viral induced diseases, circulatory diseases, fibro-proliferative diseases and pain sensitization disorders.
N-(3-acyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues: Novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor
Lee, Jeewoo,Lee, Jiyoun,Kang, Myungshim,Shin, Myoungyoup,Kim, Ji-Min,Kang, Sang-Uk,Lim, Ju-Ok,Choi, Hyun-Kyung,Suh, Young-Ger,Park, Hyeung-Geun,Oh, Uhtaek,Kim, Hee-Doo,Park, Young-Ho,Ha, Hee-Jin,Kim, Young-Ho,Toth, Attila,Wang, Yun,Tran, Richard,Pearce, Larry V.,Lundberg, Daniel J.,Blumberg, Peter M.
, p. 3116 - 3126 (2007/10/03)
Isosteric replacement of the phenolic hydroxyl group in potent vanilloid receptor (VR1) agonists with the alkylsulfonamido group provides a series of compounds which are effective antagonists to the action of the capsaicin on rat VR1 heterologously expressed in Chinese hamster ovary (CHO) cells. In particular, compound 61, N-[2-(3,4-dimethylbenzyl)-3-pivaloyloxypropyl]-N′-[3-fluoro-4- (methylsulfonylamino)benzyl]thiourea was a full antagonist against capsaicin, displayed a Ki value of 7.8 nM (compared to 520 nM for capsazepine and 4 nM for 5-iodoRTX), and showed excellent analgesic activity in mice. Structure-activity analysis of the influence of modifications in the A- and C-regions of 4-methylsulfonamide ligands on VR1 agonism/antagonism indicated that 3-fluoro substitution in the A-region and a 4-tert-butylbenzyl moiety in the C-region favored antagonism, whereas a 3-methoxy group in the A-region and 3-acyloxy2-benzylpropyl moieties in the C-region favored agonism.
