74270-72-7Relevant articles and documents
Synthesis and anti-endoplasmic reticulum stress activity of N-substituted-2-arylcarbonylhydrazinecarbothioamides
Choi, Hoon,Yun, Wheesahng,Lee, Jung-hun,Jang, Seoul,Park, Sang Won,Kim, Dong Hwan,Seon, Kyoung Pyo,Hyun, Jung-mi,Jeong, Kwiwan,Ku, Jin-mo,Nam, Tae-gyu
, p. 2142 - 2152 (2019/11/03)
Misfolded or unfolded proteins are accumulated in lumen of endoplasmic reticulum (ER) in ER stress condition. It has been implicated in many pathological conditions such as Alzheimer’s disease, diabetic retinopathy, atherosclerosis, β-cell apoptosis and lung inflammation. We found a series of N-substituted-2-arylcarbonylhydrazinecarbothioamides to potently decrease ER stress signal, showing up to almost 300-fold better activity than 1-hydroxynaphthoic acid and tauro-ursodesoxycholic acid, positive controls, respectively. Structure?activity relationship (SAR) study showed that 2-arylcarbonyl moiety is critical for the activity of the hydrazinecarbothioamide analogues and side chains tethering on thioamide moiety were relatively insensitive to the activity. Some analogues were found to consistently exert the potency under more physiologically relevant condition where ER stress was induced by palmitic acid. ER stress markers such as CHOP and phosphorylated eIF2α and PERK were accordingly decreased in western blotting upon treatment of compound 4h. Potential ER stress inhibitory activity and novel structures could provide a novel platform for new chemical chaperone and therapy for protein misfolding diseases.
Synthesis and molecular docking studies of glucose-linked isonicotinoyl- 1, 3, 4-thiadiazolidines as antitubercular agents
Chavan, Snehal A.,Ulhe, Avinash G.,Berad, Baliram N.,Chikhale, Rupesh V.
, p. 15 - 22 (2018/03/05)
Background: The recent emergence of multidrug-resistant strains of M. tuberculosis that are resistant to two major effective drugs, viz. isoniazid and rifampicin, stimulated us to make an attempt for the development of a new class of potent antitubercular
Synthesis and antitumor activity of 4-cyclohexyl/aryl-5-(pyridin-4-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones
Bhat, Mashooq Ahmad,Al-Omar, Mohamed A.,Naglah, Ahmed M.,Abdulla, Mohamed M.,Fun, Hoong-Kun
, p. 1558 - 1567 (2015/04/21)
The reaction of 2-isonicotinoyl-N-cyclohexyl/arylhydrazinecarbothioamide (2a-r) with sodium hydroxide, in each case, a single product was obtained. The structures of the compounds were confirmed on the basis of their elemental analysis and spectral data.