62473-92-1Relevant articles and documents
Preparation method and medical application of benzisothiazole and benzothiophene
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Paragraph 0166; 0170; 0171; 0209; 0213; 0214, (2021/08/19)
The invention discloses a preparation method and medical application of benzisothiazole and benzothiophene, and telates to the field of pharmaceutical chemistry. According to the invention, benzisothiazole and benzothiophene are the first type of HIF-2 agonists; compared with a compound M1001 found by the applicant in the earlier stage, the invention has better HIF-2 agonist activity, and has remarkable enhancement activity on expression of mRNA and protein of EPO, VGEF, Glut1, NDRG1 and the like at the downstream of HIF-2, so that the invention can be used for preparing drugs for treating and/or preventing chronic kidney diseases/chronic renal anemia, dyslipidemia and high cholesterol caused by abnormal expression of HIF-2; and the method has a good industrialization prospect.
O-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity
Corpas-López, Victoriano,Tabraue-Chávez, Mavys,Sixto-López, Yudibeth,Panadero-Fajardo, Sonia,Alves De Lima Franco, Fernando,Domínguez-Seglar, José F.,Morillas-Márquez, Francisco,Franco-Montalbán, Francisco,Díaz-Gavilán, Mónica,Correa-Basurto, José,López-Viota, Julián,López-Viota, Margarita,Pérez Del Palacio, José,De La Cruz, Mercedes,De Pedro, Nuria,Martín-Sánchez, Joaquina,Gómez-Vidal, José A.
supporting information, p. 5734 - 5751 (2020/07/14)
Leishmania (L.) infantum causes visceral, cutaneous, and mucosal leishmaniasis in humans and canine leishmaniasis in dogs. Herein, we describe that O-alkyl hydroxamate derivatives displayed potent and selective in vitro activity against the amastigote stage of L. infantum while no activity was observed against promastigotes. Compound 5 showed potent in vivo activity against L. infantum. Moreover, the combination of compound 5 supported on gold nanoparticles and meglumine antimoniate was also effective in vivo and improved the activity of these compounds compared to that of the individual treatment. Docking studies showed that compound 5 did not reach highly conserved pocket C and established interactions with the semiconserved residues V44, A45, R242, and E243 in pocket A of LiSIR2rp1. The surface space determined by these four amino acids is not conserved in human sirtuins. Compound 5 represents a new class of selective ligands with antileishmanial activity.
Novel compounds that are inhibitors of YAP/TAZ-TEAD interaction and their use in the treatment of malignant mesothelioma
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, (2020/02/01)
These compounds are useful as inhibitors of the YAP/TAZ-TEAD interaction.