135065-71-3Relevant academic research and scientific papers
Design, synthesis and biological evaluation of protease inhibitors containing morpholine cores with remarkable potency against both HIV-1 subtypes B and C
Cen, Shan,Ding, Jiwei,Dong, Biao,Ma, Ling,Shan, Qi,Wang, Juxian,Wang, Minghua,Wang, Yucheng,Zhang, Guoning,Zhou, Huiyu,Zhou, Jinming,Zhu, Mei
, (2022/03/15)
By following up on the design vector of optimizing amine-based HIV-1 protease inhibitors, we have designed and biologically evaluated a novel class of inhibitors with the free nitrogen or sulphone in morpholine cores as P2 ligands in combination with diverse substituted phenylsulfonamide P2′ ligands. As it turns out, a majority of these inhibitors exhibit prominent enzymatic inhibitory activity in low nanomolar ranges with relatively low cytotoxicity. Particularly, inhibitor 1e containing a morpholine carboxamide P2 ligand and a 4-hydroxyphenylsulfonamide P2′ ligand illustrates a robust enzyme inhibitory IC50 value of 90 pM. Furthermore, 1e demonstrates impressive in vivo antiviral activity with EC50 value of 89 nM and a degree of inhibitory potency against the DRV-resistant variant. More importantly, 1e exhibits remarkable activity with EC50 values of 13.59 nM and 8.23 nM against subtype C HIV-1 strains ZM246 and Indie, respectively. Furthermore, the in silico studies provide molecular insights into binding features of inhibitors with HIV-1 protease, and furnish a valuable forecast on further process.
Novel hamamelitannin analogues for the treatment of biofilm related MRSA infections–A scaffold hopping approach
Vermote, Arno,Brackman, Gilles,Risseeuw, Martijn D.P.,Coenye, Tom,Van Calenbergh, Serge
, p. 757 - 770 (2017/02/10)
Antimicrobial research is increasingly being focused on the problem of resistance and biofilm formation. Hamamelitannin (HAM) was recently identified as an antimicrobial potentiator for conventional antibiotics towards Staphylococcus aureus. This paper de
1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES
-
Page/Page column 290, (2016/07/05)
The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
5-AMINO-4-CARBAMOYL-PYRAZOLE COMPOUNDS AS SELECTIVE AND IRREVERSIBLE T790M OVER WT-EGFR KINASE INHIBITORS AND USE THEREOF????
-
Paragraph 0246, (2016/03/13)
Disclosed are compounds of Formula (I), pharmaceutical compositions comprising the same, processes for the preparation thereof, and the use thereof.
Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket
Yuan, Jing,Simpson, Robert D.,Zhao, Wei,Tice, Colin M.,Xu, Zhenrong,Cacatian, Salvacion,Jia, Lanqi,Flaherty, Patrick T.,Guo, Joan,Ishchenko, Alexey,Wu, Zhongren,McKeever, Brian M.,Scott, Boyd B.,Bukhtiyarov, Yuri,Berbaum, Jennifer,Panemangalore, Reshma,Bentley, Ross,Doe, Christopher P.,Harrison, Richard K.,McGeehan, Gerard M.,Singh, Suresh B.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
scheme or table, p. 4836 - 4843 (2011/09/16)
Structure-based design led to the discovery of a novel class of renin inhibitors in which an unprecedented phenyl ring filling the S1 site is attached to the phenyl ring filling the S3 pocket. Optimization for several parameters including potency in the p
RENIN INHIBITORS
-
Page/Page column 30-31, (2010/08/07)
Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the t
Renin Inhibitors
-
Page/Page column 51, (2010/12/29)
Disclosed are compounds having the formula (I): wherein the R1, R2, R3, X, Y, A, L, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
BENZAMIDE DERIVATIVES, THEIR PREPARATION AND USES IN MEDICINE THEREOF
-
Page/Page column 10, (2010/06/15)
The present invention discloses novel benzamide derivatives represented by general formula (I), their preparation, pharmaceutical compositions containing the derivatives and their use as medicament, especially as a 5-HT4 stimulator, wherein the
BENZAMIDE DERIVATIVES, THEIR PREPARATION AND USES IN MEDICINE THEREOF
-
Page/Page column 9, (2010/08/22)
The present invention discloses novel benzamide derivatives represented by general formula (I), their preparation, pharmaceutical compositions containing the derivatives and their use as medicament, especially as a 5-HT4 stimulator, wherein the
