- DDX3X inhibitors, an effective way to overcome HIV-1 resistance targeting host proteins
-
The huge resources that had gone into Human Immunodeficiency virus (HIV) research led to the development of potent antivirals able to suppress viral load in the majority of treated patients, thus dramatically increasing the life expectancy of people living with HIV. However, life-long treatments could result in the emergence of drug-resistant viruses that can progressively reduce the number of therapeutic options, facilitating the progression of the disease. In this scenario, we previously demonstrated that inhibitors of the human DDX3X helicase can represent an innovative approach for the simultaneous treatment of HIV and other viral infections such as Hepatitis c virus (HCV). We reported herein 6b, a novel DDX3X inhibitor that thanks to its distinct target of action is effective against HIV-1 strains resistant to currently approved drugs. Its improved in vitro ADME properties allowed us to perform preliminary in vivo studies in mice, which highlighted optimal biocompatibility and an improved bioavailability. These results represent a significant advancement in the development of DDX3X inhibitors as a novel class of broad spectrum and safe anti-HIV-1 drugs.
- Boccuto, Adele,Botta, Maurizio,Brai, Annalaura,Bugli, Francesca,Dreassi, Elena,Garbelli, Anna,Giannini, Alessia,Maga, Giovanni,Martini, Maurizio,Pennisi, Carla,Riva, Valentina,Saladini, Francesco,Sanguinetti, Maurizio,Trivisani, Claudia Immacolata,Zamperini, Claudio,Zazzi, Maurizio
-
-
- Sulfapyridine hapten and artificial antigen as well as preparation method and application thereof
-
The invention relates to sulfapyridine hapten and artificial antigen as well as a preparation method and application thereof. The structure of the sulfapyridine hapten is shown as a formula (1), wherein the R1 and R2 are hydrogen, methyl or methoxyl; m is
- -
-
Paragraph 0088; 0097; 0098; 0090; 0103; 0104
(2020/02/14)
-
- NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
-
The present invention discloses compounds according to Formula (I): (I). Wherein R1, R2, R5 and Cy are as defined herein. The present invention relates to compounds, methods for the production of said compounds, pharmaceutical compositions comprising said compounds and methods for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, pain, fibrosis and/or proliferative diseases by administering said compounds.
- -
-
Paragraph 0214
(2020/10/20)
-
- GOLD (I)-PHOSPHINE 1,2,3-TRIAZOLE DERIVATIVES WITH ANTIOBIOTIC PROPERTIES
-
The present invention relates to gold (l)-phosphine 1,2,3-triazole compounds, and their use in a human or animal medicine. The present invention also relates to using such compounds for the prevention and/or treatment of an infection, i.e. inhibitors of growth of Gram-positive and/or Gram-negative bacteria. On another aspect the invention relates to the synthesis of the gold (l)-phosphine compounds of the invention and to their synthesis intermediates. The present invention finds applications in the medical, veterinary and/or chemical fields.
- -
-
-
- Single-Molecule Observation of the Intermediates in a Catalytic Cycle
-
The development of catalysts benefits from knowledge of the intermediate steps that accelerate the transformations of substrates into products. However, key transient species are often hidden in ensemble measurements. Here, we show that a protein nanoreac
- Ramsay, William J.,Bell, Nicholas A. W.,Qing, Yujia,Bayley, Hagan
-
supporting information
p. 17538 - 17546
(2019/01/04)
-
- Alkyne-mediated domino hydroformylation/double cyclization: Mechanistic insight and synthesis of (±)-tashiromine
-
A novel domino reaction, alkyne-mediated domino hydroformylation/double cyclization, has been developed for rapid preparation of indolizidine type alkaloids. DFT calculations were applied for rationales of reactivity and selectivity. A concise synthesis of tashiromine as the application of the methodology is also reported.
- Chiou, Wen-Hua,Lin, Yi-Huei,Chen, Guei-Tang,Gao, Yu-Kai,Tseng, Yu-Che,Kao, Chien-Lun,Tsai, Jui-Chi
-
supporting information; experimental part
p. 3562 - 3564
(2011/04/26)
-
- An effective synthetic entry to fused benzimidazoles via iodocyclization
-
A protocol for the synthesis of the fused heterocyclic polycyclic compounds pyrrole[1,2-a]benzimidazoles, piperidine[1,2-a]benzimidazoles and oxa-fused benzimidazoles using iodine and silver nitrate by an exo-dig or endo-dig cyclization pathway at room te
- Zhang, Xu,Zhou, Yu,Wang, Hengshuai,Guo, Diliang,Ye, Deju,Xu, Yungen,Jiang, Hualiang,Liu, Hong
-
supporting information; experimental part
p. 1429 - 1437
(2011/08/03)
-
- Intramolecular PIFA-mediated alkyne amidation and carboxylation reaction
-
(Chemical Equation Presented) The hypervalent iodine reagent PIFA promotes the intramolecular electrophilic cyclization of easily accessible alkynylamides and alkynyl carboxylic acids, leading to the formation of pyrrolidinone and lactone skeletons, respe
- Tellitu, Imanol,Serna, Sonia,Herrero, M. Teresa,Moreno, Isabel,Dominguez, Esther,SanMartin, Raul
-
p. 1526 - 1529
(2007/10/03)
-
- Synthesis of 3-arylpropenyl, 3-arylpropynyl and 3-arylpropyl 2-azetidinones as cholesterol absorption inhibitors: Application of the palladium-catalyzed arylation of alkenes and alkynes
-
A series of 3-(3'-arylpropenyl)-2-azetidinones 8a-8k and 3-(3'-arylpropynyl)-2-azetidinones 16m-16p were prepared by the palladium-catalyzed arylation of 3-(3'-propenyl)-2-azetidinone 7, or by arylation of 4-pentenoic acid, or via ethyl 4-pentynoate followed by 2-azetidinone ring construction. The unsaturated 2-azetidinones were transformed to their saturated analogs 9a-9p by catalytic hydrogenation. Azetidinones 8a-8k, 9a-9p, and 16m-16p were evaluated for their biological activity as cholesterol absorption inhibitors in hamsters. (C) 2000 Elsevier Science Ltd.
- Rosenblum, Stuart B.,Huynh, Tram,Afonso, Adriano,Davis Jr., Harry R.
-
p. 5735 - 5742
(2007/10/03)
-
- New anionic cyclization of 4- and 5-alkynylamines: Synthesis of 2-Benzylidene pyrrolidines and piperidines
-
Treatment of 4- and 5-alkynylamines with 0.5-1.2 equiv. of butyllithium brought about a facile anionic cyclization, giving the corresponding enamine pyrrolidines and piperidines having an exo double bond in high yields. Treatment of 4-alkynamides with lit
- Tokuda, Masao,Fujita, Hirotake,Nitta, Makoto,Suginome, Hiroshi
-
p. 385 - 395
(2007/10/02)
-
- EXO- AND ENDOHORMONES, XVI SYNTHESIS OF (4E, 7Z)-4,7-TRIDECADIEN 1-YL ACETATE, THE SEX PHEROMONE FOR THE LEAFMINER LITHOCOLLETIS CORYLIFOLIELLA
-
The synthesis of the sex pheromone of the leafminer moth, Lithocolletis corylifoliella, (4E, 7Z)-4,7-tridecadien-1-yl acetate, was based on a C5+C8 scheme.The coupling reaction took place between the Grignard reagent of 4-pentin-1-1-oic acid and 1-bromo-2Z-octene.Propargylic alcohol was used as a starting material in order to obtain the two synthons.
- Gocan, Alexandra,Gansca, Lucia,Oprean, Ioan
-
p. 253 - 258
(2007/10/03)
-