175838-22-9Relevant academic research and scientific papers
Synergism of a novel 1,2,4-oxadiazole-containing derivative with oxacillin against methicillin-resistant staphylococcus aureus
Buommino, Elisabetta,D’auria, Maria Valeria,De Marino, Simona,Festa, Carmen,Piccolo, Marialuisa,Sciarretta, Martina
, (2021/11/01)
Staphylococcus aureus is an important opportunistic pathogen that causes many infections in humans and animals. The inappropriate use of antibiotics has favored the diffusion of methicillin-resistant S. aureus (MRSA), nullifying the efforts undertaken in
KCNT1 INHIBITORS AND METHODS OF USE
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Paragraph 000680, (2020/11/23)
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
3-Aryl-1,2,4-oxadiazole Derivatives Active Against Human Rhinovirus
Kim, Jinwoo,Shin, Jin Soo,Ahn, Sunjoo,Han, Soo Bong,Jung, Young-Sik
supporting information, p. 667 - 672 (2018/05/14)
The human rhinovirus (hRV) is the causative agent of the common cold that often aggravates respiratory complications in patients with asthma or chronic obstructive pulmonary disease. The high rate of mutations and variety of serotypes are limiting the development of anti-hRV drugs, which emphasizes the need for the discovery of novel lead compounds. Previously, we identified antiviral compound 1 that we used here as the starting material for developing a novel compound series with high efficacy against hRV-A and -B. Improved metabolic stability was achieved by substituting an ester moiety with a 1,2,4-oxadiazole group. Specifically, compound 3k exhibited a high efficacy against hRV-B14, hRV-A21, and hRV-A71, with EC50 values of 66.0, 22.0, and 3.7 nM, respectively, and a relevant hepatic stability (59.6 and 40.7% compound remaining after 30 min in rat and human liver microsomes, respectively). An in vivo study demonstrated that 3k possessed a desirable pharmacokinetic profile with low systemic clearance (0.158 L·h-1·kg-1) and modest oral bioavailability (27.8%). Hence, 3k appears to be an interesting candidate for the development of antiviral lead compounds.
Dihydrobenzoxathiazepine compounds, a process for their preparation and pharmaceutical compositions containing them
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Page/Page column 3, (2012/04/04)
Compounds of formula (I): wherein R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphonylaminoalkyl or N-hydroxycarboximidamide group. Medicinal products containing the same which are useful as modulators of the A
PYRAZOLE OXADIAZOLE DERIVATIVES AS S1P1 AGONISTS
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Page/Page column 89, (2010/12/29)
The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases. Wherein R1, R2 and R3 are as defined in the description.
TRIAZOLE OXADIAZOLES DERIVATIVES
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Page/Page column 115, (2009/07/25)
The invention relates to compounds of formula (I), wherein R1, R2, Ra, Rb, X have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
NEW COMPOUNDS
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Page 141, (2010/02/06)
The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
Heterocyclic compounds
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, (2008/06/13)
The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention concerns Pyrrolo ?3,2-b! carbazoles, 1H-Benzofuro ?3,2-f! indoles and 1H-?1! Benzothieno ?2,3-f! indoles, methods for their preparation, pharmaceutical formulations containing them and their use as anti-tumour agents.
