67639-58-1Relevant academic research and scientific papers
Synthesis and anti-methicillin-resistant Staphylococcus aureus activity of 5,7-dibromo-2-benzoylbenzofurans alone and in combination with antibiotics
Phan, Phuong-Thuy T.,Nguyen, Hong-Nhung T.,Kim, Son N.,Pham, Tuan-Anh N.
supporting information, p. 786 - 796 (2020/12/09)
A series of 5,7-dibromo-2-benzoylbenzofurans were synthesized by the Rap–Stoermer condensation of 5,7-dibromosalicylaldehyde with diverse phenacyl bromides and evaluated for in-vitro antibacterial activities against methicillin-sensitive Staphylococcus aureus (MSSA) ATCC 29213, methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300, and MRSA ATCC 33591 by agar dilution method. The synergistic effects were determined by using the agar dilution checkerboard assay. The derivatives bearing carboxylic acid functional groups exhibited reasonable activity against MRSA strains with the best MIC = 32 μg/mL (9b, 9d). Moreover, the additive or synergistic interactions against MRSA strains was observed in six combinations (1b + cefuroxime/gentamicin, 1c + ciprofloxacin/gentamicin, 9b + gentamicin, and 9c + ciprofloxacin) with the fractional inhibitory concentration index (FICI) values in the range of 0.375–1.0. Significantly, the MICs of these antibiotics were reduced 2–4-fold. The results of the MTT assay illustrated the low mammalian cell cytotoxicity of these potent compounds.
ROR-GAMMA INHIBITORS
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Page/Page column 288-289, (2019/04/26)
The present invention relates to compounds of formula I and pharmaceutical compositions comprising compounds of formula I. Compounds of Formula I are useful in treatment of inflammatory, metabolic or autoimmune diseases which are mediated by RORy.
2-Amino-4-arylthiazoles through One-Pot Transformation of Alkylarenes with NBS and Thioureas
Shibasaki, Kaho,Togo, Hideo
, p. 2520 - 2527 (2019/04/04)
Treatment of alkylarenes with N-bromosuccinimide in a mixture of ethyl acetate and water at 60 °C, a mixture of acetonitrile and water at 80 °C, or a mixture of diethyl carbonate and water under irradiation with a tungsten lamp, followed by a reaction with thioureas or arenethioamides provided the corresponding 2-amino- 4-arylthiazoles or 2,4-diarylthiazoles in good to moderate yields, respectively, in one pot. The present reaction is an efficient one-pot transformation method of alkylarenes into 2-amino-4-arylthiazoles and 2,4-diarylthiazoles directly under mild and transition-metal-free conditions.
A one-pot hypoiodite catalysed oxidative cycloetherification approach to benzoxazoles
Boominathan, Siva Senthil Kumar,Hu, Wan-Ping,Senadi, Gopal Chandru,Vandavasi, Jaya Kishore,Wang, Jeh-Jeng
supporting information, p. 6726 - 6728 (2014/06/23)
A practical one-pot hypoiodite catalysed oxidative cyclization approach to synthesize α-ketobenzoxazole derivatives was successfully developed. This operationally simple protocol utilizes easily-accessible starting materials and has a broad substrate scope with excellent yields. This journal is the Partner Organisations 2014.
Hepatitis C Virus Inhibitors
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Page/Page column 160, (2008/06/13)
The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
Model studies towards the synthesis of gilvocarcin M
Cordera-Vargas, Alejandro,Quiclet-Sire, Beatrice,Zard, Samir Z.
, p. 4432 - 4443 (2007/10/03)
In model studies towards the synthesis of gilvocarcin M, a convergent, xanthate-based free-radical strategy was tested in order to construct the key aromatic ring attached to the sugar unit. The Royal Society of Chemistry 2005.
Synthesis, in vitro binding profile, and central nervous system penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazol e
Rosen,Seeger,McLean,Nagel,Ives,Guarino,Bryce,Furman,Roth,Chalabi,Windels
, p. 3020 - 3023 (2007/10/02)
4-(2-Methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole (5) is a highly potent member of a structurally novel series of selective serotonin-3 receptor antagonists. The synthesis of tritriated 5 and its binding profile in neuroblastoma-glioma 108
