33405-06-0Relevant academic research and scientific papers
Benzoic acid derivative as well as preparation method and medicinal application thereof
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Paragraph 0225; 0230-0232; 0266-0268, (2021/09/21)
The invention discloses a benzoic acid derivative as well as a preparation method and a pharmaceutical application thereof, and belongs to the technical field of medicines. The invention specifically discloses a benzoic acid derivative represented by a co
A straightforward TBHP-mediated synthesis of 2-amidobenzoic acids from 2-arylindoles and their antimicrobial activity
Patel, Om P.S.,Dhiman, Shiv,Khan, Shahid,Shinde, Vikki N.,Jaspal, Sonam,Srivathsa, Manu R.,Jha, Prabhat N.,Kumar, Anil
, p. 5962 - 5970 (2019/06/24)
A simple and highly efficient strategy has been developed for the synthesis of 2-amidobenzoic acids through the tert-butyl hydroperoxide (TBHP)-mediated oxygenation and sequential ring opening of 2-arylindoles in a one-pot fashion under metal-free aerobic conditions. The developed synthetic protocol is operationally simple, tolerates a wide range of functional groups, and is amenable to the gram-scale. Radical trapping experiments revealed that the reaction involves a radical pathway. The synthesized compounds (2a-s) were tested for in vitro antimicrobial activity. Among all screened compounds, 2d showed the maximum antibacterial activity against P. aerugunosa (ZOI = 17 mm, MIC = 32 μg mL-1) and compounds 2d and 2p showed the maximum (32 μg mL-1) antifungal activity against A. flavus and C. albicans.
The design and synthesis of novel orally active inhibitors of AP-1 and NF-κB mediated transcriptional activation. SAR of in vitro and in vivo studies
Palanki, Moorthy S. S.,Erdman, Paul E.,Ren, Minghuan,Suto, Mark,Bennett, Brydon L.,Manning, Anthony,Ransone, Lynn,Spooner, Cheryl,Desai, Sonal,Ow, Arnie,Totsuka, Ryuichi,Tsao, Peter,Toriumi, Wataru
, p. 4077 - 4080 (2007/10/03)
We have developed novel orally active quinazoline analogues as inhibitors of AP-1 and NF-κB mediated transcriptional activation. Among the derivatives prepared, 1-[2-(2-thienyl)quinazolin-4-ylamino]-3-methyl-3- pyrroline-2,5-dione (10) showed significant activity in an adjuvant-induced arthritis rat model by reducing the swelling by 65% in the non-injected foot. The synthesis, structure-activity relationship, and in vivo activity are described.
Synthesis of derivatives of thiophene using methyl 2-isothiocyanatobenzoate
Deck,Turner,Deck,Papadopoulos
, p. 343 - 347 (2007/10/03)
A variety of 2-substituted thiophenes is readily obtained from 2-(2-thienyl)-4H-3,1-benzothiazin-4-one (2), which is formed when thiophene reacts with methyl 2-isothiocyanatobenzoate (1) in the presence of anhydrous stannic chloride.
