219929-43-8Relevant academic research and scientific papers
Synthesis, cyclooxygenase inhibition, and anti-inflammatory evaluation of novel diarylheterocycles with a central pyrazole, pyrazoline, or pyridine ring
Abdellatif, Khaled R. A.,Abdelall, Eman K. A.,Fadaly, Wael A. A.,Kamel, Gehan M.
, p. 2632 - 2644 (2015)
Five groups of diarylheterocycles with a central pyrazole ring (12a-d), pyrazoline ring (14a-d), or pyridine ring (15a-d, 16a-d and 17a-d) were synthesized and evaluated in vitro for COX-1/COX-2 inhibitory activity and in vivo for anti-inflammatory activity. All compounds that possessed anti-inflammatory activity were assessed for their ulcerogenic liability in comparison with ibuprofen and celecoxib. The pyrazole derivative 12b and the pyrazoline derivative 14b were the least ulcerogenic compounds with relative ulcerogenicities to celecoxib 0.85 and 0.90 respectively. (Chemical Equation Presented)
A CONTINUOUS FLOW MICRO-TOTAL PROCESS SYSTEM FOR PREPARATION OF CELECOXIB AND ANALOGS THEREOF
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Page/Page column 16-17; 23-24, (2020/08/22)
The present invention relates to preparation of pyrazoles. This invention further relates to a continuous flow micro-total process system for preparation of celecoxib, a COX-2 selective non-steroidal anti-inflammatory drug, and analogs thereof.
An Integrated Continuous Flow Micro-Total Ultrafast Process System (μ-TUFPS) for the Synthesis of Celecoxib and Other Cyclooxygenase Inhibitors
Sthalam, Vinay Kumar,Singh, Ajay K.,Pabbaraja, Srihari
supporting information, p. 1892 - 1899 (2019/10/11)
Integrated continuous manufacturing has emerged as a promising device for the rapid manufacturing of active pharmaceutical ingredients (APIs). We herein report a newly designed continuous flow micro-total process system platform for the rapid manufacturing of celecoxib, a selective nonsteroidal anti-inflammatory drug. This approach has been proven generally for the synthesis of several alkyl and aryl substituted pyrazoles. In order to minimize the tedious work-up process of potential reaction intermediates/products, we have developed a continuous flow extraction and separation platform to carry out the entire reaction sequence resulting in a short residence time with good yield. The present process was further extended to gram-scale synthesis of the COX-2-related API, viz. celecoxib, in the continuous flow process.
Synthesis of 1-p-sulfamylphenyl-3 trifluoromethylpyrazoles class of cyclooxygenase-2 inhibitors
Asiri, Abdullah M.,Faidallah, Hassan M.,Albar, Hassan M.,Sharshira
, p. 483 - 488 (2007/10/03)
Condensation of p-sulfamylphenylhydrazine with diketones 1. afforded pyrazoles 2. Reaction of 2 with isocyanate and isothiocyanate derivatives gave the corresponding ureas 3 and thioureas 4 respectively. Cyclization of the thioureido group of compounds 4 by treating with ethyl bromoacetate, ethyl β-bromopropionate and α-bromoacetophenone afforded the corresponding thiazolidinone, thiazinone and thiazoline derivatives 5, 6 and 7 respectively.
Compounds and methods for inducing apoptosis in proliferating cells
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Page 18, (2008/06/13)
Compounds useful for inducing apoptosis in proliferative cells, particularly cancer cells, including but not limited to prostate cancer, leukemia, non-smalll cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, bladder cancer, lymphoma, and breast cancer. These compounds are particularly useful in the treatment of androgen-independent cancers, including hormone-refractory prostate cancer. Further provided are methods of treating cancer in a subject in need of such treatment using the compounds of the present invention. Further provided are methods for using the compounds of the present invention to treat, inhibit, or delay the onset of cancer in a subject. Further provided are methods of inducing apoptosis in rapidly proliferating cells, particularly, though not necessarily cancer cells, using the compounds of the present invention.
Substituted pyrazolyl benzenesulfonamide for the treatment of inflammation
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, (2008/06/13)
A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: STR1
SUBSTITUTED PYRAZOLYL BENZENESULFONAMIDES
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, (2008/06/13)
A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: or a pharmaceutically-acceptable salt thereof
