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526-08-9

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The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition
In this study, a series of sulfonamide compounds was designed and synthesized through the systematic optimization of the antibacterial agent sulfaphenazole for the treatment of Mycobacterium tuberculosis (M. tuberculosis). Preliminary results indicate that the 4-aminobenzenesulfonamide moiety plays a key role in maintaining antimycobacterial activity. Compounds 10c, 10d, 10f and 10i through the optimization on phenyl ring at the R2 site on the pyrazole displayed promising antimycobacterial activity paired with low cytotoxicity. In particular, compound 10d displayed good activity (MIC = 5.69 μg/mL) with low inhibition of CYP 2C9 (IC50 > 10 μM), consequently low potential risk of drug-drug interaction. These promising results provide new insight into the combination regimen using sulfonamide as one component for the treatment of M. tuberculosis.
Chen, Hui,Wang, Bin,Li, Peng,Yan, Hong,Li, Gang,Huang, Haihong,Lu, Yu
(2021/03/26)

Process for formulating a synthetic drug for use in animal feed, and resulting formulation
A method of formulating a synthetic drug for use in animal feed, for the purpose of reducing carry-over of the synthetic drug to subsequent lots of animal feed in the feed mill.
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(2008/06/13)

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Chemical Properties

Melting Point: 179-183 °C
Boiling Point: 541.9°Cat760mmHg
Flash Point:281.5°C
Density: 1.39g/cm³
Solubility:Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
Storage Temp.:2-8°C
Vapor Pressure: 8.34E-12mmHg at 25°C
Refractive Index: 1.6440 (estimate)
PKA: pKa 5.71(H2O t = 25 I = 0.05) (Uncertain)
PSA: 98.39000
LogP: 3.99030

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