220641-69-0Relevant academic research and scientific papers
METHOD FOR THE SYNTHESIS OF BENZAZOLE
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Paragraph 0045, (2017/09/19)
PROBLEM TO BE SOLVED: To obtain a benzazole in a short reaction time with high yields. SOLUTION: A method for the synthesis of a benzazole includes a chemical reaction represented by the chemical reaction formula (1) to occur in subcritical water or supercritical water (X is NR6, O, or S. Y is H, OR7, halogen, or NR8R9. R1 to R9 are a C1-C20 aliphatic or aromatic substituent which may have O, N, S, B, Si, halogen, or P (two or more substituents of R1 to R6 may be coupled together, R8 and R9 may be coupled together, and two or more substituents of R1 to R9 may be the same) or H). SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis
Patrick, Donald A.,Gillespie, J. Robert,McQueen, Joshua,Hulverson, Matthew A.,Ranade, Ranae M.,Creason, Sharon A.,Herbst, Zackary M.,Gelb, Michael H.,Buckner, Frederick S.,Tidwell, Richard R.
supporting information, p. 957 - 971 (2017/02/19)
A previous publication from this lab (Patrick, et al. Bioorg. Med. Chem. 2016, 24, 2451-2465) explored the antitrypanosomal activities of novel derivatives of 2-(2-benzamido)ethyl-4-phenylthiazole (1), which had been identified as a hit against Trypanosoma brucei, the causative agent of human African trypanosomiasis. While a number of these compounds, particularly the urea analogues, were quite potent, these molecules as a whole exhibited poor metabolic stability. The present work describes the synthesis of 65 new analogues arising from medicinal chemistry optimization at different sites on the molecule. The most promising compounds were the urea derivatives of 2-aryl-benzothiazol-5-amines. One such analogue, (S)-2-(3,4-difluorophenyl)-5-(3-fluoro-N-pyrrolidylamido)benzothiazole (57) was chosen for in vivo efficacy studies based upon in vitro activity, metabolic stability, and brain penetration. This compound attained 5/5 cures in murine models of both early and late stage human African trypanosomiasis, representing a new lead for the development of drugs to combat this neglected disease.
COMPOUNDS FOR TREATMENT OF TRYPANOSOMES AND NEUROLOGICAL PATHOGENS AND USES THEREOF
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Paragraph 0190, (2017/09/24)
The present invention relates to novel compounds that cross the blood-brain barrier and are effective inhibitors of neurological pathogens such as trypanosomes. The invention further relates to the use of these compounds for treating disorders related to trypanosomes and neurological pathogens.
