1083282-65-8Relevant academic research and scientific papers
Synthesis and evaluation of 2,4,5-trisubstitutedthiazoles as carbonic anhydrase-III inhibitors
Al-Jaidi, Bilal A.,Al-dhoun, Mohammad A.,Bardaweel, Sanaa K.,Bataineh, Yazan A.,Dakkah, Abdel Naser,Deb, Pran Kishore,Khames Aga, Qutaiba Ahmed Al,Mailavaram, Raghuprasad,Nair, Anroop B.,Telfah, Soha Taher,Venugopala, Katharigatta N.,Ahmad Al-Subeihi, Ala’ Ali,Odetallah, Haifa’a Marouf
, p. 1483 - 1490 (2020/07/15)
A series of 17 compounds (12–16 b) with 2,4,5-trisubstitutedthiazole scaffold having 5-aryl group, 4-carboxylic acid/ester moiety, and 2-amino/amido/ureido functional groups were synthesised, characterised, and evaluated for their carbonic anhydrase (CA)-III inhibitory activities using the size exclusion Hummel–Dreyer method (HDM) of chromatography. Compound 12a with a free amino group at the 2-position, carboxylic acid moiety at the 4-position, and a phenyl ring at the 5-position of the scaffold was found to be the most potent CA-III inhibitor (Ki = 0.5 μM). The presence of a carboxylic acid group at the 4-position of the scaffold was found to be crucial for the CA-III inhibitory activity. Furthermore, replacement of the free amino group with an amide and urea group resulted in a significant reduction of activity (compounds 13c and 14c, Ki = 174.1 and 186.2 μM, respectively). Thus, compound 12a (2-amino-5-phenylthiazole-4-carboxylic acid) can be considered as the lead molecule for further modification and development of more potent CA-III inhibitors.
2-AZA-BICYCLO[3.3.0]OCTANE DERIVATIVES
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Page/Page column 12, (2011/02/15)
The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
1,2-DIAMIDO-ETHYLENE DERIVATIVES AS OREXIN ANTAGONISTS
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Page/Page column 25, (2011/11/06)
The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as medicaments, especially as orexin receptor antagonists.
PYRROLIDINES AND PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 11, (2010/08/08)
The invention relates to compounds of formula (I) wherein Y, A, N and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to the use of such compounds as medicaments, especially
2-CYCLOPROPYL-THIAZOLE DERIVATIVES
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Page/Page column 23, (2010/09/07)
The invention relates to selected 2-cyclopropyl-thiazole derivatives of the formula (I) wherein B, Y and R1 are as described in the description; to salts and especially pharmaceutically acceptable salts thereof, and to the use of such compounds use as med
2-AZA-BICYCLO[3.3.0]OCTANE DERIVATIVES
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Page/Page column 24, (2009/03/07)
The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
1,2-DIAMIDO-ETHYLENE DERIVATIVES
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Page/Page column 56-57, (2009/04/25)
The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) NHNR 3 OAOR 1 R 2 (I) wherein R1, R 2, R 3, and A are as described in the description and their use as medicaments, especially as orexin receptor
2-CYCLOPROPYL-THIAZOLE DERIVATIVES
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Page/Page column 47, (2009/01/20)
The invention relates to selected 2-cyclopropyl-thiazole derivatives of the formula (I) wherein B, Y and R1 are as described in the description; to salts and especially pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.
