80625-18-9Relevant academic research and scientific papers
Competition of the Hantzsch and Boese reactions in the interaction of 1-thiocarbamoylthiosemicarbazide and phenylchloropyruvic acid methyl ester
Mamedov,Nurkhametova,Gubaidullin,Litvinov,Levin
, p. 1357 - 1363 (1999)
1-Thiocarbamoylthiosemicarbazide, the synthetic equivalent of thiourea and thiosemicarbazide, reacts with phenylchloropyruvic acid methyl ester exclusively as thiourea (Hantzsch reaction) forming 2-hydrazo-4-methoxycarbonyl-5-phenylthiazole. Diacetylation
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.
SUBSTITUTED 2-AZABICYCLO[3.1.1]HEPTANE AND 2-AZABICYCLO[3.2.1]OCTANE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 98; 99, (2019/03/17)
There is provided a compound of formula (I), wherein L1 to L3, R1 to R4, X, A and B have meanings given in the description, and pharmaceutically acceptable salts, solvates and prodrugs thereof, which compounds are useful as antagonists of the orexin-1 and orexin-2 receptors or as selective antagonists of the orexin-1 receptor, and thus, in particular, in the treatment or prevention of inter alia substance dependence, addiction, anxiety disorders, panic disorders, binge eating, compulsive disorders, impulse control disorders, cognitive impairment and Alzheimer's disease.
INHIBITORS OF HEAT SHOCK FACTORS AND USES THEREOF
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, (2018/04/13)
The present disclosure relates to a class of mammalian heat shock factor (HSF) inhibitors, to pharmaceutical compositions comprising these inhibitors as well as to methods for using the inhibitors. The inhibitors inhibit stress-induced expression from heat shock gene promoters. Furthermore, the inhibitors are cytotoxic to a variety of human cancer cells types.
Novel Thiazole Carboxylic Acid derivatives possessing a "zinc Binding Feature" as Potential human glyoxalase-I inhibitors
Al-Balas, Qosay A.,Hassan, Mohammad A.,Jabal, Ghazi A. Al,Al-Shari, Nizar A.,Almaaytah, Ammar M.,El-Elimat, Tamam
, p. 1124 - 1134 (2017/11/14)
Glyoxalase-I (Glo-I) enzyme is an attractive new target for developing new cancer therapeutics. This enzyme is a dimeric mononuclear zinc coordinating metalloenzyme, and the core zinc ion was utilized in designing potentially active inhibitors possessing
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.
3-AZA-BICYCLO[3.3.0]OCTANE COMPOUNDS
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Page/Page column 38, (2009/03/07)
The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.
TRANS-3-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES
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Page/Page column 58, (2009/03/07)
The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n 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-AZA-BICYCLO[2.2.1]HEPTANE DERIVATIVES
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Page/Page column 45-46, (2009/10/18)
The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as m
