09/28/21 News Final Thoughts on Chemistry for 4-(Trifluoromethyl)thiazol-2-amine

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4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

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Reference:
Thiazole | C3H4943NS – PubChem,
Thiazole | chemical compound | Britannica

28-Sep News Some scientific research about 4-(Trifluoromethyl)thiazol-2-amine

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The activation of the NF-kappaB transcription factor is a major adaptive response induced upon treatment with EGFR kinase inhibitors, leading to the emergence of resistance in nonsmall cell lung cancer and other tumor types. To suppress this survival mechanism, we developed new thiourea quinazoline derivatives that are dual inhibitors of both EGFR kinase and the NF-kappaB activity. Optimization of the hit compound, identified in a NF-kappaB reporter gene assay, led to compound 9b, exhibiting a cellular IC50 for NF-kappaB inhibition of 0.3 muM while retaining a potent EGFR kinase inhibition (IC50 = 60 nM). The dual inhibitors showed a higher potency than gefitinib to inhibit cell growth of EGFR-overexpressing tumor cell lines in vitro and in a xenograft model in vivo, while no signs of toxicity were observed. An investigation of the molecular mechanism of NF-kappaB suppression revealed that the dual inhibitors depleted the transcriptional coactivator CREB-binding protein from the NF-kappaB complex in the nucleus.

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Reference:
Thiazole | C3H4913NS – PubChem,
Thiazole | chemical compound | Britannica

10/9/2021 News Properties and Exciting Facts About 4-(Trifluoromethyl)thiazol-2-amine

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This invention relates to azabicyclo[4.1.0]hept-4-yl derivatives and their use as pharmaceuticals.

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Reference:
Thiazole | C3H4894NS – PubChem,
Thiazole | chemical compound | Britannica

Brief introduction of 4-(Trifluoromethyl)thiazol-2-amine

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The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.

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Reference:
Thiazole | C3H4903NS – PubChem,
Thiazole | chemical compound | Britannica

Can You Really Do Chemisty Experiments About 4-(Trifluoromethyl)thiazol-2-amine

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We report herein a synthetic protocol for the preparation of 1,3-dibromo-1,1-difluoro-2-propanone, a new synthon used for the first time in a reaction with aromatic amines and sodium thiocyanate, leading to thiazoles which are useful candidates in drug discovery programs. The new synthon allows to introduce a bromodifluoromethyl group at the C4 of the thiazole, and it is amenable of further transformation such as the Br/F exchange useful in radiopharmaceutics. Application of the strategy to the preparation of a precursor of the biologically relevant DF2755Y is also reported.

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Reference:
Thiazole | C3H4892NS – PubChem,
Thiazole | chemical compound | Britannica

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The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3

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Reference:
Thiazole | C3H4904NS – PubChem,
Thiazole | chemical compound | Britannica

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Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor for which only short-chain fatty acids (SCFAs) have been reported as endogenous ligands. We describe the discovery and optimization of phenylacetamides as allosteric agonists of FFA2. These novel ligands can suppress adipocyte lipolysis in vitro and reduce plasma FFA levels in vivo, suggesting that these allosteric modulators can serve as pharmacological tools for exploring the potential function of FFA2 in various disease conditions.

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Reference:
Thiazole | C3H4923NS – PubChem,
Thiazole | chemical compound | Britannica

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An efficient C-H heteroarylation of heteroarenes is achieved through visible-light photoredox-catalyzed diazotization of heteroarylamines in situ by tBuONO at room temperature. A library of functionalized biheteroaryls is obtained by using this protocol. The reaction avoids the use of transition-metal catalysts, additives, and acidic reaction medium.

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Reference:
Thiazole | C3H4932NS – PubChem,
Thiazole | chemical compound | Britannica

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A series of alkyl thiazole-2-carboxylates containing a range of substituents at the 4- and 5-positions has been prepared.Solutions of these esters (mostly new compounds) show well resolved doublets in the i.r.C=O region which arise from rotational isomers.The higher wavenumber components are assigned to the more polar carbonyl O,S-anti-s-trans-rotamers and the lower wavenumber components to the carbonyl O,S-syn-s-trans-forms.Small, but systematic, differences between the methyl esters are noted.

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Reference:
Thiazole | C3H4935NS – PubChem,
Thiazole | chemical compound | Britannica

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Treatment of 2-trifluoroacetamido-4-(trifluoromethyl)thiazole with two equivalents of n-butyllithium at -78 deg C produced the thiazole dianion 5 in situ, which reacted preferentially at the 5-position with a variety of electrophiles.These electrophiles include: an aldehyde, ketone, chloroformate, acid chloride, phosphorus oxychloride, silicon chloride, and disulfide.Dianion 5 also combined with dibromodifluoromethane at -98 deg C to give the corresponding 5-(bromodifluoromethyl)thiazole 7, which is an unusual reaction for an aromatic or heteroaromatic system.Compound 7 was converted to a 4,5-bis-(trifluoromethyl)thiazole 8 using tetrabutylammonium fluoride.

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Reference:
Thiazole | C3H4893NS – PubChem,
Thiazole | chemical compound | Britannica