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The present invention relates to an oxidatively curable coating formulation comprising an oxidatively curable alkyd-based resin and a bispidon-based chelant, which chelant may optionally be complexed with a suitable transition metal ion. The formulations may be paints or other oxidatively curable coating compositions. The invention also provides methods for making such formulations and compositions resultant from the curing of such formulations.

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Reference:
Thiazole | C3H9262NS – PubChem,
Thiazole | chemical compound | Britannica

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Provided herein are compounds of formula I: wherein A, B, X, R1 , R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions

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Reference:
Thiazole | C3H9304NS – PubChem,
Thiazole | chemical compound | Britannica

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The reactions of hydrazones, derived from various aromatic aldehydes bound to Rink resin and hydrazines, with trimethylsilanolate have been studied. In this process, the aldehydes were oxidized to the corresponding carboxylic acids. The reaction was also tested with success in solution, with various aromatic aldehydes easily being oxidized in one pot via hydrazone formation and trimethylsilanolate treatment. A mechanism for the hydrazone cleavage is proposed. The reaction may be used as an alternative method for aldehyde oxidation with the selectivity complementary to that of currently used reactions.

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Reference:
Thiazole | C3H9258NS – PubChem,
Thiazole | chemical compound | Britannica

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2-Arylidene Hydrazinecarbodithioates as Potent, Selective Inhibitors of Cystathionine gamma-Lyase (CSE)

Hydrogen sulfide is produced from l-cysteine by the action of both cystathionine gamma-lyase (CSE) and cystathionine beta-synthase (CBS) and increasingly has been found to play a profound regulatory role in a range of physiological processes. Mounting evidence suggests that upregulation of hydrogen sulfide biosynthesis occurs in several disease states, including rheumatoid arthritis, hypertension, ischemic injury, and sleep-disordered breathing. In addition to being critical tools in our understanding of hydrogen sulfide biology, inhibitors of CSE hold therapeutic potential for the treatment of diseases in which increased levels of this gasotransmitter play a role. We describe the discovery and development of a novel series of potent CSE inhibitors that show increased activity over the benchmark inhibitor and, importantly, display high selectivity for CSE versus CBS.

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Reference:
Thiazole | C3H9319NS – PubChem,
Thiazole | chemical compound | Britannica

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Selective Functionalization of 2-Nitro-p-phenylenediamine : Part III – A New Route to 1-Arylbenzimidazole 5-carbamates, Including Cambendazole

Reaction of 3,4-diaminophenylcarbamic acid ethyl ester (2) with carboxymethyl dithiobenzoate (3) gives the thiobenzanilides (4a or 4b), which could be cyclized by acid to 2-phenylbenzimidazole-5-carbamic acid ethyl ester (5).The same product is obtained by the reaction of 2 with benzaldehyde and sulphur.Other aromatic aldehydes have been similarly reacted to give (9b-d).Cambendazole (9e) is obtained by the reaction of thiazole-4-aldehyde and sulphur with 3,4-diaminophenylcarbamic acid isopropyl ester (6e).

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Reference:
Thiazole | C3H9303NS – PubChem,
Thiazole | chemical compound | Britannica

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Synthesis and biological evaluation of thiabendazole derivatives as anti-angiogenesis and vascular disrupting agents

Abstract Thiabendazole, already approved by FDA for oral use as an anti-fungal and anti-helminthic drug since 1967, has recently been repurposed as a vascular disrupting agent. By optimization of the structure of the lead compound, we successfully identified compound TBZ-19 and the new derivative is over 100-fold more potent than the lead compound against the growth of four different cell lines (A549, HCT-116, HepG2 and HUVECs). The most potent two candidates TBZ-07 and TBZ-19, exhibiting moderate inhibitory cell proliferation activity, were also verified as anti-angiogenesis and vascular disrupting agents. Therefore, TBZ-07 and TBZ-19 would be promising candidates with vasculature targeting activity and merit further development.

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Reference:
Thiazole | C3H9344NS – PubChem,
Thiazole | chemical compound | Britannica

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Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists

CC-chemokine receptor 5 (CCR5) is an attractive target for preventing the entry of human immunodeficiency virus 1 (HIV-1) into human host cells. Maraviroc is the only CCR5 antagonist, and it was marketed in 2007. To overcome the shortcomings of maraviroc, structure-based drug design was performed to minimize CYP450 inhibition and to enhance anti-HIV potency and bioavailability. Thirty-four novel 1-heteroaryl-1,3-propanediamine derivatives (1-34) were synthesized, displaying CCR5-antagonist activities in the 2.3-296.4 nM range. Among these, compounds 21 and 34 were the most potent CCR5 antagonists, with excellent in vitro anti-HIV-1 activity, low cytotoxicity, and an acceptable pharmacokinetic profile. Furthermore, the X-ray crystal structures of compounds 21 and 34 bound to CCR5 were determined at 2.8 A resolution. Compound 34 exhibited no CYP450-inhibition activity at 25 muM, which overcomes the potential drug-drug interaction of maraviroc. Compound 34 represents a promising drug candidate for HIV-infection treatment.

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Reference:
Thiazole | C3H9336NS – PubChem,
Thiazole | chemical compound | Britannica

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The compounds are 2-alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides, for example 2-methoxy-N-methyl-3-morpholino-2-(2-pyridyl)thiopropanamide, which are inhibitors of gastric acid secretion.

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Thiazole | C3H9290NS – PubChem,
Thiazole | chemical compound | Britannica

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Optimization of KDM6B (JMJD3) HTS hit 12 led to the identification of 3-((furan-2-ylmethyl)amino)pyridine-4-carboxylic acid 34 and 3-(((3-methylthiophen-2-yl)methyl)amino)pyridine-4-carboxylic acid 39 that are inhibitors of the KDM4 (JMJD2) family of histone lysine demethylases. Compounds 34 and 39 possess activity, IC50 ? 100 nM, in KDM4 family biochemical (RFMS) assays with ?50-fold selectivity against KDM6B and activity in a mechanistic KDM4C cell imaging assay (IC50 = 6-8 muM). Compounds 34 and 39 are also potent inhibitors of KDM5C (JARID1C) (RFMS IC50 = 100-125 nM).

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Reference:
Thiazole | C3H9308NS – PubChem,
Thiazole | chemical compound | Britannica

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COMPOUNDS FOR MODULATING DDAH AND ADMA LEVELS, AS WELL AS METHODS OF USING THEREOF TO TREAT DISEASE

Disclosed are compounds that can modulate DDAH and the amount of asymmetric dimethylarginine (ADMA) in a subject. Also provided are pharmaceutical compositions comprising these compounds, as well as methods of using these compositions to treat and/or prevent diseases associated with elevated or low levels of DDAH and ADMA.

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Reference:
Thiazole | C3H9327NS – PubChem,
Thiazole | chemical compound | Britannica