Day: October 31, 2022

On May 14, 2009, Bouillot, Anne Marie Jeanne; Laroze, Alain published a patent.Formula: C6H8N2O2S The title of the patent was Triazole derivatives as SCD inhibitors and their preparation, pharmaceutical compositions and use in the treatment of SCD-mediated diseases. And the patent contained the following:

The invention relates to substituted triazole compounds of the formula I: and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming AB42 peptide such as Alzheimer’s disease and the like. Compounds of formula I wherein X is CONH, NHCO and CH2NH; R1 is (un)substituted C6-10 aryl; R2 is H, C1-6 alkyl and C1-3 alkyl-O-C1-3 alkyl; R3 is (un)substituted C5-9 heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by 1-[(3,4-dichlorophenyl)methyl]-5-methyl-1H-1,2,3-triazole-4-carboxylic acid with 2-amino-6-methoxybenzothiazole. All the invention compounds were evaluated for their SCD inhibitory activity. Example compound II and several other example compounds exhibited pIC50 values of greater than 5.5. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Formula: C6H8N2O2S

The Article related to triazole preparation stearoyl coa desaturase inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Formula: C6H8N2O2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 31, 2022, Peplowski, Lukasz; Szczesny, Robert; Skowronski, Lukasz; Krupka, Anastasiia; Smokal, Vitaliy; Derkowska-Zielinska, Beata published an article.Application of 2010-06-2 The title of the article was Vibrational spectroscopy studies of methacrylic polymers containing heterocyclic azo dyes. And the article contained the following:

This paper presents the IR characterization of methacrylic polymers containing heterocyclic azo dyes thin films using FTIR and Raman spectroscopies. The observed FTIR vibrational frequencies were analyzed and compared with theor. predicted IR spectra. The hybrid-type exchange-correlation potential of Becke, Lee, Yang and Paar (B3LYP) method and 6-311++G(d,p) basis set was applied to calculate polymers spectra. The computed IR spectra showed appreciable agreement with the exptl. results. One can notice that the IR properties of azo dyes polymers strongly depend on the type of substitution in the azobenzene moiety. Different substitution pattern in azobenzene moiety leads to significant changes in the spectrum. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Application of 2010-06-2

The Article related to methacrylic polymer heterocyclic azo dye thin film vibrational spectroscopy, Dyes, Organic Pigments, Fluorescent Brighteners, and Photographic Sensitizers: Azo Dyes and Pigments and other aspects.Application of 2010-06-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On February 28, 2022, Daud, Saima; Abid, Obaid-ur-Rahman; Sardar, Asma; Shah, Basit Ali; Rafiq, Muhammad; Wadood, Abdul; Ghufran, Mehreen; Rehman, Wajid; Zain-ul-Wahab; Iftikhar, Fatima; Sultana, Rifhat; Daud, Habiba; Niaz, Basit published an article.Related Products of 2010-06-2 The title of the article was Design, synthesis, in vitro evaluation, and docking studies on ibuprofen derived 1,3,4-oxadiazole derivatives as dual α-glucosidase and urease inhibitors. And the article contained the following:

Present study aimed at the discovery of new non-sugar α-glucosidase inhibitors included synthesis of a series of 1,3,4-oxadiazole based Schiff base derivatives of ibuprofen. Initially oxadiazoles from ibuprofen were synthesized by treating ibuprofen hydrazide with carbon disulfide. Oxadiazoles upon treatment with different substituted phenacyl bromides gave acylated 1,3,4-oxadizole derivatives I [R1 = 2-MeC6H4, 3-MeC6H4, 4-MeC6H4, 4-PhC6H4, 2-O2NC6H4] which further react with amines to gave 1,3,4-oxadiazole based Schiff base derivatives of ibuprofen II [R1 = 2-MeC6H4, 3-MeC6H4, 4-MeC6H4, 4-PhC6H4, 2-O2NC6H4; R2 = Ph, 2-MeC6H4, 2-(4-Ph)thiazolyl]. Synthesized ibuprofen derivatives were characterized by 1H NMR, 13C NMR and HRMS (EI). These derivatives were evaluated in vitro for their α-glucosidase and urease inhibitory activity. In case of α-glucosidase enzyme, all the synthesized derivatives showed potent inhibition in comparison to standard acarbose and the most potent amongst these was the compoundsII [R1 = 4-PhC6H4, R2 = 2-(4-Ph)thiazolyl; R1 = 3-H3CC6H4, R2 = Ph] having IC50 value 16.01 ± 1.27μM and 39.06 ± 0.27μM, resp. In case of urease enzyme, the synthesized derivatives showed varying degree of inhibitory potential, however, potent inhibition was shown by I [R1 = 2-O2NC6H4] (IC50 = 9.36 ± 1.02μM), I [R1 = 4-MeC6H4] (IC50 = 17.65 ± 1.03μM), II [R1 = 4-PhC6H4, R2 = 2-(4-Ph)thiazolyl] (IC50 = 18.29 ± 1.26μM), I [R1 = 2-MeC6H4] (IC50 = 19.52 ± 1.25μM) and II [R1 = 4-PhC6H4, R2 = 2-H3CC6H4] (IC50 = 19.63 ± 1.08μM). The mol. docking was performed in order to check binding interactions between the synthesized derivatives and the enzymes. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Related Products of 2010-06-2

The Article related to oxadiazole schiff base preparation alpha glucosidase inhibitor urease docking, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Related Products of 2010-06-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 22, 2014, Lemieux, Rene M.; Popovici-Muller, Janeta; Salituro, Francesco G.; Saunders, Jeffrey O.; Travins, Jeremy; Chen, Yongsheng published a patent.Electric Literature of 64987-16-2 The title of the patent was Preparation of substituted bisthiadiazoles as glutaminase inhibitors. And the patent contained the following:

The invention relates to compounds of formula I as glutaminase inhibitors; their preparation and use in the treatment of cancer. Compounds of formula I wherein X is C3-7 cycloalkylene; each W, Y and Z is independently S, CH, O, N, etc.; A is (CH2)0-2; each R1 and R2 are independently NH2, NR3COR4, CONR3R4, etc.; R3 is H, C1-6 alkyl and aryl; R4 is C1-6 alkyl, aryl, heteroaryl, etc.; each R6 is H, F, OH, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their glutamase inhibitory activity. From the assay, it was determined that example compound II exhibited IC50 value of < 100 nM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Electric Literature of 64987-16-2

The Article related to substituted bisthiadiazole preparation glutaminase inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 15, 2008, Yang, Bingwei Vera; Doweyko, Lidia M.; Vaccaro, Wayne; Huynh, Tram N.; Tortolani, David R.; Dhar, T.g. Murali published a patent.Name: 2-Amino-4-(4-iodophenyl)thiazole The title of the patent was N-Heteroaryl carboxamides as modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula I an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds Compounds of formula I wherein M is (un)substituted alkyl, cycloalkyl, (hetero)aryl and heterocyclyl; Ma and Za are independently a bond and C1-3 alkylene; Q is H, (un)substituted C1-4 alkyl; Q and R6 taken together to form a 3- to 6-membered cycloalkyl; Q and M taken together to form a 3- to 7-membered heterocyclic ring; Z is cycloalkyl, heterocyclyl and (hetero)aryl; R1 – R4 are independently H, halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, NO2, CN, OH and derivatives, etc.; R6 is (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, CHO, acyl, CO2H and derivatives, etc.; R7 is halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, NO2, CN, OH and derivatives, etc.; R22 is H, (un)substituted alkyl, CO-alkyl, CO2-alkyl, SO2-alkyl, alkoxy, (un)substituted amino, (hetero)aryl, heterocyclyl, and cycloalkyl; and their enantiomers, diastereoisomers, and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 2,2-diphenyl-1-methylcyclopropane-1-carboxylic acid with 2-aminothiazole. All the invention compounds were evaluated for their GR and AP-1 modulatory activity. From the assay, it was determined that compound II exhibited Ki value of 103.8 % RBA. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).Name: 2-Amino-4-(4-iodophenyl)thiazole

The Article related to heteroaryl carboxamide preparation glucocorticoid receptor ap1 nfkb modulator, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Name: 2-Amino-4-(4-iodophenyl)thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Chopra, Rakesh; Singh, Lovepreet; Chibale, Kelly; Singh, Kamaljit published an article in 2019, the title of the article was Synthesis, In Silico Molecular Docking, ADME Evaluation and In Vitro Antiplasmodial Activity of Pyrimidine-Based Hybrid Molecules.Category: thiazole And the article contains the following content:

Synthesis of new pyrimidine based mol. hybrids comprising of pyrimidine and aryl/heteroaryl groups linked, conveniently through 1,2,3-triazole. In vitro antiplasdmodial activity of this series of compounds against chloroquine sensitive NF54 strain of the human malaria parasite Plasmodium falciparum, revealed interesting trends and correlation with the physicochem. properties of the hybrids. In silico docking of the most active (IC50 4.40±1.00 μM) (more active than reference artesunate) member 16a in the active binding sites of wild type PfDHFR-TS (P. falciparum Dihydrofolate Reductase-Thymidylate Synthase) and PfDHFR-TS Quadruple mutant showed interactions suggesting their role as PfDHFR inhibitors. Further, all the members of the series showed favorable in silico ADME (Adsorption Distribution, Metabolism, Excretion) profile. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Category: thiazole

The Article related to pyrimidine based hybrid triazoles preparation mol docking antiplasmodial human, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica