Category: thiazole

Liu, Gui-Chun; Dong, Zhi-Wei; Hou, Qing-Bai; He, Jin-Wu; Zhao, Ruo-Ping; Wang, Wen; Li, Xue-Yan published the artcile< Second Rhagophthalmid Luciferase Cloned from Chinese Glow-worm Menghuoius giganteus (Rhagophthalmidae: Elateroidea)>, Quality Control of 2591-17-5, the main research area is sequence luciferase mol cloning Rhagophthalmus Menghuoius.

The pH-insensitive beetle luciferases cloned from Rhagophthalmidae, Phengodidae, and Elateridae exhibit great potential application as reporter assays for monitoring gene expression. At present, however, only one luciferase has been reported from the enigmatic and predominantly Asian distributed luminous family Rhagophthalmidae. Here, we cloned the second rhagophthalmid luciferase from the Chinese glow-worm Menghuoius giganteus (Rhagophthalmidae: Elateroidea) by combining reverse transcription polymerase chain reaction (RT-PCR) with rapid amplification of complementary DNA ends (RACE). The luciferase consisted of 546 amino acids and showed high identity to that of Rhagophthalmus ohbai (90.4%). The recombinant M. giganteus luciferase was produced in vitro and exhibited significant bioluminescent activity under neutral conditions (pH 7.8), with low KM for D-luciferin (2.2μM) and ATP (53μM). Activity was highest at 10°C and inactivation occurred at 45°C. This luciferase showed pH-insensitivity and maximum emission spectrum at 560 nm. Phylogenetic analyses based on the deduced amino acids indicated a close relationship between the M. giganteus luciferase and that of R. ohbai. These results increase our understanding of rhagophthalmid luciferases and provide a new resource for the application of luciferases.

Photochemistry and Photobiologypublished new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Quality Control of 2591-17-5.

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

Pena, S.; Fagundez, C.; Medeiros, A.; Comini, M.; Scarone, L.; Sellanes, D.; Manta, E.; Tulla-Puche, J.; Albericio, F.; Stewart, L.; Yardley, V.; Serra, G. published the artcile< Synthesis of cyclohexapeptides as antimalarial and anti-trypanosomal agents>, Formula: C12H18N2O4S, the main research area is cyclohexa peptide synthesis antimalarial antitrypanosomal agent structure activity; solid phase peptide synthesis macrocyclization.

Cyclohexapeptide analogs of natural products were obtained in very good yields by a combination of solid-phase peptide synthesis, for the linear peptide, and solution cyclization. The activities against Plasmodium falciparum K1, Trypanosoma brucei brucei and murine macrophages (cell line J774) of these novel compounds and azolic macrocycles, previously reported by us, were evaluated. Seven macrocycles showed submicromolar activities against Plasmodium falciparum K1 and a high selectivity (SI > 125) for the parasite. In addition, two compounds displayed one digit micromolar EC50 against T. brucei brucei and satisfactory selectivity (SI 82 and 95). Preliminary structure-activity relationships are presented.

MedChemCommpublished new progress about Antimalarials. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Formula: C12H18N2O4S.

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

Lu, Cuifen; Nie, Junqi; Yang, Guichun; Chen, Zuxing published the artcile< An improved synthesis of sitophilure>, SDS of cas: 171877-39-7, the main research area is asym synthesis sitophilure aldol reaction chiral auxiliary.

The asym. synthesis of sitophilure (I) was carried out in 8 steps, with 42% overall yield and 97% enantiomeric excess from propionaldehyde. The synthesis relied on an approach employing an asym. acyl-thiazolidinethione propionate aldol reaction to establish two stereogenic centers.

Canadian Journal of Chemistrypublished new progress about Aldol condensation, stereoselective. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, SDS of cas: 171877-39-7.

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

Aryanasab, F.; Shokri, A.; Saidi, M. R. published the artcile< A simple approach to the synthesis of 3-substituted rhodanines and thiazolidine-2,4-diones>, Quality Control of 10574-69-3, the main research area is rhodanine thiazolidinedione preparation green chem; primary amine carbon disulfide bromoacetate three component reaction.

The green synthesis of 3-substituted rhodanine and thiazolidine-2,4-dione derivs . I [R = C6H5CH2, (CH2)3CH3, C6H5, 4-ClC6H4, etc.; X = S, O] via one-pot three-component reaction of primary amines RNH2, carbon disulfide and methyl-2-bromoacetate in water or under solvent-free conditions is described.

Scientia Iranica, Transaction C: Chemistry, Chemical Engineeringpublished new progress about Green chemistry. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Quality Control of 10574-69-3.

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

Al-Shamkhani, Zeki A. Naser; Al-Hazam, Hanan A. published the artcile< Microwave Assisted Synthesis, Characterizations and Antibacterial Activity of Some of Thiazole Derivatives>, Computed Properties of 57493-24-0, the main research area is thiazole amino preparation antibacterial microwave.

A series of substituted 2-amino thiazole compounds I (R = H, 4-OH, 2-F, etc.) were synthesized by reaction of substituted acetophenone with thiourea and iodine in microwave oven. The biol. screening data of the synthesized compounds I were also studied.

Research Journal of Pharmaceutical, Biological and Chemical Sciencespublished new progress about Antibacterial agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Computed Properties of 57493-24-0.

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

Zhu, Yan-Ping; Yuan, Jing-Jing; Zhao, Qin; Lian, Mi; Gao, Qing-He; Liu, Mei-Cai; Yang, Yan; Wu, An-Xin published the artcile< I2/CuO-catalyzed tandem cyclization strategy for one-pot synthesis of substituted 2-aminothiazole from easily available aromatic ketones/α,β-unsaturated ketones and thiourea>, SDS of cas: 57493-24-0, the main research area is aminothiazole preparation thiourea aromatic ketone butenone cyclization.

A concise and efficient one-pot process from easily available Me ketones or unsaturated Me ketones and thiourea was developed for the synthesis of 2-aminothiazoles with I2/CuO as catalyst. The method gave the E-isomers of 4-ethenyl-2-aminothiazoles. All these target mols. were characterized by NMR, HRMS and IR spectra.

Tetrahedronpublished new progress about 1,3-Dicarbonyl compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, SDS of cas: 57493-24-0.

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

Jaffett, Victor A.; Nerurkar, Alok; Cao, Xufeng; Guzei, Ilia A.; Golden, Jennifer E. published the artcile< Telescoped synthesis of C3-functionalized (E)-arylamidines using Ugi-Mumm and regiospecific quinazolinone rearrangements>, Safety of Thiazole-5-carboxyaldehyde, the main research area is arylamidine stereoselective preparation; azidobenzoic acid isocyanide aldehyde bismethylaminoethane Ugi Mumm regiospecific rearrangement.

An efficient four-step, six-transformation protocol was developed to afford bioactive N-alkyl- or N-arylamide (E)-arylamidines I (R1 = Cy, 4-OMeC6H4, i-Pr, etc.; R2 = i-Pr, i-Bu, H, etc.; R3 = H, 5-CH3, 5-F, etc.) featuring strategic amidine C3 modifications which were inaccessible or low yielding by previous methods. This synthetic approach, exemplified with 24 amidines and requiring only a single purification, highlights a multicomponent Ugi-Mumm rearrangement to afford highly diversified quinazolinones which undergo regiospecific rearrangement to afford new amidines. The method extensively broadens the structural scope of this new class of trisubstituted amidines and demonstrates the tolerance of regional C3 amidine steric bulk, visualized with X-ray crystallog. anal.

Organic & Biomolecular Chemistrypublished new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Safety of Thiazole-5-carboxyaldehyde.

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

Hansen, Ida K. O.; Loevdahl, Tomas; Simonovic, Danijela; Hansen, Kine O.; Andersen, Aaron J. C.; Devold, Hege; Richard, C. Eline S. M.; Andersen, Jeanette H.; Strom, Morten B.; Haug, Tor published the artcile< Antimicrobial activity of small synthetic peptides based on the marine peptide turgencin a: prediction of antimicrobial peptide sequences in a natural peptide and strategy for optimization of potency>, Name: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is turgencin antimicrobial peptide Escherichia Staphylococcus; Arctic; Synoicum turgens; antimicrobial; ascidian; peptide; synthetic.

Turgencin A, a potent antimicrobial peptide isolated from the Arctic sea squirt Synoicum turgens, consists of 36 amino acid residues and three disulfide bridges, making it challenging to synthesize. The aim of the present study was to develop a truncated peptide with an antimicrobial drug lead potential based on turgencin A. The experiments consisted of: (1) sequence anal. and prediction of antimicrobial potential of truncated 10-mer sequences; (2) synthesis and antimicrobial screening of a lead peptide devoid of the cysteine residues; (3) optimization of in vitro antimicrobial activity of the lead peptide using an amino acid replacement strategy; and (4) screening the synthesized peptides for cytotoxic activities. In silico anal. of turgencin A using various prediction software indicated an internal, cationic 10-mer sequence to be putatively antimicrobial. The synthesized truncated lead peptide displayed weak antimicrobial activity. However, by following a systematic amino acid replacement strategy, a modified peptide was developed that retained the potency of the original peptide. The optimized peptide StAMP-9 displayed bactericidal activity, with minimal inhibitory concentrations of 7.8 μg/mL against Staphylococcus aureus and 3.9 μg/mL against Escherichia coli, and no cytotoxic effects against mammalian cells. Preliminary experiments indicate the bacterial membranes as immediate and primary targets.

International Journal of Molecular Sciencespublished new progress about Anti-inflammatory agents. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Name: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

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

Wang, Mu-Xuan; Qin, Hong-Wei; Liu, Chao; Lv, Shen-Ming; Chen, Jia-Shu; Wang, Chun-Gu; Chen, Ying-Ying; Wang, Jia-Wei; Sun, Jin-Yue; Liao, Zhi-Xin published the artcile< Synthesis and biological evaluation of thiazolidine-2-thione derivatives as novel xanthine oxidase inhibitors>, SDS of cas: 96-53-7, the main research area is thiazolidine thione preparation xanthine oxidase inhibitor SAR mol modeling.

In this study, a series of novel thiazolidine-2-thione derivatives I (R1 = Et, Pr, Ph, benzyl) and II (R2 = Et, 3-pyridyl, cyclohexyl, etc.) were synthesized as XO inhibitors, and the XO inhibitory potencies of obtained compounds I and II was evaluated by in vitro enzyme catalysis. The result shown that compound II [R2 = (4-fluorobenzene)sulfonyl] behaved the strongest XO inhibitory activity with an IC50 value of 3.56μmol/L, which was approx. 2.5-fold more potent than allopurinol. The structure-activity relationship revealed that the phenyl-sulfonamide group was indispensable for thiazolidine-2-thione derivatives II [R2 = (4-fluorobenzene)sulfonyl] to produce XO inhibitory activity. The enzyme inhibition kinetics analyses confirmed that compound II [R2 = (4-fluorobenzene)sulfonyl] exerted a mixed-type XO inhibition. Addnl., the mol. docking results suggested that the 4-fluorophenyl-sulfonyl moiety could interact with Gly260 and Ile264 in the innermost part of the active pocket through 2 hydrogen bonds, while the thiazolidinethione moiety could form two hydrogen bonds with Glu263 and Ser347 in hydrophobic pockets. In summary, the results described above suggested that compound II [R2 = (4-fluorobenzene)sulfonyl] could be a valuable lead compound for the treatment of hyperuricemia as a novel XO inhibitor.

PLoS Onepublished new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, SDS of cas: 96-53-7.

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

da Silva, Monize M.; Ribeiro, Gabriel H.; de Camargo, Mariana S.; Ferreira, Antonio G.; Ribeiro, Leandro; Barbosa, Marilia I. F.; Deflon, Victor M.; Castelli, Silvia; Desideri, Alessandro; Correa, Rodrigo S.; Ribeiro, Arthur B.; Nicolella, Heloiza D.; Ozelin, Saulo D.; Tavares, Denise C.; Batista, Alzir A. published the artcile< Ruthenium(II) Diphosphine Complexes with Mercapto Ligands That Inhibit Topoisomerase IB and Suppress Tumor Growth In Vivo>, Application In Synthesis of 96-53-7, the main research area is melanoma antitumor lung breast cancer hTopIB docking ruthenium complexes.

Ruthenium(II) complexes (Ru1-Ru5), with the general formula [Ru(N-S)(dppe)2]PF6, bearing two 1,2-bis(diphenylphosphino)ethane (dppe) ligands and a series of mercapto ligands (N-S), have been developed. The combination of these ligands in the complexes endowed hydrophobic species with high cytotoxic activity against five cancer cell lines. For the A549 (lung) and MDA-MB-231 (breast) cancer cell lines, the IC50 values of the complexes were 288- to 14-fold lower when compared to cisplatin. Furthermore, the complexes were selective for the A549 and MDA-MB-231 cancer cell lines compared to the MRC-5 nontumor cell line. The multitarget character of the complexes was investigated by using calf thymus DNA (CT DNA), human serum albumin, and human topoisomerase IB (hTopIB). The complexes potently inhibited hTopIB. In particular, complex [Ru(dmp)(dppe)2]PF6 (Ru3) (I), bearing the 4,6-diamino-2-mercaptopyrimidine (dmp) ligand, effectively inhibited hTopIB by acting on both the cleavage and religation steps of the catalytic cycle of this enzyme. Mol. docking showed that the Ru1-Ru5 complexes have binding affinity by active sites on the hTopI and hTopI-DNA, mainly via π-alkyl and alkyl hydrophobic interactions, as well as through hydrogen bonds. Complex Ru3 displayed significant antitumor activity against murine melanoma in mouse xenograph models, but this complex did not damage DNA, as revealed by Ames and micronucleus tests.

Inorganic Chemistrypublished new progress about Antitumor agents. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Application In Synthesis of 96-53-7.

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