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There are currently still no approved antiviral drugs to treat or prevent chikungunya virus (CHIKV) infections despite the fact that this arbovirus continues to cause outbreaks in Africa, Asia, and South- and Central-America. Thus 20 new conjugated compounds in the families of bis(benzofuran?1,3-thiazolidin-4-one)s and bis(benzofuran?1,3-thiazinan-4-one)s were designed based on the structural features of suramin. These new compounds were synthesized by chemical methods and their structures were confirmed spectroscopically. In CPE reduction assays, six of these new bis-conjugates inhibited CHIKV replication in Vero E6 cells with EC50 in the range of 1.9?2.7 muM and selectivity index values of ?75 or higher. These results and compounds provide a starting point for further optimization, design, and synthesis of new antiviral agents for this (re)emerging disease.

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A series of Ethyl 2-[2-(2,5-disubstituted-1H-indol-3-yl)-4-oxothiazolid-3-ylamino]-5,6-dihydro-5-oxo-4H-1,3,4-thiadiazine-6-carboxylates (4a?g) were synthesized from cyclocondensation of Ethyl 2-{(2E)-2-[(2,5-disubstituted-1H-indol-3-yl) methy leno] hydrazine}-5-oxo-5,6-dihydro-4H-1,3,4-thiadiazine-6-carboxylates (3a?g) with thioglycolic acid in the presence of the catalytic amount of zinc chloride. The compounds 3a?g were obtained from the reaction of Ethyl 2-hydrazinyl-5,6-dihydro-5-oxo-4H-1,3,4-thiadiazine-6-carboxylate (2) with various substituted indole-3-carboxaldehydes 1a?g. Newly synthesized compounds were characterized by using IR, 1H NMR, Mass spectral and analytical data. Title compounds were evaluated for their in vitro antimicrobial activities against various microbial strains and selected compounds were tested for their analgesic and anti-inflammatory activities. Some of the newly synthesized Indolyl 4-thiazolidinone analogues displayed significant activity towards antimicrobial, analgesic and anti-inflammatory activities.

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The compounds of the invention are antagonists of MDM2 and/or MDMX, with excellent specificity for MDM2 and/or MDMX over other proteins. Several analogs demonstrate selective binding affinity to MDMX over MDM2. The disclosed compounds can therefore regulate p53 activity and treat a variety of cancers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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New discoveries in chemical research and development in 2021. Chemical research careers are more diverse than they might first appear, as there are many different reasons to conduct research and many possible environments. In a patent, 76186-04-4, name is (S)-4-Isopropylthiazolidine-2-thione, introducing its new discovery. Product Details of 76186-04-4

A total synthesis of the proposed structure of the natural polyketide-macrolactone phomolide H 2 has been achieved following a bidirectional strategy from l-tartaric acid. The originally assigned structure of phomolide H displayed discordant NMR spectroscopic data in comparison with synthetic 2. The synthetic strategy was extended to prepare diastereomers and epimeric methyl-ethers of the natural product, structural analysis of which revealed a match of the natural product with diastereomer 27. The structural revision of phomolide H from 2 to the methanol solvate of compound 27 is presented.

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We recently reported a new C3-symmetric (R)-phenylglycinol N-1,3,5-benzenetricarboxylic acid-derived chiral high-performance liquid chromatography (HPLC) stationary phase (CSP 1) that demonstrated better results as compared to a previously described N-3,5-dintrobenzoyl (DNB) (R)-phenylglycinol-derived CSP. Over a decade ago, (S)-leucinol, (R)-phenylglycine, and (S)-leucine derivatives were used as the starting materials of 3,5-DNB-based Pirkle-type CSPs for chiral separation. In this study, three new C3-symmetric CSPs (CSP 2, 3, and 4) were prepared by combining the ideas and results mentioned above. Here we describe the synthetic procedures and applications of the new C3-symmetric CSPs (CSP 2?CSP 4).

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New series of N-[2-{2-(substitutedphenyl)-4-oxo-5-(substitutedbenzylidene)-1,3-thiazolidine}-iminoethyl]-2-amino-5-nitrothiazole, 5(a-m) have been synthesized from 2-amino-5-nitrothiazole as a starting material by conventional as well as microwave methods. All the synthesized compounds 4(a-m) were screened for their antibacterial and antifungal activities against some selected bacteria and fungi and antitubercular activity screened against Mycobacterium tuberculosis. The structure of all the synthesized compounds were confirmed by chemical and spectral analyses such as IR, 1H NMR, 13C NMR and FAB-Mass.

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4-Formylpyrazoles are useful building blocks in organic synthesis. This review focuses on the applications of 4-formylpyrazoles to generate a large variety of organic compounds and heterocycles such as Schiff bases, pyrazolylpyrazolines, pyrazoloquinolinones, 4H-pyrazolopyran, pyrazolylbenzoxazole, pyrazolothiadiazepines, pyrazolyloxazolone, pyrazolyloxadiazolines, pyrazolylthiadiazolines, imidazolylpyrazoles, pyrazolopyridines, chromenopyrazolones, thiopyranothiazolylpyrazoles and many others. Many of these molecules exhibit excellent biological activities.

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4-Thiazolidinone compounds have been reported to display good antioxidant activity. In the present work, the five-membered ring has been studied extensively at the DFT-B3LYP/6-311(++)G(d,p) level of theory. The geometrical features of the ring have been explored in the gas and solvent phase. Various molecular descriptor characteristics of the antioxidant compound have been calculated and compared with the reference antioxidant, trolox. Three probable antioxidant mechanisms, hydrogen atom transfer (HAT), single electron transfer (SET), and sequential proton loss electron transfer (SPLET), have been explored, both in the gas and solvent phase. It has been found that the ring exerts its antioxidant activity predominantly following the HAT pathway, both in the gas and solvent phase. In order to determine the feasibility of the overall redox reaction, the standard redox potentials have been calculated for the ring and free radicals. Furthermore, the effect of substitution on the antioxidant parameters of the ring has been explored. Results indicate that substitution at the C2 position is advantageous over that at C5 in improving such parameters. Along with this, the effect of substitution at the C2 position on the proton affinity of the C5 position has also been investigated in detail.

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Enantioselective approaches to the construction of four complex building blocks of the structurally intricate marine macrolide known as spongistatin 1 are presented. The first phase of the synthetic effort relies on a practical approach to a desymmetrized, enantiomerically pure spiroketal ring system incorporating rings A and B. Concurrently, the C17-C28 subunit, which houses one-fifth of the stereogenic centers of the target in the form of rings C and D, was assembled via a composite of stereocontrolled aldol condensations. Once arrival at the entire C1-C28 sector had been realized, routes were devised to provide two additional highly functionalized sectors consisting of C29-C44 and C38-C51. A series of subsequent transformations including cyclization of the E ring and hydroboration to afford the B-alkyl intermediate for the key Suzuki coupling to append the side chain took advantage of efficient stereocontrol. Ultimately, complete assembly and functionalization of the western EF sector of spongistatin was thwarted by an inoperative Suzuki coupling step intended to join the side chain to the C29-C44 sector, and later because of complications due to protecting groups, which precluded the complete elaboration of the late stage C29-C51 intermediate.

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An amino-thiazolidinone platinum(II) compound which could rapidly induce apoptosis in tumor cells and showed no cross resistance against the cisplatin-resistant cells, was firstly to study of protein-drug interactions. To investigate the potential of Pt(II) compounds as therapeutic drugs, two Pt(II) complexes (1 and 2) were explored the influences based on their interaction in vitro with human serum albumin (HSA) by fluorescence spectrometry and UV?Vis absorption. The binding interactions of two compounds with HSA results in the formation of corresponding HSA-drug complexes, van der Waals forces and hydrogen bonding played key roles in stabilizing these complexes. Both of two compounds were through a dynamic quenching mechanism, this dynamic reversible binding process was of great significance to the equilibrium of drug concentrations in vivo, which ensured that the internal environment of the organism was in a relatively stable state.

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