A simple fluorescent schiff base, X, based on imidazo[2,1-b]thiazole-6-carboxylic acid and 3-ethoxy-2-hydroxybenzaldehyde, was designed and synthesized for detection of Zn2+ and PPi. X showed excellent sensitivity and selectivity toward Zn2+ by exhibiting a large fluorescence enhancement (about ...

A series of bis(indolyl) hydrazide–hydrazones 5a–n were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 in presence of catalytic amount of acetic acid afforded 5a–n in good yiel...

The mild steel anti-corrosion potential by newly synthesized thiazole hydrazones, 4-(4-methoxy-phenyl)-thiazole-2-carboxylic acid benzylidene-hydrazide (TH-1), 4-(4-methoxy-phenyl)-thiazole-2-carboxylic acid (3-hydroxy-benzylidene)-hydrazide (TH-2) and 4-(4-methoxy-phenyl)-thiazole-2-carboxylic ...

Novel C-nucleosides (2′S, 3′S)-2-[2′, 3′-(bishydroxymethyl)-oxetan-1′-yl]-1,3-thiazole-4-carboxamide3 and its carbocyclic analog 4 have been synthesized. Compound 4 enhanced NGF-induced differentiation on PC12 cells at 100 μg/ml, and moreover, 4 alone also induced morphological differentia...

2-(β-d-xylofuranosyl)thiazole-4-carboxamide (2) and two new tiazofurin analogues with 5-hydroxymethyl-2-methyl-tetrahydro-furo[2,3-d][1,3]dioxol-6-ol moiety as a sugar mimic (27 and 28) have been synthesized and evaluated for their in vitro antitumour activity against a panel of human tumour ce...

Trifluoroacetylthiophene carboxamides have recently been reported to be class II HDAC inhibitors, with moderate selectivity. Exploration of replacements for the carboxamide with bioisosteric pentatomic heteroaromatic like 1,3,4-oxadiazoles, 1,2,4-oxadiazoles and 1,3-thiazoles, led to the discove...

This paper presents a novel method for the chemical synthesis of cholest-4-ene-3,6-dione, which is a naturally occurring steroid and a potential intermediate in steroid chemistry. Pyridinium chlorochromate (PCC) in refluxing benzene has been found to be an effective and convenient reagent for th...

(25R)-5α-Cholest-8(14)-ene-3β,15β,26-triol (III) was prepared by reduction of (25R)-3β,26-diacetoxy-5α-cholest-8(14)-en-15-one with sodium borohydride followed by treatment of the crude product with lithium aluminium hydride. The trihydroxysterol III, a potential metabolite of 3β-hydroxy-5...

In this work, a series of novel room temperature ionic liquids (ILs) have been synthesized with cheap, naturally α-amino acid ester as cations and bis(trifluoromethylsulfonyl)imide as anion. The glass transition temperature and thermal decomposition temperature of these ILs, partition coefficie...

Starting from 1-tert-butyloxycarbonyl-3-methyl-4-ethoxycarbonyl-1,2-diaza-1,3-diene and β,β,β and α,β-substituted enamines a careful choice of solvents and temperatures allows the divergent synthesis of 5,6-dihydro-4H-pyridazines, 2-(1-N-boc-hydrazono-ethyl)-4-pyrrolidin-1-yl-but-3-enoic ac...

There have been few reports on synthetic methods for cis-1,2-diaminocyclohexane bearing a third ring substituent. Starting from 3-cyclohexenecarboxylic acid, we developed efficient methods for synthesizing the 3,4-diaminocyclohexanecarboxylic acid derivatives 2–5. We also evaluated their anti-X...

Methyl 5-methoxy-1H-indole-2-carboxylate (MMIC) was prepared via esterification of commercially available 5-methoxyindole-2-carboxylic acid. The title molecule MMIC was characterised using FT-IR and FT-Raman in the ranges of 4000–500 and 4000–50 cm−1, respectively. The fundamental modes of the...

Two new fluorescent carboxylic acid derivatives having 6-hydroxy-1-keto-1,2,3,4-tetrahydrocarbazole moiety, 2-(1-oxo-2,3,4,9-tetrahydro-1H-carbazol-6-yloxy)acetic acid [OTHCA] and 2-(7-methoxy-1-oxo-2,3,4,9-tetrahydro-1H-carbazol-6-yloxy)acetic acid [MOTHCA] were synthesized by Japp–Klingemann ...

The direct reaction of 2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline (EEDQ) with chitosan amino groups, which resulted in the formation of N-(ethoxycarbonyl)chitosan, was found and confirmed chemically and by IR and 1H NMR spectroscopy.

3,5-dinitrosalicylic acid (DNS) reducing sugar assay is the most convenient method for quantification of total reducing sugar in biomass hydrolysate, fermentation samples, sugar industry and biotechnology laboratories. The dimeric proton transfer salt 2-aminoethanaminium 2-(ethoxycarbonyl)-4,6-d...

A series of ethyl 1H-indole-3-carboxylates 9a1–6 and 9b1–2 were prepared and evaluated in Huh-7.5 cells. Most of the compounds exhibited anti-hepatitis C virus (HCV) activities at low concentration. The selectivity indices of inhibition on entry and replication of compounds 9a2 (>10; >16.7) an...

A series of novel acylsulfonamide, acylsulfamide, and sulfonylurea bioisosteres of carboxylic acids were prepared as CXCR2 antagonists. Structure–activity relationships are reported for these series. One potent orally bioavailable inhibitor had excellent PK properties and was active in a lung i...

A convenient and practical synthesis of 6-carboalkoxy-13-cycloalkyl-5H-indolo[2,1-a][2]benzazepine-10-carboxylic acid derivatives (6) has been developed. The key step in the synthesis utilizes an intramolecular tandem reaction sequence of a Michael addition followed by a Horner–Wadsworth–Emmon...

The umifenovir salts of maleic, salicylic, glutaric, and gentisic acid as well as the chloroform solvate of the salicylate were prepared. Single crystals of the five compounds were obtained and their molecular and crystal structures determined by X-ray diffraction. In each structure the conforma...

The treatment of 8,9,10-trimethoxy-7H-pyrrolo[3,2,1-de]phenanthridine-4,5-dicarboxylic acid with phenyliodine diacetate and potassium iodide in tetrahydrofuran gave the corresponding 4,5-diiodo derivative, which was converted to kalbretorine via reduction, demethylation, followed by alkylation.