4-Chloro-2-(1-hydroxybenzyl)pyridine and 4-chloro-2-(1-hydroxyalkyl)pyridines were obtained with moderate to excellent enantiomeric excesses and high isolated yields by bioreduction with Baker’s yeast of the corresponding ketones. The resulting optically active alcohols were transformed into ad...
In this study, we explore a series of novel potential antiprotozoal S-(−)-limonene-based benzaldehyde thiosemicarbazones were synthesised and their activity effective against the extracellular promastigote form of Leishmania amazonensis examined. Likewise, in parallel, a series of R-(+)-limonene...
The title compound 1 is readily prepared by a Pinner reaction on the adduct of phenylsulfinic acid with acrylonitrile. The anion derived from 1 adds 1,4 to enones to give specific enolates which are trapped with trimethylsilyl chloride. The resulting trimethylsilyl enol ethers cyclise smoothly t...
Approximate rate constants for intermolecular additions of alkyl radicals to phenylsulfonyl oxime ethers (2a and 2b) have been determined to be ka=9.6×105 M−1s−1 at 25 °C for 2a and ka=7.3×104 M−1s−1 at 60 °C for 2b, indicating that the additions are fast and highly efficient processes. The ...
An efficient and operationally simple strategy for the stereoselective synthesis of novel C-3 functionalized 3-sulfonyl-β-lactam heterocycles is described. The C-3 functionalized 3-phenyl/benzylsulfonyl-β-lactams 3/3′, 5/5′ has been synthesized via Michael addition using different Michael ac...
Syntheses, biological evaluation, and structure–activity relationships for a series of novel 2-substituted 3-benzenesulfonyl-5,6-dimethyl-pyrazolo[1,5-a]pyrimidines are disclosed. In spite of a wide, four orders of magnitude, SAR range (Ki varied from 260 pM to 2.96 μM), no significant correla...
Triprolidine hydrochloride is extensively used as antihistamine and anticholinergic drug. We have examine the binding mechanism of triprolidine hydrochloride (TRP) with human serum albumin (HSA) using fluorescence spectroscopy, circular dichroism (CD), isothermal titration calorimetry (ITC) and ...
Longan fruit has a limited postharvest life due to aril breakdown, a typical senescence characteristics. In this study, effects of l-cysteine hydrochloride (LCH) on senescence of harvested longan fruit associated with modification of redox status were investigated. Application of LCH delayed ari...
An electrochemical sensor for cadmium ions is described which is made by modifying a gold electrode with 3-mercaptopropionic acid followed by covalently coupling the cadmium-selective hexapeptide His–Ser–Gln–Lys–Val–Phe. The resultant electrode had significantly superior analytical performa...
Acute mountain sickness (AMS) is a dangerous hypoxic illness that can affect humans who rapidly reach a high altitude above 2500 m. In the study, we investigated the changes of cytokines induced by plateau, and the acetazolamide (ACZ) influenced the cytokines in rats exposed to high altitude. Wi...
A novel, simple, sensitive and selective spectrofluorimetric method was developed for the determination of Acetazolamide in pharmaceutical tablets and serum samples using photo probe Tb3+-ACAC. The Acetazolamide can remarkably quench the luminescence intensity of Tb3+-ACAC complex in DMSO at pH ...
Chloride was recently recognized to play an important role in the pathophysiology of heart failure (HF). Chloride manipulation, including the use of acetazolamide, may be a requisite therapeutic target in HF treatment. An 87-year-old male patient with advanced HF and hypertrophic cardiomyopathy ...
A compatibility study of drug substance with excipients is a crucial step in the drug development process in order to generate potent final drug formulations for efficient and safe therapy for various diseases. Thus, the development of new methods for compatibility studies is a great challenge. ...
The intent of this study was to provide topical delivery of acetazolamide by preparing chitosan-STPP (sodium tripolyphosphate) nanoparticles of acetazolamide and evaluate the particle size, zeta potential, drug entrapment, particle morphology; in vitro drug release and in vivo efficacy. The part...
In the present work, the antiglaucoma drug, acetazolamide, was formulated as microsponges in situ gel for ocular drug delivery aiming an improved therapeutic efficacy and reduction in the systemic side effects of oral acetazolamide. The microsponges were prepared by the quasi emulsion solvent di...
Vascular calcification is a recognised source of morbidity among mid-age and elderly subjects. Its development follows classical mineralisation pathways, inhibited by acidosis. It is known that the final mechanism of tissue mineralization involves three processes, all of which are highly pH depe...
The behavior of several alpha-monosubstituted cyclohexanone oximes under Beckmann rearrangement conditions is compared. Alpha-1-chlorocyclohexane and cyclohexane substituted oximes undergo the normal rearrangement, while the alpha-cyclohexene substitution gives rise to fragmentation products. Th...
Cyclic allylic acetates undergo smooth allylation and alkynylation with allyltrimethylsilane and alkynyl silanes in the presence of molecular iodine under mild conditions to afford the corresponding allylated and alkynylated cyclohexene derivatives in good yields with high selectivity.
Reaction of cuprates derived from R3MgBr/CuI/LiBr (R3 = n-alkyl) with R1CCCH(O2CR2)2 (R1 = sp2 hybridised substituent, R2 = mainly Me, alkyl, Ph) provides access to allenyl esters R1R3CCCH(O2CR2) (51–88%). Such species are not accessible via rearrangement of precursor propargylic R1R3C(O2CR2)CCH.
The photochemical transformation of 1-cyclohexenyl phenyl ketone (1) to the hexahydrofluorenone 2 (“photo-Nazarov cyclization”) was reinvestigated on the level of conventional preparative chemistry backed up by nuclear magnetic resonance (NMR) spectroscopy and deuteration experiments. Hitherto...
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