Treatment of nosocomial and community acquired Staphylococcus aureus infections has become more challenging due to the egression of multi-drug resistance. This has spurred the need for rapid development of new therapeutic agents which can effectively negate the resistance mechanisms. In our curr...

A new series of 2-mercapto-3-substituted-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-ones were synthesised by reacting 3-amino-2-mercapto-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one with different aldehydes and ketones. The starting material 3-amino-2-mercapto-5,6-dimethylthieno[2,3-d]pyrimidin-4(...

A differential pulse anodic stripping voltammetric method was developed for the determination of Ag(I) at a 3-amino-2-mercapto quinazolin-4(3H)-one modified carbon paste electrode. The analysis procedure consisted of an open circuit accumulation step in stirred sample solution for 12 min. This w...

P2Y12 plays an important role in platelet aggregation, which makes it an interesting target for antithrombotic agents. Compounds that antagonize P2Y12 include the active metabolites of thienopyridines and molecules that are structurally related to ATP, which is an antagonist of P2Y12. During the...

A series of heterocyclic benzenesulfonamides incorporating 2-mercapto-3H-quinazolin-4-one tails were prepared by condensation of substituted anthranilic acids with 4-isothiocyanato-benzenesulfonamide. These sulfonamides were investigated as inhibitors of the human carbonic anhydrase (hCA, EC 4.2...

Condensation of substituted anthranilic acids with 4-isothiocyanatoethyl-benzenesulfonamide led to series of heterocyclic benzenesulfonamides incorporating 2-mercapto-quinazolin-4-one tails. These sulfonamides were investigated as inhibitors of the human carbonic anhydrase (hCA, EC 4.2.1.1) isof...

Some derivatives of 3-ethyl-2-mercapto-thieno[2,3-d]pyrimidin-4(3H)-ones were synthesized using ethyl 2-aminothiophene-3-carboxylates as precursors in order to estimate their cytotoxicity, respectively proliferative activity.Thienopyrimidinones containing thiosemicarbazide as well as 1,3,4-thiad...

Aedes albopictus (Skuse) (Diptera: Culicidae), an aggressive and annoying vector of several arbovirus including Chikungunya and Zika, is a serious health problem worldwide. Control of this mosquito is difficult because of high adaptability, egg resistance to dehydration and ability to exploit ma...

The FTIR and FT-Raman spectra of 2-mercapto-4(3H) quinazolinone have been recorded in the region 4000–450 and 4000–100 cm−1, respectively. The optimized geometry, frequency and intensity of the vibrational bands of 2-mercapto-4(3H) quinazolinone (2MQ) were obtained by the density functional th...

A new series of 2-substituted mercapto-4(3H)-quinazolinone 1–26 were synthesized and assessed for in vivo anti-inflammatory and analgesic activities and in vitro inhibition of cyclooxygenase COX-1/COX-2.A new series of 2-substituted mercapto-4(3H)-quinazolinone 1–26 were synthesized and assess...

There iridium(III) complexes, [Ir(3-MeO-Phtpy)Cl3] (1), [Ir(2-MeO-Phtpy)Cl3] (2) and [Ir(4-MeO-Phtpy)Cl3] (3) with 4′-(3-methoxyphenyl)-2,2′:6′,2″-terpyridine (3-MeO-Phtpy), 4′-(2-methoxyphenyl)-2,2′:6′,2″-terpyridine (2-MeO-Phtpy) and 4′-(4-methoxyphenyl)-2,2′:6′,2″-terpyridine (4-M...

Non linear optical material of t-3-ethyl-r-2,c-6-bis(4-methoxyphenyl)-1-nitrosopiperidin-4-one (NPM3EPO) is grown by slow evaporation technique by using methanol as solvent. The absorption spectrum range of grown crystals is identified by UV-Vis spectroscopy. The presence of functional groups an...

The compounds 5-(4-hydroxy-3-methoxy-phenyl)-3,7-dimethyl-5H-thiazolo[3,2-a]pyrimidine-2,6-dicarboxylic acid 2-ethyl ester 6-methyl ester (2a) and 3,7-dimethyl-5-naphthalen-1-yl-5H-thiazolo[3,2-a]pyrimidine-2,6-dicarboxylic acid diethyl ester (2b) were synthesized by the base catalyzed cyclocond...

An efficient and practical method for synthesis of the optically active hexahydro-1,4-diazepine 2, which is a key intermediate of DAT-582, a potent and selective serotonin-3 receptor antagonist, is described. Treatment of the (R)-1,2,3-trisubstituted aminopropane dihydrochloride 5b prepared from...

The title compound was obtained with high regioisomeric and enantiomeric purity starting from the tartrate salt of (1S,2S)-1-hydroxy-2-methylaminocyclohexane. The determination of the enantiomeric excess both of the title compound and of its precursor (2S)-2-(N-methyl-N-benzyloxycarbonylamino)cy...

The first total synthesis of a new enantiopure polyhydroxylated cyclopentyl β-amino acid [methyl (1S,2R,3S,4R,5S)-2-benzyloxy-5-benzyloxycarbonylamino-3-hydroxy-4-methoxycyclopentanecarboxylate] was achieved according to our recent novel strategy for the transformation of nitrohexofuranoses int...

Glutathione S-transferases (GST) from corn, giant foxtail, onion, pea, house fly, and equine liver catalyzed conjugation of tridiphane with glutathione (GSH). The conjugate was characterized by soft ionization mass spectral methods. Tridiphane and the GSH conjugate of tridiphane both inhibited G...

Cyclic carbonates were synthesized by reactions of the corresponding oxiranes with β-butyrolactone using quaternary salts such as tetrabutylammonium bromide or 18-crown-6 = KBr as a catalyst.

The synthesis of N-[7-(2-amino-3,4-dihydro-4-oxo-quinazolin-6-yl)-6-formyl-1-oxo-heptyl]-l-glutamic acid (2, abenzyl 10-formyl-5,8,10-trideazafolic acid) as a potential enzyme-assembled tight binding inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) or aminoimidazole carboxamide...

N-carboxamide-substituted 7-deazaguanine-7-carboxamides and their ribofuranosyl compounds have been synthesized as echiguanine derivatives, and evaluated for inhibition of phosphatidylinositol (PI) 4-kinase. The ethylamide derivative and the corresponding ribofuranosyl compound inhibited PI 4-ki...