The synthesis of a series of thiazolo3,2-apyrimidine derivatives were described. The structures of the compounds were elucidated by IR, 1H-NMR, 13C and elementary analysis. The compounds were ...evaluated for their calcium antagonistic activities using nifedipine as standard compound. All of the compounds were found to be less potent than nifedipine.
Some new tetrahydropyrimidine-2-thione, octahydroquinazoline-2-thione and thiazolo3,2-apyrimidine derivatives have been synthesized and tested for their antihypertensive activity. Among them, ...compounds 1 and 2b can be considered more potent than the reference, nifedipine (CAS 21829-25-4), while compounds 3b and 10a are equipotent to it. In addition, compound 6 showed significant antihypertensive activity.
Our strategy for the exploration of new NSAIDs starts on the synthesis of derivatives of 5-oxo-5H-Thiazolo 3,2-a pyrimidines. The compounds were achieved by the following methods: (a) condensation of ...2-amino-4-alkylthiomethilthiazole with ethyl 4-chloro-3-oxobutanoate (PPA method), (b) triphenyl phosphonium salts preparation, (c) Wittig-reaction of the salts with suitable aldehyde. Synthesized compounds were screened for antiinflammatory activity in the carrageenin rat paw oedema assay according to Winter et al. Some of the new synthesize compounds, at the dose used (50 mg/Kg) reduced meaningfully the oedema. The pharmacological effect varies according to the administration time.
Several derivatives of two mesoionic xanthine analogs, mesoionic thiazolo3,2-alphapyrimidine-5,7-diones and mesoionic 1,3,4-thiadiazolo3,2-alphapyrimidine-5,7-diones, were synthesized and evaluated ...as inhibitors of cyclic AMP phosphodiesterase. A significant number of these compounds demonstrated theophylline-like activity.
Fused pyrimidines play an imperative role in our life due to their biological importance in the struggle of microorganisms. A series of 4-aryl-3-methyl-1-phenyl-1,4,6,7-tetrahydropyrazolo3,4-d ...thiazolo3,2-apyrimidine (4a-j) were synthesized by cyclization of 3-methyl-1-phenyl-4-aryl-1,4,5,7-tetrahydro-6H-pyrazolo3,4-dpyrimidine-6-thiones (3a-j) with 1,2-dibromoethane in presence of anhydrous potassium carbonate. Earlier, compounds (3a-j) were synthesized by the condensation of 5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one (2), different substituted benzaldehyde and thiourea with catalytic amount of con. HCl in methanol. Compound 2 was synthesized by condensation of ethyl acetoacetate (1) and phenylhydrezine in presence of a catalytic amount of acetic acid at reflux temperature. The constitution of the synthesized products has been characterized by using elemental analysis, Infrared, 1H-NMR spectroscopy and further supported by Mass spectroscopy. All the products have been screened for their in-vitro biological assay like antibacterial and antifungal activity at concentration of 500 μg/ml. It was exposed that most of the compounds displayed inspiring antibacterial and antifungal activity compared to the used reference standard.
Humic acid, a rarely used non virulent, easily accessible, inexpensive, environmentally benign, high molecular weight polymer, because of its extraordinary catalytic activity has been explored for ...the synthesis of functionalised 4
H
-benzo4,5thiazolo3,2-
a
pyrimidine-3-carboxylate and its derivatives along with functionalised benzo
d
thiazole. Environmental friendliness, low catalyst loading, outstanding yield, magnificent functional group forbearance and renewability up to fifth run without any noteworthy loss of its activity at the finishing point of reaction, are the cue significances of these methods.
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EMUNI, FIS, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, MFDPS, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, SBNM, UKNU, UL, UM, UPUK, VKSCE, ZAGLJ
A cubic phase of pure MgO nanopowders was prepared in an aqueous solution containing freshly squeezed orange juice with pulp and characterized by X‐ray diffraction (XRD), field emission scanning ...electron microscopy (FE‐SEM), energy‐dispersive X‐ray spectroscopy (EDS), and Fourier transform infrared (FT‐IR) spectroscopic techniques. The catalytic potential of MgO nanopowders was evaluated in preparation of pyrano4,3‐dthiazolo3,2‐apyrimidine and chromeno4,3‐dthiazolo3,2‐apyrimidines derivatives using the three simple methods including thermal, ultrasonic irradiation, and high‐speed ball milling (HSBM) technique under solvent‐free conditions. All products were successfully formed in high yields.
Three simple methods including thermal, ultrasonic irradiation, and HSBM technique are reported for the preparation of pyrano4,3‐dthiazolo3,2‐apyrimidine and chromeno4,3‐dthiazolo3,2‐apyrimidine derivatives in the presence of MgO nanopowders under solvent free conditions. MgO nanopowders were prepared in an aqueous solution containing freshly squeezed orange juice with pulp and characterized by XRD, FE‐SEM, EDS, and FT‐IR techniques.
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FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
A new series of 6-methyl-4-aryl-2-thio-1,2,3,4-tetrahydropyrimidine-5-carboxylic acids ethyl esters was synthesized. The reaction of the obtained esters with dimethyl 2-chloroethynylphosphonate leads ...to the selective formation of new ethyl 3-(dimethoxyphosphoryl)-5-aryl-7-methyl-5
H
-thiazolo3,2-
a
pyrimidine-6-carboxylates.
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EMUNI, FIS, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, MFDPS, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, UKNU, UL, UM, UPUK, VKSCE, ZAGLJ
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