Sinteza i anthelmintičko djelovanje novih 2-supstituiranih-4,5-difenil imidazola

A series of 2-substituted-4,5-diphenyl imidazoles 1a-j were synthesized by refluxing benzil with different substituted aldehydes in the presence of ammonium acetate and glacial acetic acid. Structures of the synthesized compounds were confirmed on the basis of IR, 1H NMR and mass spectral data. Compounds 1a-j were screened for anthelmintic activity. Test results revealed that compounds showed paralysis time of 0.24 to 1.54 s and death time of 0.39 to 4.40 s while the standard drugs albendazole and piperazine citrate showed paralysis time of 0.54 and 0.58 s and death time of 2.16 and 2.47 s, respectively, at the same concentration of 1 % (m/V). Five compounds, 2-[2-hydroxyphenyl]-4,5-diphenyl imidazole (1b), 2-[3-methoxyphenyl]-4,5-diphenyl imidazole (1c), 2-[2-phenylethenyl]-4,5-diphenyl imidazole (1e), 2-[4-fluorophenyl]-4,5-diphenyl imidazole (1g) and 2-[3-nitrophenyl]-4,5-diphenyl imidazole (1h) showed significant anthelmintic activity compared to the standard drugs.Refluksiranjem benzila s različitim supstituiranim aldehidima u prisutnosti amonijeva acetata i ledene octene kiseline sintetizirana je serija 2-supstituiranih-4,5-difenil imidazola (1a-j). Strukture sintetiziranih spojeva potvrđene su IR, 1H NMR i masenom spektroskopijom. U testovima na anthelmintičko djelovanje određeno je vrijeme paralize 0,24 do 1,54 min i vrijeme smrti 0,39 do 4,40 min, dok standarni lijekovi albendazol i piperazin citrat imaju vrijeme paralize 0,54 i 0,58 min, a vrijeme smrti 2,16, odnosno 2,47 min pri istim koncentracijama (1 % m/V). Pet spojeva, 2-[2-hidroksifenil]-4,5-difenil imidazol (1b), 2-[3-metoksifenil]-4,5-difenil imidazol (1c), 2-[2-feniletenil]-4,5-difenil imidazol (1e), 2-[4-fluorofenil]-4,5-difenil imidazol (1g) i 2-[3-nitrofenil]-4,5-difenil imidazol (1h) pokazuju značajno anthelmintičko djelovanje u odnosnu na standardne lijekove

3-Propynyl-2-substituted Carboxylic Acid Derivatives of Quinazolinone

Alkylation of quinazolinone-2-carboxylic acids with propargyl bromide in dimethylformamide in the presence of potassium carbonate afforded 3-prop-2-ynyl quinazolinone-2-substituted carboxylic acid derivatives. Further reaction of 4b-c produced 5b-c, which indicates that N-alkylation occurs before esterification with a propynyl moiety

Triflate-mediated Synthesis of 3-(4-Methoxyquinazolin-2-yl)- quinazolin-2,4-(1H,3H)-dione and its Antimicrobial Activity.

The synthesis of a novel quinazolinone was accomplished by the reaction of quinazolin- 2,4-(1H,3H)-dione with trifluoromethanesulfonic anhydride in triethylamine. The antimicrobial activity was determined against eight microorganisms. The organisms were all susceptible to 3-(4-methoxyquinazolin-2-yl)-quinazolin-2,4-(1H,3H)-dione 3 at the concentrations used. The gram positive organisms showed more susceptibility than the gram negative ones

Reaction of Prop-2-ynylamine with Isochromadiones : Formation of Amides

The ring opening of isochromadiones by prop-2-ynylamine was accomplished in non-polar solvents to form N-prop-2-ynylbenzamide-2-acetic acid 3 N-prop-2-ynylhomophthalimide 4. Compound 3 was found out to be an intermediate product in the formation of 4. These compounds were screened for anticonvulsant and antibacterial properties and were found to have no activity

Determination of Dihydroartemisinin In Bulk And Pharmaceutical Formulations By Redox Titrations And UV - Spectrophotometry Using Potassium Permanganate As Oxidimetric Reagent

ABSTRACT Two new methods are proposed for the determination of dihydroartemisinin (DHA) in bulk and pharmaceutical formulations. Method A Titrimetry, based on the redox reaction of DHA and potassium permanganate in acid medium. Method B, UV-Spectrophotometry based on the redox reaction of DHA and potassium permanganate in acid medium giving a product which absorbs UV light at 520nm. In both methods the amount of potassium permanganate used is proportional to the amount of DHA. Experimental conditions for good linearity, sensitivity, specificity accuracy and precision were optimized. In method A (titrimetry) the calculations are based on a 2:5 (DHA: KMnO 4 ) reaction stoichiometry) and this method is applicable over the practical range of 5.0 -20mgml -1 . Method B obeys Beer's law. The calibration curve generated is linear with correlation coefficient of (r) of 0.9998 (n = 10). The molar absoptivity is 2.27 x10 3 Lmol cm -1 and sandell sensitivity of 0.126gcm -2 The limit of detection (LOD) and limit of quantification (LOQ) were determined as per the current ICH guidelines and found to be 0.88 and 2.66gml -1 respectively. Accuracy and precision of both method were determined using intra and inter day variations at three different concentration level of DHA the relative standard deviation (RSD %) were <2.00 and <2.5 respectively. The two methods were used to assay DHA in 4 brands of tablets formulation procured locally in Uyo. South-South, Nigeria at three different concentration level, t and F value of <2.40 and <3.0 at 95% confidence level and 5 degree of freedom. These values are lower than tabulated t and F values. The methods were statistically compared with an official method with congruent results. There was no interference from common pharmaceutical excipients. Recovery study was also performed via standard addition procedure with excellent recoveries