Preparation and Identification of some new Pyrazolopyrin derivatives and their Polymerizations study

The work involves synthesis of new Schiff bases ([V] a, b and [VI] a, b), pyrazoles [VII] a, b and pyrazolines [VIII] a, b derivatives containing isoxazoline unit starting with chalcones. 4-bromoacetophenone was reacted with 4-hydroxybenzaldehyde or 4-hydroxyacetophenone was reacted with 4-bromobenzaldehyde in basic medium to give chalcone by Claisen-Schemidt reaction. The chalcons [I] a, b was reacted with hydroxylamine hydrochloride to form isoxazolines [II] a, b. which were reacted with ethyl chloro acetate in basic medium to get ester compounds [III] a, b. The condensation new ester [III] a, b with hydrazine hydrate80% yieldedacid hydrazide [IV] a, b. The later compound refluxing with 4-substituted benzaldehyde in dry benzene to give Sc

Non-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphon

This study includes design and synthesis of new non-steroidal anti-inflammatory agents (NSAIDs) with expected cyclooxygenase-2 (COX-2) selective inhibition to achieve better activity and low gastric side effects. Two series of compounds have been designed and synthesized as potential NSAIDs,these  are:     Salicylamide derivatives (compounds 3,4,5 ) and Diflunisal derivatives (compounds 10&11). In vivo acute anti-inflammatory effect of one of the synthesized agents (compound 3)  was evaluated in the rat using egg-white induced paw edema model of inflammation. Preliminary pharmacological study revealed that compound 3 exhibited less anti-inflammatory effect  compared to that of aspirin after

compound [1] was formed from the reaction of benzoin and benzaldehyde in the presence of ammonia, which was reacted with sodium hydride in DMF to obtain imidazole salt. This salt was reacted with adipoyl chloride to give compound [2]. Acid hydrazide derivative [3] was obtained from the reaction of compound [2] with hydrazine hydrate. After that Shiff bases [4-9] have been synthesized from the reaction of compound [3] with different aromatic aldehydes. These new formed compounds were diagnosed by 13C-NMR, 1H-NMR for some of them (in Ahl-Albate University in Jordan) and FT-IR spectroscopy (In Baghdad University). All of the prepared products have been studied their biological activities toward two kinds of bacteria. These products show

New membrane electrodes for determination of ciprofloxacin hydrochloride were prepared depending on ciprofloxacin hydrochloride - phosphotungstic acid (CFH-PT) as an active material and these electrodes were made with three plasticizers: Di-octylphenylphosphonate(DOPH), Di-butyl phosphate (DBP)Tri-n-butyl phosphate(TBP), in PVC matrix. One of the ciprofloxacin electrodes was gave Nernstian slope equal to 57.21 mV/ decade for DOPH membrane with concentration range from 1.5×10-5 to1.0×10-1 M, and detection limit equal to 1.5×10-6 M .Lifetime was 93 days. Non- Nernstian responses equal to 39.40 and 30.70 mV/ decade for membranes DBP, TBP, respectively. These electrodes were gave concentration range from 1.0× 10-5 to 1.0×10-2 and from 4.0

4, 4s (pyridine 2, 6 diylbis (1, 3, 4 oxadiazole 5, 2 diyl)) bisphenol monomer (3) was synthesized from cyclization of Ns2, Ns6 bis (4 hydroxybenzylidene) pyridine 2, 6 dicarbohydrazide (2) in the presence of bromine in glacialacetic acid. Newly five polymers (P1P5) were synthesized from reaction bis 1, 3, 4 oxadiazole bisphenolmonomer with five different di acid chloride. The antibacterial activity of the synthesized polymers was screened against gram positive and gram negative bacteria. Polymers P4 and P5 exhibited significant antibacterial against all microorganisms, as well these polymers showed highest antifungal activity.

This search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in dry pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [2-amino-5-mercapato-1,3,4-thiadiazole] was prepared through the reaction of thiosemicarbazide with carbon disulphide (CS2) in entity of anhydrous (Na2CO3) in (abs. ethanol ). Compound (VI) [2-(5-mercapto-1,3,4-thiadiaz

4-amino-3-(4-(((4-hydroxy-3, 5dimethoxybenzyl) oxy) methyl) phenyl)-1, 2, 4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoyl) hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1, 2, 4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2, 2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays