Propranolol is a nonselective-adrenergic blocker used in the treatment of hypertension, cardiac arrhythmias, and angina pectoris. A significant problem in propranolol therapy is that it undergoes extensive presystemic metabolism after oral administration leading to reduced bioavailability. In this study, two new propranolol derivatives have been designed, synthesized and characterized. These compounds were formed by acylation of propranolol followed by nucleophilic substitution reaction of acylated propranolol, these derivatives were analyzed for IR, CHN, melting points, and evaluated for their lipophilic properties compared with propranolol. The lower partition coefficient of these two derivatives revealed that the prodrug approach may be an effective means of avoiding first- pass metabolism.
A new series of morpholine derivative were prepared by reacting the morpholine with ethyl chloro acetate in the presence triethylamine as an catalyst and benzene as a solvent gave the ethyl morpholin-4-ylacetate reaction with hydrazine hydrate and ethanol as a solvent gave the 2-(morpholin-4-yl)acetohydrazide gave series of Schiff base were prepared by reacting 2-(morpholin-4- yl)acetohydrazide with different aromatic aldehydes and ketons . The new series of (3-9 )were synthesis by reaction of Schiff base (10-14) with chloroacetyl chloride, triethyl amine as an catalyst and 1,4dioxane as a solvent .The chemical structures of the synthesis compound were identified by spectral methods their [ IR ,1H-NMR and 13C-NMR ].The synthesised compoun
... Show MoreNitrogen-comprising heterocyclic compounds and their derivatives have empirically been invaluable as therapeutic agents. Fundamentally, 4-chloro-6-nitro-2-amino-1,3-benzothiazole 1 was synthesized via bromination of 2-chloro-4-nitro aniline with ammonium thiocyanate. This new heterocyclic haloorganoamino-1,3-benzothiazole derivative, was a starting material, which condensed and tethered with three different aromatic aldehyde pendant arm in presence of ethanol and glacial acetic acid isolating an interesting sequence of tridentate Schiff bases 2-4. These compounds were used for complexation reactions in 1:1 (metal: ligand) stoichiometry to obtain heteroleptic Al(III), Ni (II) and K(I) benzothiazole chelat
... Show MoreIn this research two series of the new derivatives of Trimethoprim and paracetamol drugs have been prepared which known as a high medicinal effectiveness. Series (A) is including the interaction of diazonium salt of trimethoprim and coupling with some substituted phenol compounds (2-amino phenol, 3-ethyl phenol, 1-naphthol, 2-nitro phenol, Salbutamol). Series (B) is including the interaction coupling alkali solution of paracetamol with diazonium salt of some substituted aniline compounds (Benzedine, 2, 3-di chloro aniline, Trimethoprim, Anilinium chloride, 2-nitro- 4-chloro aniline).Chemical structures of all synthesized compounds were confirmed by UV-visible and FTIR spectroscopy.
This research discloses the synthesis of various polyester resins, the polyesters containing homoring aromatic and others heterocyclic were synthesized by the condensation polymerization of suitable monomers (which are containing variety function groups in different structures) with phthalic anhydride. The main objective is synthesis of new polyester with keeping a reasonable electrical insulating behavior. The structural of polymer was characterized by Fourier Transform infra-red spectroscopy FTIR and HNMR. The dielectric constant (real ε' and imaginary parts ε") and AC conductivity (σAC) for all the polyester samples are studied by varying the frequency (30, 50, 70, 90, 120, 300, 500Hz and 1KHZ) at 25⁰ C. Indeed, study of the electri
... Show MoreThe development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1
... Show MoreIn the present study, ( Schiff's bases 6a - 6e) and (new amids derivatives 6f - 6j) have been synthesized . The glutaroyl chloride(2) has been prepared by the reacting of glutaric acid and thionyl chloride in presence of (DMF) . The new compound bis(4-formylphenyl) glutarate (3) has been Synthesized from reaction of one mole of glutaroyl chloride and two moles of 4-hydroxybenzaldehyde . Compound 4,4'-(glutaroylbis(oxy))dibenzoic acid (4) was Synthesized from one mole of glutaroyl chloride and two moles of 4-hydroxybenzoic acid, while compound bis(4-(chlorocarbonyl)phenyl) glutarate (5) was prepared from 4,4'-(glutaroylbis(oxy))dibenzoic acid and Thionyl chloride . Then Schiff's bases 6a - 6e that prepared
... Show MoreA variety of liquid crystals comprising heterocyclics 1,3,4-oxadiazol ring [III], aminooxazol [IV]a, and aminothiazol [IV]b were synthesized through a number of steps, beginning of the reaction of 3, 3'- dimethyl - [1, 1'-biphenyl] -4, 4'- diamin, ethyl monochloroacetate and sodium acetate to synthesize diacetate compound[I]. The diester reacted with hydrazine hydrate(N2H4-H2O) to give dihydrazide compound [II], then reacted with Pyruvic acid and phosphorous oxychloride to produce diketone compound [III]. The last compound was reacted with urea and thiourea to give aminooxazol and aminothiazol respectively. The synthesized compounds actually characterized and determined the structures by melting points, FT-IR and 1H-NMR spectroscopies. By u
... Show MoreThis research involved synthesis of new β-Lactam derivative from Azo compound[4-amino-N-(pyrimidine-2-yl)-3-(pyrimidine-2-yldiazenyl) benzene sulfonamide] (S1) record previously by many steps. Starting conversion the free amino group in an azo comp. to chloro acetamide derivative(S2), then reacted it with urea to give the oxazole ring derivative (S3) that which containing free amino group. The condensation reaction between the amino group and P-bromobenzaldehyde to produce Shiff base (B14). Finally staudinger's cyclo addition reaction go run between the Shiff base derivative (B14) and chloro acetyl chloride in the presence of tri ethyl amine (Et3N) as Base catalyst and dioxane a
... Show MoreMetoclopramide HCl (MTB) is a potent antiemetic drug used for the treatment of nausea and vomiting. Many trials were made to prepare a satisfactory MTB orodispersible tablet using direct compression method.Various super disintegrants were used in this study which are croscarmellose sodium (CCS), sodium starch glycolate (SSG) and crospovidone (CP). The latter was the best in terms of showing the fastest disintegration time in the mouth.Among the different diluents utilized, it was found that a combination of microcrystalline cellulose PH101 (MCC 101), mannitol, dicalcium phosphate dihydrate (DPD) and Glycine was the best in preparing MTB orodispersible tablet with fastest disintegration time in the mouth.The physical parameters of the pre
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