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.
In this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids were dehydrated in the third step via treatment with acetic anhydride and anhydrous sodium acetate to afford a series of the desirable N-(substitu
... Show MoreFive N-substituted poly diimides were prepared by two steps. First step was included the preparation of five N-substituted diamides by reaction of adipoyl chloride with different amines .The second step was involved reaction of diamides with poly acryloyl chloride to obtain five new poly diimides having different physical properties which may used in different applications.
Schiff bases of Ceftizoxime sodium were synthesized in an attempt to improve the antimicrobial spectrum of Ceftizoxime. Aminothiazole ring of Ceftizoxime is linked directly through an imino group to different aromatic aldehydes reacted by nucleophilic addition using trimethylamine (TEA), as a catalyst and refluxed in methanol. The antimicrobial activity was evaluated for such Schiff bases using disc diffusion method. Molecular docking was conducted on certain penicillin-binding proteins (PBPs) and carboxypeptidases using 1- click docking software. Schiff bases of Ceftizoxime were prepared with reasonable yields and their chemical structures were confirmed by spectral analysis (FTIR, 1H-NMR) and elemental microanalysis (CHNS). The antibacter
... Show MoreNew complexes of Cu (ll), Ni (ll), Co (ll), and Zn (ll) wi th 2-amino-5-p-Fiouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(Ff-IR), UV-Vis and the melting points were determined. The new Schiff base (L) has been used to prepare some complexes. The prepared complexes were identified and their structural geometry were suggested
To synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap
... Show MoreThis study involves the synthesis of a new class of silicon polymers, designated as P1-P7, derived from dichlorodimethylsilane (DCDMS) in combination with various organic compounds (Schiff bases prepared from different amines and appropriate aldehydes or ketones) [I-V] through condensation polymerization. The structures of all monomers and polymers were characterization by FTIR and 1HNMR spectroscopy (for some polymers). The results of thermogravimetric analysis (TGA) and differential scanning calorimetry DSC test show stable thermal behaviour. Polymers with a higher concentration of aromatic rings in their repeating structural units exhibited a higher temperature for weight loss, indicating increased thermal stability. Thermal meas
... Show MoreThe present work involved four steps: First step include reaction of acrylamide ,N-?-Methylen-bis(acryl amide) and N-tert Butyl acryl amide with poly acryloyl chloride in the presence of triethyl amine (Et3N) as catalyst, the second step include homopolymerization of all products of the first step by using benzoyl peroxide(BPO) as initiator in (80-90)Co in the presence of Nitrogen gas(N2). In the third step the poly acrylimide which prepare in second step was convert into potassium salt by using alcoholic potassium hydroxide solution. Fourth step include Alkylation of the prepared polymeric salts in third step by react it with different alkyl halides(benzyl chloride, allylbromide , methyl iodide) by using DMF as solvent for(10-12) hours.
... Show MoreWith the aim of developing potential antimicrobials, a series of novel Ciprofloxacin methylene isatin derivatives incorporating different aromatic aldehydes were synthesized and characterized by FTIR, 1H NMR, Mass spectroscopy and bases of elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique. A majority of compounds were showing activity against several of the microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds is discussed. From comparisons of the compounds, 3c was determined to be the most active compound.
Dylan Thomas (1914-1953) is a modern poet belongs to the apocalyptic movement of the 1940's.This movement is influenced by the doctrines and techniques of surrealism.
Poetry for him should not be primarily concerned with man in society, but with the celebration of spiritual truth. It should bring to light the hidden causes, hence his personal interest is to strip darkness and explore the inward motives. To do this he uses a cluster of images: a constant building up and breaking down of images. His poetry depends on the romantic spontaneity, suggestiveness of the Symbolists and the the surrealists' mysterious liberation of the unconsciousness and
... Show MoreDylan Thomas (1914-1953) is a modern poet belongs to the apocalyptic movement of the 1940's.This movement is influenced by the doctrines and techniques of surrealism. Poetry for him should not be primarily concerned with man in society, but with the celebration of spiritual truth. It should bring to light the hidden causes, hence his personal interest is to strip darkness and explore the inward motives. To do this he uses a cluster of images: a constant building up and breaking down of images. His poetry depends on the romantic spontaneity, suggestiveness of the Symbolists and the the surrealists' mysterious liberation of the unconsciousness and the emotional involvement in the dynamics of life. In "Light Breaks
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