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

This work includes two steps of synthesis, the first one is the synthesis of indole which was prepared according to literature of the reaction of phenyl hydrazine with acetaldehyde in glacial acetic acid afforded phenyl hydrazone of acetaldehyde , this product was fused with zinc chloride to give the indole.Reaction of cyclohexanone with phenyl hydrazine using the same procedure for the preparing giving 1,2,3,4-Tetrahydrocarbazole.Second step involved synthesis of a series of (17) of mannich bases derivatives of indole and 1,2,3,4-Tetrahydrocarbazle. Mannich reaction involves the condensation of aldehyde usually formaldehyde with different secondary amine and with compound containing an activated hydrogen.The reaction illustrated by the fo

This study includes the synthesis of new derivatives of 1, 2, 4- Triazole which are contain Schiff bases derived from 1, 4, 5, 6- tetrahydropyrimidine. The structures of these derivatives were characterized from their melting points, infrared spectroscopy and elemental analysis. These derivatives were tested for inhibition of E-coli and were all found to be active.

N-Benzylidene m-nitrobenzeneamines (Schiff bases) were prepared by condensation of m-nitroaniline with aromatic aldehydes. These Schiff bases were found to react with maleic anhydride to give 2-Aryl-3-(m-nitrophenyl)-2, 3-dihydro [1, 3] oxazepine–4, 7–diones and with phthalic anhydride to give 2-Aryl-3–(m-nitrophenyl)–2, 3–dihydrobenz|| 1, 2-e|||| 1, 3] oxazepine–4, 7-diones which were reacted with pyrrolidine to give the anilide–pyrrolidides of maleic acid and phthalic acid.

In this work a series of fourteen new compounds were synthesized. Compound [1] was formed from the reaction of 2-aminobenzothiazole and p-bromophenacyl bromide. Aldehyde group [2] was obtained from the reaction of compound [1] with pocl3 in presence of DMF and CHCl3 .After that shiff bases have been synthesized from the reaction of compound [2] with different aromatic amine to give new shiff bases [3- 5]. These new shiff bases have been reduced to their corresponding amine [6-8] by means of sodium borohydride. Then reaction of shiff bases [3-5] with phenyl isocyanate gives 3-cyclic lactam derivatives [9-11]. 3-cyclic Oxazepine derivatives [12-14] were obtained by reaction of shiff bases [3-5] with succinic anhydride. These new formed co

Compound 4-(((6-amino-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl)methoxy)methyl)- 2,6-dimethoxyphenol (6) was synthesized by multi steps. The corresponding acetonitrile thioalkyl (7) was cyclized by refluxing with acetic acid to afford 4-(((6-amino-7H-[1,2,4]triazolo[3,4- b][1,3,4]thiadiazin-3-yl)methoxy)methyl)-2,6-dimethoxyphenol (8). Two new series of 4-(((6-(3- (4-aryl)thioureido)-7H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazin-3-yl)methoxy)methyl)-2,6- dimethoxyphenol (9a-c) and of 4-(((6-(substitutedbenzamido)7H-[1,2,4]triazolo[3,4- b][1,3,4]thiadiazin-3-yl)methoxy)methyl)-2,6-dimethoxyphenol (10a-c) were synthesized as new derivatives for fused 1,2,4-trizaole-thiadiazine(8). The antioxidants of newly compounds were evaluated by DPPH

Compound 4-(((6-amino-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (6) was synthesized by multi steps. The corresponding acetonitrile thioalkyl (7) was cyclized by refluxing with acetic acid to afford 4-(((6-amino-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (8). Two new series of 4-(((6-(3-(4-aryl) thioureido)-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (9a-c) and of 4-(((6-(substitutedbenzamido) 7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (10a-c) were synthesized as new derivatives for fused 1, 2, 4-trizaole-thiadiazine (8). The antioxidant

In 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.