SYNTHESIS OF SOME IBUPROFEN AMINO ACID HETEROCYCLIC COMPOUNDS
WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES (Issue : 11) (Volume : 8)
Ibuprofen amino acid esters (2a-e) were synthesized by the reaction of
ibuprofen (extraction from ibuprofen drug) with amino acid esters
(glycine, phenylalanine, tyrosine, isoleucine, methionine) and they
were converted to corresponding hydrazides (4a-e) by hydrazine
hydrate. Hydrazones (5a-b) were synthesized by the reaction of
hydrazide with p-nitrobenzaldehyde which cyclized to 1, 3, 4-
oxadiazole 2, 5- disubstituted (7a-b) and phthalazine (6) by the
reaction with lead oxide and hydrochloric acid, respectively. Ibuprofen
amino acid amides (3a-d) were synthesized by passing ammonia gas
through corresponding esters. The structures of the synthesized
compounds were confirmed by physical and spectral methods. The
antifungal activity of the compounds (Ibuprofen, 2e, 4c, 5a, 7a) against four types of fungi (A.
Niger, A. tubingensis, A. foatiday, A. awamori) were studied and discussed.
SYNTHESIS AND SPECTRAL CHARACTERIZATION OF BIS (SUB-PYRROLIDINYL) DIONES
WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES (Issue : 6) (Volume : 7)
The present work describes the synthesis of new pyrrolidines and chalcone derivatives. Synthesis of chalcones (10-17) were acheved by condensation of diacetyl with substituted benzaldehyds in ethanolic sodium hydroxide (50%)(1: 2). The later compounds reacted with Schiff bases (1-8) to yield 1, 2-bis (2, 4, 5-tri (4-aryl) pyrrolidin-3-yl) ethane-1, 2-dione (20-27). The characterization of some resulting products were confirmed by physical properties, and spectral data UV-Visible, FT-IR, 1 H NMR, 13 C NMR.
Synthesis of Some New Oxadiazole and Tetrazole Derived from Naproxen Drugs
Swift Journal of Pharmacy and Pharmacology (Issue : 1) (Volume : 1)
Naproxen amino acid ester (2a-b) prepared by the reaction of naproxen with amino acid esters. Hydrazides (3a-b) were obtained by reaction of corresponding esters with hydrazine hydrate. These hydrazides were used to synthesize a series of five membered ring heterocyclic compounds, the hydrazides (3a-b) were converted to 1,3,4-oxadiazole-2-thione (4a-b) by their reaction with carbon disulfide in ethanolic potassium hydroxide. 2,5-Disubstituted 1,3,4-oxadiazole (6a-b) were obtained from the reaction of lead oxide with naproxen amino acid hydrazone (5a-b) where hydrazone prepared from the reaction of hydrazides (3a-b) with p-nitrobenzaldehyde. Mono substituted 1,3,4-oxadiazole (8a-b) were synthesized from the reaction of 2-formyl hydrazine (7a-b) with Phosphorous pentoxide. Finally, 4-amino 1,2,4-triazol-5-thiol (10a) was prepared from the reaction of dithiocarbazate salt with hydrazine hydrate. The structures of synthesized compounds were confirmed by physical and spectral means.
Synthesis of Some New Tetrazole and 1,3-Thiazolidin-4-One Derived from Schiff Base
Swift Journal of Pure and Applied Chemistry (Issue : 1) (Volume : 2)
A series of heterocyclic compounds tetrazole (3a-d) and 1,3-thiazolidin-4-one (4a-d) derivatives were synthesized by the reaction of Schiff base derivative (2a-d) with sodium azide, 2-mercptoactic acid respectively. The IR and 1HNMR spectral data of the synthesized compounds were also discussed.
Synthesis and Biological Evaluation of Some Dipeptide Derivatives and Their Heterocyclic Compounds
Journal of University of Zakho (Issue : 1) (Volume : 3)
The protected dipeptide esters (3a-e, 4a-l) is prepared by the reaction of compounds (1a-e, 2a-d) with
dicyclohexylcarbodiamide (as coupling reagent) and amino acid esters .Thereafter hydrazides (5a-e, 6a-j)
are obtained by the reaction of corresponding esters with hydrazine hydrate. Hydrazones (7a-e, 8a-e) are
synthesized by the reaction of the above hydrazides with p-nitro benzaldehyde , which was cyclized to 2,5-
disubstituted 1,3,4- oxadiazole (9a-e, 10a-e) through lead oxide and to phthalazines (13a-b) through
hydrochloric acid. 1,3,4- oxadiazole -2- thione (11a-b, 12a-e) were prepared by the reaction of the
corresponding hydrazides with carbon disulfide in alcoholic potassium hydroxide. Hydrazides were
reacted with ammonium thiocyanate to afford thiosemicarbazide (14a-c) which were cyclized to 1,2,4-
triazole -3- thione (15a-b) in sodium hydroxide medium. The structures of the synthesized compounds
were confirmed by physical and spectral methods. The antibacterial activity of the prepared compounds
(5d, 7a, 9e, 10d, 11a, 12e, 13a, 14b) against the gram +ve and –gram –ve Bactria (Staphylococcus aureus,
Bacillus subtilis, Escherichia coli and Proteus mirabilis) were studied and discussed.
Synthesis and Biological Activity of Copper (Ii), Nickel (Ii) and Cobalt (Ii) With Tetradentate Schiff Bases Complexes Derived From 2-Hydroxy-1-Naphthaldehyde and Aromatic Diamines
Science Journal of University of Zakho (Issue : 1) (Volume : 1)
2-hydroxy-1-napthaldehyde reacted with diaminophenol in absolute EtOH in a ratio 2: 1 to give new Schiff bases (H 2 L 1, H 2 L 2 and H 2 L 3). The obtained Schiff bases which were in tautomeric equilibrium (enol-imine OH… N, keto-amine O… HN forms) were used as ligands to coordinate Cu (II), Ni (II), and Co (II) leading complexes. The ligands and the complexes were characterized by physicochemical, elemental and spectroscopic analyses. The complexes exhibited 1: 1 metal to ligand coordination ratio (ML 1),(ML 2),(ML 3). Both Ligands and complexes were evaluated for antibacterial properties using disc diffusion method.. The complexes showed higher activity than the free ligands.
Synthesis of some Phthalazine from Hydrazone of Amino Acids Authors H.A. Basheer and N.S. Ezzat
Tikrit Journal of Pure Science (Issue : 1) (Volume : 13)
A number of hydrazone (2a-h) were synthesiszed from
the reaction of protected amino acid hydrazide and
substituted benzaldehyde. The obtained products then
treated with amyl alcohol saturated with HCl gas to give
a number of substituted phthalazine (3a-h). The
structures of the synthesized compounds were confirmed
by IR spectra methods.
Synthesis of Some Substituted Pyrano 1, 3-oxazine
National Journal of Chemistry (Volume : 28)
Chloro-2-methyl thio-2-N-ethyl carbazato, 2N-acetyl tyrosyl hydrazido 4, 5-dioxo pyrano [3, 4-e]-1, 3-oxazine-4, 5-dione , 2, 7-di (N-ethyl carbazato) 4, 5-dioxo pyrano [3, 4-e]-1, 3-Oxazine-4, 5-dione  and, 7-chloro 2N-acetyl amino acid hydrazido, 2N-benzoyl amino acid Hydrazido-4, 5-dioxo pyrano [3, 4-e]-1, 3-oxazine 4, 5-dione  were synthesized by standard methods. The pyrano-1, 3-oxazine  was prepared from condensation of two moles of malonyl chloride with methyl or benzyl thiocyanate. Spectroscopic characteristics (IR, NMR) of the pyrano-1, 3-oxazine derivatives are presented and discussed.
Synthesis of Imidine Hydrochloride and Some Heterocyclic Compounds
Iraqi National Journal Of Chemistry (Volume : 21)
Some heterocyclic compounds were prepared from the reaction of primary amine derivatives with imidate (which was prepared by the reaction of nitrile (1) with ethanol in presence of hydrogen chloride). Imidine was also prepared by the reaction of nitrile (1) with some primary amines in presence of aluminum chloride. The synthesized compounds were confirmed by IR spectra.
Synthesis of 1,2,4-Oxadiazolidine and Isoxazolidine Derivatives from Addition of Isocyanates and Alkenes to Nitrones
Rafidain Journal of Science (Issue : 8) (Volume : 16)
Some new heterocyclic compounds of 1,2,4-oxadiazolidine-5-one derivatives
[3a-m] were synthesized from the reaction of nitrone compounds with some isocyanates
of amino acid esters in good yields.
The reaction of nitrone compounds with cyclooctene and tetrahydrophthalic
anhydride gave oxazolidine derivatives [4a-d]. The synthesized compounds were formed
via 1,3-cycloaddition reaction of isocyanates and alkenes to nitrones. The I.R. spectral
data of the synthesized compounds were also discussed.
Synthesis of N-(Thiazolyl and benzothiazolyl) Dipeptide ester
J. Educ. Sci. (Issue : 2) (Volume : 16)
N-(thiazloyl /benzothiazoyl) dipeptide ethyl ester were synthesized from the reaction of chloro acetic acid with 2-amino (thiazole/ benzothiazole).The products allowed to under goes reactions with thionyl chloride and then with some amino acid ester (glycine, tryrosine, cysteine, methionine, valine, phenyl alanine and lucine). The synthesized compounds have been characterized by I.R.and C.H.N. analyses.
Synthesis of N-(Thiazolyl and benzothiazolyl) Dipeptide ester
J. Educ. Sci. (Issue : 2) (Volume : 16)
N-(thiazloyl /benzothiazoyl) dipeptide ethyl ester were synthesized from the reaction of chloro acetic acid with 2-amino (thiazole/ benzothiazole).The products allowed to under goes reactions with thionyl chloride and then with some amino acid ester (glycine, tyrosine, cysteine, methionine, valine, phenyl alanine and leucine). The synthesized compounds have been characterized by I.R.and C.H.N. analyses.
Synthesis and Antibacterial Evaluation of Some N-Amino Acid-3-Phthalimidine Amino Acid Esters
Teachers College Researchers journal (Issue : 1) (Volume : 1)
Some new amino acid derivatives were prepared from the reaction of amino acids esters (glycine, tyrosine and cystine) with 2-thioxo phthaloyl of the following amino acids (leucine, valine, glycine and alanine), The reaction products were tested against six types of bacteria. The results indicated that N-valyl-3-phthalimidine ethyl tyrosinate and N-anyl-3-phthalimidine ethyl cystinate showed remarkable activity against Pseudomonas araginosa. The synthesized compounds were characterized by using elemental analysis. IR spectral methods and their melting points.
Synthesis and antibacterial evaluation of some 1,2,4- triazole 5-one and semicarbazide derivatives
J. Educ. Sci. (Issue : 1) (Volume : 15)
A series of heterocyclic compounds, 1,2,4-triazole-5-one (4a-f) derivatives and substituted semicarbazides (3a-k) were prepared by condensation of N-acetyl or N- benzoyl amino acid hydrazides (1a-g) with isocyanate of some amino acid esters.(2a-e). The antimicrobial activity of some of the synthesized compounds especially compounds (3i and 4e) against six species of bacteria showed a significant activity against all types of the bacteria sutdieded. the products were identified on the bases of I.R. spectral data and elemental analysis
Synthesis of some new 1,3,4- Oxadiazole derivatives
Raf.Jour. Sci (Issue : 1) (Volume : 13)
A series of 1,3,4- Oxadiazole-2-one were synthesized by the reaction of amino acid hydrazides and dipeptides (valine, leucine, tyrosine, methionine, cysteine, and glycine) with carbone disulphide in alkaline medium gave 1,3,4-oxadiazol-2-one. The synthesized compounds were characterized by physical and spectral analysis.