Preferred Language
Articles
/
bijps-513
Design and Synthesis of New Non-Steroidal Anti-inflammatory Agents with Expected Selectivity toward Cyclooxygenase-2 Inhibition

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 120 and 210 minutes, which encourage the continuation of the search to demonstrate or identify the preliminary pharmacological activity for the  synthesized compounds and to identify their selectivity toward COX-2 isoenzymes.

Keywords:nonsteriodal anti-inflammatory drugs(NSAID),aspirin derivatives ,diflunisal, Cyclooxygenase -1(cox-1),cyclooxygenase-2(cox-2)

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Thu Aug 20 2020
Journal Name
Al-mustansiriyah Journal Of Science
The Importance of 2-AminoThiazole Schiff Bases as Antimicrobial and Anticancer Agents

The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.

Crossref (2)
Crossref
View Publication
Publication Date
Thu Aug 20 2020
Journal Name
Al-mustansiriyah Journal Of Science
The Importance of 2-AminoThiazole Schiff Bases as Antimicrobial and Anticancer Agents

The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.

Crossref (2)
Crossref
Publication Date
Thu Oct 31 2019
Journal Name
Asian Journal Of Pharmaceutical And Clinical Research
DESIGN, SYNTHESIS, DOCKING, ANTITUMOR SCREENING, AND ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION PREDICTION OF NEW HESPERDIN DERIVATIVE

Objective: Hesperidin (HSP) is a pharmacologically active organic compound found in citrus fruits and peppermint. We synthesized a new HSP derivative by reacting it with 5-Amino-1,3,4-thiadiazole-2-thiol in acetic acid. Methods: This compound was characterized by Fourier-transform infrared, proton nuclear magnetic resonance, and electron impact mass spectra. A molecular docking study explores the predicted binding of the compound and its possible mode of action. Bioavailability, site of absorption, drug mimic, and topological polar surface was predicted using absorption, distribution, metabolism, and excretion (ADME) studies. Results: The docking study predicts that the new compound binds to the active sites of Aurora-B

... Show More
Crossref (1)
Crossref
View Publication Preview PDF
Publication Date
Mon Oct 30 2023
Journal Name
Iraqi Journal Of Science
Design and Synthesis of Novel Bis Thiazolo[4,5-c]Isoxazolines Bearing 1,2,4-triazole Ring Derived From the Related 4-thiazolidinons as Antimicrobial Agents

Design and synthesis of novel poly heterocycles together using same heterocyclic compound is the main task of the present paper. The target compounds entitled 4,4’-[benzene-1,4-diylbis[ethylidenehydrazine-2-ylidene]bis[4-[3,5-di(5-substitutedpyridin-2-yl)-3,3a-dihydro[1,3]thiazolo[4,5-c][1,2]oxazol-6(5H)-yl]-4H-3-yl-1,2,4-triazole-3-thiol] have been synthesized starting from the reaction of 1,4-diacetylphenyl and carbohydrazide to give Schiff base derivatives then 1,2,4- triazole derivatives from the reaction with CS2 and an excess of hydrazine hydrate. The same applies for the condensing of these newly heterocyclic amines with different pyridine-2-carbaldehydes, which resulted in the synthesis of some new Schiff bases, whic

... Show More
Scopus (2)
Crossref (1)
Scopus Crossref
View Publication Preview PDF
Publication Date
Sun Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Few New Carrier Polymers Derived from 2-hydrazinylbenzo[d]thiazole

2-hydrazinylbenzo[d]thiazole compound [1] is produced from reaction of 2-mercapto-benzothiazole with hydrazine hydride in ethanol. Compound [1] reacted with maleic anhydride in DMF to produce (Z)-4-(2-(benzo[d] thiazol-2yl) hydrazinyl)-4-oxobut-2-enoic acid [compound (2)]. While the treatment of compound [2] with the ammonium persulfate (NH4)2S2O8 (as the initiator) in order to produce compound [3], then compound [3] reacted with thionyl chloride in benzene to produce compound [4], finally compound [4] reaction with various drugs: cephalexin, amoxicillin, sulfamethizole, elecoxib obtained polymers [5–8]. The structure of synthesized compounds identified by spectral data: fourier transform infrared (FTIR) and proton nuclear magneti

... Show More
Scopus (1)
Scopus Crossref
View Publication Preview PDF
Publication Date
Sun Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Few New Carrier Polymers Derived from 2-hydrazinylbenzo[d]thiazole

2-hydrazinylbenzo[d]thiazole compound [1] is produced from reaction of 2-mercapto-benzothiazole with hydrazine hydride in ethanol. Compound [1] reacted with maleic anhydride in DMF to produce (Z)-4-(2-(benzo[d] thiazol-2yl) hydrazinyl)-4-oxobut-2-enoic acid [compound (2)]. While the treatment of compound [2] with the ammonium persulfate (NH4)2S2O8 (as the initiator) in order to produce compound [3], then compound [3] reacted with thionyl chloride in benzene to produce compound [4], finally compound [4] reaction with various drugs: cephalexin, amoxicillin, sulfamethizole, elecoxib obtained polymers [5–8]. The structure of synthesized compounds identified by spectral data: fourier transform infrared (FTIR) and proton nuclear magneti

... Show More
Scopus (1)
Scopus Crossref
View Publication
Publication Date
Sat Jun 18 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Anti-Inflammatory Activity of Gingko Biloba Extract in Cotton Pellet-Induced Granuloma in Rats: A comparative Study with Prednisolone and Dexamethasone

The current study was designed to evaluate the anti-inflammatory effect of GKB in the rat model of granulomatous inflammation. Thirty rats were distributed into five groups:  The first group served as negative control group that received distilled water (DW) only without inducting inflammation, positive control group; treated with DW with the induction of inflammation and they were assigned to cotton pellet-induced granuloma, ginkgo biloba (GKB) treated group (200mg/kg/day), dexamethasone-treated group (1mg/kg), and Prednisolone treated group (5mg/kg). All the treatments were given orally for seven consecutive days.  On day eight, the rats were anesthetized and the pellets together with granulation tissue were carefully removed

... Show More
Scopus (4)
Crossref (2)
Scopus Crossref
View Publication Preview PDF
Publication Date
Sat May 08 2021
Journal Name
Iraqi Journal Of Science
Synthesis and Identification of Some Imino Chalcone Derivatives with Evaluating their Anti-oxidant Activity

This work involves the preparation of high yield iminochalcon compounds (B1-B15)  through two parts. The first part involves the preparation of 2,4-dihydroxy Chalcone (A1-A15) by the condensation of 2,4-dihydroxy acetophenone  with  aryl aldehyde in the presence of sodium hydroxide (40%) as a catalyst. The second part includes the preparation of  iminochalcon from the condensation of p-hydroxy aniline with 2,4-dihydroxy chalcone  derivatives  )A1-A15)  in the presence of some drops of conc. H2SO4. Thin-layer chromatography ((TLC)  was used to control the chemical reaction . These new derivatives were characterized by using FT-IR and  1H-NMR spectroscopy. These synthesized

... Show More
Scopus (2)
Scopus Crossref
View Publication Preview PDF
Publication Date
Wed Dec 26 2018
Journal Name
Iraqi Journal Of Science
Design of New Dynamic Cryptosystem with High Software Protection

     In this paper a design of new robust and dynamic cryptosystem using stream key generator with good random statistical properties is introduced. The results of the statistical tests, initialization and the components of the proposed generator of the suggested cryptosystem are detailed in [1]. The proposed cryptosystem called Robust and Efficient Dynamic Stream Cipher Cryptosystem (RDSCC). The dynamic here means the generator of RDSCC has unfixed construction; the design will be changed as the seed (initial) key changed. The generator will construct itself by barrows number of Linear Feedback Shift Registers (LFSR’s), randomly, stored in protected bank file. The RDSCC is constructed to be flexibl

... Show More
View Publication Preview PDF
Publication Date
Wed Jul 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Scopus (2)
Crossref (1)
Scopus Crossref
View Publication