A new compounds of 2,4-substituted-1,3- thiazole containing amines [I] and [II], Schiff bases [IV] and [V], amides [VI]-[X],esters [XI] - [XIII], thiazolidinones [XIV]-[XVIII] and 1,3-oxazepines [XIX]-[XXV] were Synthesized and characterized by melting points, FTIR spectroscopy, elemental analysis, 1HNMR,13CNMR, dept135and Mass spectroscopy. The liquid crystalline properties of the synthesized compounds were verified by using hot-stage polarizing optical microscopy (POM) and differential scanning calorimeter (DSC). The compound [I] was found to be nematic textures (N). The first series of this study [II]n display only enantiotropic nematic phase when n=1-5 while the compounds with n =6-8 display two mesophasese smectic C(SmC) and nematic phases(N). All compounds of series [IV]n were found to be enantiotropic nematic phase. Compounds[VI]a and[VI]b showed both semctic and nematic phases. Compounds [XI]a, b and [XIII]a, b showed only nematic texture but the compounds [XI]c and [XIII]c did not show any liquid crystalline properties. All compounds of series [XVII]n with n=1,3-7 display only nematic texture but compound with n=8 showed semactic C phase (SmC) in addition of ne
Nonsteroidal anti-inflammatory drugs (NSAIDs) are drugs that help reduce inflammation, which often helps to relieve pain. In this research new ibuprofen oxothiazolidnone derivatives were synthesized from the reaction of Schiff base derivatives of Ibuprofen with mercapto acetic acid VI a-c, to improve the potency and to decrease the drug's potential side effects, a new series of 4-thiazolidinone derivatives of ibuprofen was synthesized VI a-c . The characterizations of the compounds were identified by using FTIR, 1HNMR technique and by measuring the physical properties.
Newly acid hydrazide was synthesized from ethyl 2-(2,3-dimethoxyphenoxy) acetate (2), which is cyclized to the corresponding 4-amino-1,2,4-triazole (3). Five newly azo derivatives (4a-e) were synthesized from this 1,2,4-triazole by converting the amine group to diazonium salt then reacted with various substituent phenol,as well three newly imine derivatives (5a-c) were synthesized from reacting the amine group of compound (3) with three aryl aldehyde. The thermal electro conductivity of these compounds was tested at 30, 50, 75 and 100 áµ’C. compound 4a showed interesting electro conductivity at 75áµ’C as well 5a at 75áµ’C while 5b showed significant conductivity at 100 áµ’C
The pandemic SARS-CoV-2 is highly transmittable with its proliferation among nations. This study aims to design and exploring the efficacy of novel nirmatrelvir derivatives as SARS entry inhibitors by adapting a molecular modeling approach combined with theoretical design. The study focuses on the preparation of these derivatives and understanding their effectiveness, with a special focus on their binding affinity to the S protein, which is pivotal for the virus’s access to the host cell. Considering molecular docking aspects in the scope of a study on nirmatrelvir derivatives and S protein, dynamics simulations with 25 nanoseconds of their binding are explored. The study shows that these derivatives might work as effective antivi
... Show MoreHeterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehy
... Show MoreFive derivatives of thiadiazole were prepared with aldehydes and alkyl halides, compoundA: 2-amino-5-thiol-1,3,4- thiadiazole, compound B :2-(o-hydroxybenzylidine)amino-5-thiol-1,3,4-thiadiazole, compoundC: 2(2-butan-lidine)amino-5-thiol-1,3,4-thiadiazole, compound E: 2- amino-5-(2-Propanylthio)-1,3,4-thiadiazol) and compound F:2(o-chlorobenzylamino)-5-(2-propanyl thio)-1,3,4 thiadiazol. All prepared compounds were diagnosed by (IR) and (UV) Spectroscopy. All of those compounds were screened for their anti-microbial activity in vitro. The results show that most of the compounds A, B, C exhibited moderate to good activity against Gram-positive bacteria and the same compound exhibit low to moderate activity on most gram-negative bacte
... Show MoreThe compounds 3-[4̄-(4˭-methoxybenzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one(3)aand 4-(1-(5-oxo- 2-thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(3)b were prepared from the reaction of aromatic aldehyde or ketone(1)a,bwith thiosemicarbazide to give aryl thiosemicarbazones(2)a,b ,followed by cyclization with ethylchloroacetate in the presence of fused sodium acetate. Treatment the compounds(3)a,bwith 4- hydroxybenzenediazoniumchloride yielded the correspondings4-((4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)methyl)phenyl 4-methoxybenzoate(4)aand4-(1-(4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(4)b.The new 2-thioxo-imidazolidin-4-one with esters (5-7)a,b sy
... Show MoreThe synthesis of new benzodiazepine, imidazole, isatin, maleimide, pyrimidine and 1,2,4-triazole derived from 2-amino-4-hydroxy-1,3,5-triazine, via its cyclocondensation reaction with different organic reagents, is described. FT-IR, 1H-NMR and as well as 13C-NMR spectra disclosed the structures of the precursors and heterocyclic derivatives formed.
A new series of 5-methoxy-2-mercapto benzimidazole derivatives were synthesized by the reaction of 5-methoxy- 2-mercaptobenzimidazole with chloroacetic acid and affords 2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio) acetic acid (1),which on cyclization with acetic anhydride and pyridine gives 7- methoxybenzo[4,5]imidazo[2,1-b]thiazol- 3(2H)-one(2), which on condensation with different aryl aldehydes in the presence of anhydrous sodium acetate in glacial acetic acid, furnishes a arylidene thiazolidinone. The purity of the synthesized compounds was confirmed by melting point and TLC.The structures were established by different spectral analysis such as FTIR,1HNMR, and CHN analysis. The newly synthesized compounds (3a-d) were in vivo evaluated f
... Show MoreA new carbonyl complexes of triazole and oxadiazole were synthesized. These complexes were identified and their structural geometric were suggested by using FT-IR and UV-Vis spectra, conductivity measurements and other chemical and physical properties. The spectra data (FT-IR, UV, Vis.) with the substantial aid of group theoretical calculations gave so many evidences for the proposed geometries and the type of bonding of these compounds