scholarly journals Synthesis and Bio-Evaluation of Novel N-(4-(8-Methoxy-2-Oxo-2H-Chromen-3-Yl) Thiazol-2-Yl) Amide Derivatives

2016 ◽  
Vol 71 ◽  
pp. 19-28
Author(s):  
Nilay Shah ◽  
Pineshkumar N. Patel ◽  
Dhanji Rajani ◽  
Denish C. Karia
Keyword(s):  
Acid Chloride ◽  
Antimalarial Activity ◽  
Mass Spectral ◽  
H Nmr ◽  
Chemical Structures ◽  
Compound C ◽  
Amide Derivatives ◽  
Ft Ir ◽  
Derivatives Of ◽  
Solvent Free Reaction

In present work, novel derivatives of substituted N-(4-(8-methoxy-2-oxo-2H-chromen-3-yl) thiazol-2-yl) amide have been synthesized. The solvent free reaction of 2-Hydroxy-3-methoxybenzaldehyde with Ethyl acetoacetate in presence of Piperidine catalyst produces 3-acetyl-8-methoxy-2H-chromen-2-one (C). Compound C was α- brominated using CuBr2and subsequently cyclized using Thiourea to produce 3-(2-aminothiazol-4-yl)-8-methoxy-2H-chromen-2-one as main scaffold (E). This scaffold E was finally reacted with different Acid chloride to isolate title compound derivatives. The chemical structures of synthesized compounds were confirmed by1H-NMR, FT-IR and Mass spectral/LCMS analysis. The synthesized compounds were screened for potential Antimicrobial, Antifungal and Antimalarial activity.

scholarly journals Synthesis, Spectral and Microbial Studies of Some Novel Schiff Base Derivatives of 4-Methylpyridin-2-amine

2009 ◽  
Vol 6 (4) ◽  
pp. 1205-1210 ◽  
Author(s):  
J. J. Vora ◽  
S. B. Vasava ◽  
K. C. Parmar ◽  
S. K. Chauhan ◽  
S. S. Sharma
Keyword(s):  
Schiff Base ◽  
Antimicrobial Activities ◽  
Dilution Method ◽  
Mass Spectral ◽  
H Nmr ◽  
Schiff Base Derivatives ◽  
Ft Ir ◽  
Acid Catalyzed ◽  
Derivatives Of ◽  
Broth Dilution

Schiff base derivatives ofN-{(1E)-[3-(mono or di-substituted aryl)-1-phenyl-1H-pyrazol-4-yl]methylene{-4-methylpyridin-2-amine were synthesized by the acid catalyzed condensation of 3-(mono- or di- substituted aryl)-1-phenyl-1H-pyrazole-4-carbaldehyde derivatives with 4-methylpyridin-2-amine. Schiff base derivatives were characterized by FT-IR,1H-NMR, Mass spectral analysis and elemental analysis. All the synthesized compounds have been screened for their antimicrobial activities by using broth dilution method.

scholarly journals Synthesis and Antimicrobial Studies of Pyrimidine Pyrazole Heterocycles

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Rakesh Kumar ◽  
Jyoti Arora ◽  
Sonam Ruhil ◽  
Neetu Phougat ◽  
Anil K. Chhillar ◽  
...  
Keyword(s):  
Genetic Material ◽  
Oxidative Cyclization ◽  
Antifungal Drugs ◽  
Mass Spectral ◽  
H Nmr ◽  
Antimicrobial Studies ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
Derivatives Of

Prompted from the diversity of the wider use and being an integral part of genetic material, an effort was made to synthesize pyrimidine pyrazole derivatives of pharmaceutical interest by oxidative cyclization of chalcones with satisfactory yield and purity. A novel series of 1,3-dimethyl-6-hydroxy-2,4-dioxo-5-(1′-phenyl-3′-aryl-1H-pyrazol-5′-yl)-1,2,3,4-tetrahydropyrimidines (5a–d) and 1,3-diaryl-6-hydroxy-4-oxo-2-thioxo-5-(1′-phenyl-3′-aryl-1H-pyrazol-5′-yl)-1,2,3,4-tetrahydropyrimidines (5e–l) has been synthesized. The structures of these compounds were established on the basis of FT-IR, 1H NMR, 13C NMR, and mass spectral analysis. All the synthesized compounds were screened for their antimicrobial activity against bacteria and fungi. Among all the compounds, 5g was found to be the most active as its MIC was 31.25 µg/mL against S. aureus and B. cereus. The compounds 5h, 5c, and 5e also possess antibacterial activity with MIC values as 62.50, 125.00, and 500.00 µg/mL, respectively. The compounds 5c and 5j were found to have antifungal activity against Aspergillus spp. As antifungal drugs lag behind the antibacterial drugs, therefore we tried in vitro combination of these two compounds with standard antifungal drugs (polyene and azole) against Aspergillus spp. The combination of ketoconazole with 5c and 5j showed synergy at 1 : 8 (6.25 : 50.00 µg/mL) and 1 : 4 (25 : 100 µg/mL) against A. fumigatus (ITCC 4517) and A. fumigatus (VPCI 190/96), respectively.

scholarly journals Synthesis and Antioxidant Activity of 2-Amino-5-methylthiazol Derivatives Containing 1,3,4-Oxadiazole-2-thiol Moiety

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kikkeri N. Mohana ◽  
Chikkur B. Pradeep Kumar
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Radical ◽  
Radical Scavenging ◽  
Spectral Studies ◽  
Mass Spectral ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir ◽  
Assay Methods

A series of new 5-(2-amino-5-methylthiazol-4-yl)-1,3,4-oxadiazole-2-thiol derivatives 6(a–j) were designed and synthesized with various substituted aldehydes. The chemical structures were confirmed by elemental analyses, FT-IR, 1H NMR, and mass spectral studies. The antioxidant activity of the synthesized compounds was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl, nitric oxide, and superoxide radical scavenging assay methods. Compounds 6a, 6e, and 6c showed significant radical scavenging potential due to the presence of electron donating substituent on substituted aldehydes.

scholarly journals Synthesis of some New Quinoxalines Bearing Pyridinyl Thiazole Moiety

2015 ◽  
Vol 52 ◽  
pp. 74-83
Author(s):  
Haresh G. Kathrotiya ◽  
Yogesh T. Naliapara
Keyword(s):  
Elemental Analysis ◽  
Condensation Reaction ◽  
Mass Spectral Data ◽  
Structural Class ◽  
Mass Spectral ◽  
H Nmr ◽  
Chemical Structures ◽  
Quinoxaline Derivatives ◽  
Ft Ir ◽  
C Nmr

Keeping the objective to build up a new structural class of quinoxaline, a new series of quinoxaline derivatives bearing the pyridinyl thiazole nucleus have been synthesized by base-catalyzed chloro-amine condensation reaction approach. The protocol offers expeditious and easy synthesis with excellent yield. The chemical structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data.

scholarly journals Synthesis of Novel Highly Substituted Pyrimidines Bearing Furanyl Thiazole Nucleous

2015 ◽  
Vol 60 ◽  
pp. 47-57
Author(s):  
Haresh G. Kathrotiya ◽  
Yogesh T. Naliapara
Keyword(s):  
Elemental Analysis ◽  
Aromatic Aldehydes ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Chemical Structures ◽  
Ketene Dithioacetals ◽  
Guanidine Nitrate ◽  
Ft Ir ◽  
C Nmr

A series of novel highly substituted pyrimidines bearing furanyl thiazole nucleous have been synthesized. In which reaction of guanidine nitrate with ketene dithioacetals 3c produced substituted pyrimidines 4d which further treated with various aromatic aldehydes to afford title compounds 5(a-t). The chemical structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Studies ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
H Nmr ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.0 2,6 ] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1 H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC 50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC 50 ＞ 79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC 50 =65.3μM), it indeed significantly abrogated endothelia cell migration (IC 50 =6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

scholarly journals Synthesis of New Imidazolidine and Tetrahydropyrimidine Derivatives

2014 ◽  
Vol 2014 ◽  
pp. 1-4 ◽  
Author(s):  
Hamid Beyzaei ◽  
Reza Aryan ◽  
Zahra Keshtegar
Keyword(s):  
Ring Opening ◽  
Reaction Times ◽  
Reaction Conditions ◽  
Ir Spectrometry ◽  
H Nmr ◽  
Chemical Structures ◽  
Thioamide Group ◽  
Solvent Free Conditions ◽  
Ft Ir ◽  
C Nmr

Synthesis of new imidazolidine and tetrahydropyrimidine derivatives 3a, b and 4a–c as cyclic 1,3-diamines under two reaction conditions (A and B) is described. Under reaction conditions-A, a suspension of (E)-2-cyano-2-(oxazolidin-2-ylidene)ethanethioamide 1 (1 eq.) and diaminoalkanes 2a–e (2 eq.) in absolute ethanol is heated under reflux for 16–22 h to afford 3a, b and 4a–c. Alternatively, under reaction conditions-B, a solution of thioamide 1 (1 eq.) in diaminoalkanes 2a–e (3 eq.) is stirred under solvent-free conditions at room temperature for 3 days to give desired products. Reaction conditions-A for having higher yields, shorter reaction times, and required less diamines is more effective than reaction conditions-B. Oxazolidine ring opening is observed by reacting compound 1 with all of the diamines 2a–e, but the thioamide group only reacts with nonbulky diamines 2a, b. The chemical structures of novel compounds were confirmed by 1H NMR, 13C NMR, elemental analysis, and FT-IR spectrometry.

Synthesis and characterization of N-glucosylated dithiadiazepine derivatives through carbon-sulfur bond formation

2015 ◽  
Vol 21 (5) ◽  
pp. 269-272 ◽  
Author(s):  
Snehal A. Chavan ◽  
Avinash G. Ulhe ◽  
Baliram N. Berad
Keyword(s):  
Bond Formation ◽  
Synthesis And Characterization ◽  
Mass Spectral ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
New Compounds ◽  
Sulfur Bond ◽  
C Nmr

AbstractNew 4,7-bis(arylamino)-2-tetra-O-acetyl-β-d-glucopyranosylimino-1,3,5,6-dithiadiazepines were synthesized via reaction of N-tetra-O-acetyl-β-d-glucopyranosyl isocyanodichloride with 1,6-diaryl-2,5-dithio-bis-ureas without using any catalyst. Thus, the synthesis of 7-membered heterocycles containing two sulfur and two nitrogen atoms through carbon-sulfur bond formation was explored. The chemical structures of these new compounds were elucidated by IR, 1H NMR, 13C NMR, mass spectral, and elemental analyses.

Synthesis of Bis(2, 4-Dihydro-2H-3-(4-N-Maleimido) Phenyl -1, 3-Benzoxazine)Isopropane

2011 ◽  
Vol 287-290 ◽  
pp. 688-693
Author(s):  
Guo Tao ◽  
You Hui Xu ◽  
Gang Yang
Keyword(s):  
Maleic Anhydride ◽  
Target Object ◽  
The Novel ◽  
H Nmr ◽  
Chemical Structures ◽  
Ft Ir

The novel bis(2, 4-dihydro-2H-3-(4-N-maleimido) phenyl-1, 3-benzoxazine)isopropane (BMIPBI) was synthesized from maleic anhydride, p-nitroaniline, formaldehyde and 2,2-bis(4-hydr -oxyphenyl)propane by a few steps reactions via the N-(4-nitrophenyl)maleimide(NPMI), N-(4-amin -ophenyl)maleimide(APMI),1,3,5-three(4-(maleimido)phenyl)-1,3,5-triazine(TMIPT)intermediate production. The chemical structures of BMIPBI were confirmed by 1H-NMR, FT-IR and EA. The results show that the production was the target object BMIPBI. The synthesized condition had been studied too. The BMIPBI was a loosened yellow solid and the yield of product was 58.8%.

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