scholarly journals Syntheses and Studies of 8-Substituted-2-(2-Chlorophenyl/3-chlorophenyl)- 4-(4-hydroxyphenyl/phenyl)-2,3/2,5-dihydro-1,5-benzothiazepines

2021 ◽  
Vol 33 (11) ◽  
pp. 2653-2656
Author(s):  
Seema Pant ◽  
Pushpa Godwal ◽  
Kumari Sanju

Syntheses of novel twelve 8-substituted-2-(2-chlorophenyl/3-chlorophenyl)-4-(4-hydroxyphenyl/ phenyl)-2,3/2,5-dihydro-1,5-benzothiazepines have been carried out by the reactions of 5-substituted 2-aminobenzenethiols, the substituents being fluoro, chloro, bromo, methyl, methoxy or ethoxy with α,β-unsaturated ketones, 3-(2-chlorophenyl)-1-(4-hydroxyphenyl)-2-propenone or 3-(3-chloro-phenyl)-1-phenyl-2-propenone in dry ethanol in acidic medium in quest for the synthesis of 1,5-benzothiazepine compounds, which may have interesting biological activities. The precursors, substituted α,β-unsaturated ketones were obtained by employing the Claisen-Schmidt reaction; and the final products, obtained by Michael condensation, were characterized by analytical and spectral data comprising IR, 1H NMR and mass spectral studies. Two different series, 2,3-dihydro and 2,5-dihydro series of the final compounds were obtained depending on the substituents present, as indicated by the 1H NMR spectra. The newly synthesized compounds were studied for their antimicrobial activities against Staphylococcus aureus, Escherichia coli and Candida albicans taking imipenem, vancomycin and fluconazole as reference standards using Paper Disc method. Five of the compounds tested showed good antifungal activity against Candida albicans at the concentration of 200 μg/disc.

2019 ◽  
Vol 11 (1) ◽  
pp. 43
Author(s):  
Festus Sunday Fabiyi ◽  
Friday O. Nwosu

Six new mixed-ligand complexes of Mo(IV) and W(IV) ions have been prepared and characterized. The three new complexes of Mo(IV) ions have the molecular formulae MoC12N2O5H18, MoC15N2O5H22 and MoC14N2O6H19 , while the W(II) ions are WC12N2O5H18, WC15N2O5H22 and WC14N2O6H19. The structures of the complexes were deduced from their ir, 1H nmr, and mass spectral studies. All the complexes were found to exhibit octahedral structures. Their antimicrobial activities against some bacteria and fungi species were found to be moderate.


2020 ◽  
Vol 33 (1) ◽  
pp. 127-131
Author(s):  
Riddhi A. Nayak ◽  
Anvita D. Mangte

In view of applications of N-glycosylated compounds in medicinal chemistry and in many other ways, herein the synthesis of novel N-glycosyl hydrazino carbothioamides is reported. New N-glycosyl hydrazino carbothioamides were synthesized by the condensation of per-O-acetyl glycosyl isothiocyanate with different aromatic hydrazides. The newly synthesized compounds were characterized by using the IR, 1H NMR and mass spectral studies. Antimicrobial evaluation of the synthesized N-glycosyl hydrazino carbothioamide was also examined. Antimicrobial activities of the synthesized compound were evaluated against bacteria E. coli, P. aeruginosa, S. aureus, S. pyogenus and fungi C. albicans, A. niger and A. clavatus. All the N-glycosyl hydrazino carbothioamides exhibit promising antimicrobial activity.


2019 ◽  
Vol 74 (6) ◽  
pp. 473-478 ◽  
Author(s):  
Abd El-Galil E. Amr ◽  
Ahmed M. Naglah ◽  
Nermien M. Sabry ◽  
Alhussein A. Ibrahim ◽  
Elsayed A. Elsayed ◽  
...  

AbstractInterest in the synthesis of heterocyclic organic molecules with peptide moieties has gained attention due to their potential biological activities. The current work aimed at synthesizing new macrocyclic tripeptide imides and evaluating their possible antimicrobial activities. A series of 11 derivatives were prepared from dimethyl 3,5-pyridinevalinyl ester either by NaOH or NH2NH2 treatment, followed by cyclization and further reaction with NaOH or NH2NH2. The majority of synthesized derivatives showed promising antibacterial and antifungal activities in comparison to standard known antibiotics. Compounds 5a and 7b showed the most potential antibacterial against Staphylococcus aureus and antifungal activities against Candida albicans, respectively.


2019 ◽  
Vol 31 (5) ◽  
pp. 1087-1090 ◽  
Author(s):  
Pradip P. Deohate ◽  
Roshani S. Mulani

Microwave irradiative synthesis of triazine substituted pyrazoles i.e. (4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-(5-methyl-2-substituted benzoyl/isonicotinoyl/cinnamoyl-pyrazol-3-yl)-amines have been achieved by the cyclocondensation of N-(4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-3-oxo butyramide with substituted acid hydrazides. Synthesis of required butyramide was done by reacting 2,4-diamino-6-methyl-[1,3,5]-triazine with benzaldehyde and then condensing the product with ethyl acetoacetate. Structural investigation of synthesized compounds has been done by chemical transformation, elemental analysis and IR, 1H NMR, mass spectral studies. Study of antitubercular and antimicrobial activity of title compounds against some selected Gram-positive and Gram-negative microorganisms was performed to establish the relationship between structure and activity of compound.


2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Mohammed M. Ansari ◽  
Shirish P. Deshmukh ◽  
Rizwan Khan ◽  
Mohammed Musaddiq

A series of S-benzyl aryl thiourea were condensed with o-Methoxy phenyl isocyanate to yield respective isothiobiuret derivatives. The newly synthesized compounds were characterized by 1H-NMR, IR, and Mass Spectral studies and tested for biological activities.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Reena Jain ◽  
Rajeev Singh ◽  
N. K. Kaushik

A new series of organotin(IV) complexes with purine bases theophylline (HL1) and theobromine (L2) of the types R3Sn(L1), R2Sn(L1)Cl, R3Sn(L2)Cl, and R2Sn(L2)Cl2(R = C6H5CH2–;p-ClC6H4CH2–) have been synthesized in anhydrous THF. The complexes were characterized by elemental analysis, conductance measurements, molecular weight determinations, UV-vis, IR,1H,13C NMR, and mass spectral studies. Various kinetic and thermodynamic parameters of these complexes have also been determined using TG/DTA technique. The thermal decomposition techniques indicate the formation of SnO2as a residue. The results show that the ligands act as bidentate, forming a five-member chelate ring. All the complexes are 1 : 1 metal-ligand complexes. In order to assess their antimicrobial activity, the ligands and their corresponding complexes have also been testedin vitroagainst bacteria (E. coli, S. aureus, andP. pyocyanea) and fungi (Rhizopus oryzaeandAspergillus flavus). All the complexes exhibit remarkable activity, and the results provide evidence that the studied complexes might indeed be a potential source of antimicrobial agents.


2014 ◽  
Vol 37 (2) ◽  
pp. 219-229
Author(s):  
Shah Mohammad Fatah-Ur Rahman ◽  
Farah Shahjin ◽  
Koushi Fukunishi

A novel thioindigo dye was synthesized, from 7, 7’-bis-chlorocarbonyl thioindigo, containing OH groups at the terminal positions of the oxyethylene side chains. The resultant dye 7, 7’-Bis[[2- [2-(2-hydroxyethoxy)ethoxy]ethoxycarbonyl]thioindigo (1) was characterized by 1H NMR, IR, and mass spectral studies. The thioindigo derivative (1), which possesses a molecular architecture, undergoes reversible photochromic reaction and capable of capturing different metal ions and transports them through liquid membrane. Enhancement of binding ability (i) by incorporating OH groups instead of large phenyl or methyl groups, (ii) by trans to cis photoisomerization of (1), iii) the highest amount of transported Ag+ by (1) across a liquid membrane when irradiated with 550 and 480 nm light alternately, were found. DOI: http://dx.doi.org/10.3329/jbas.v37i2.17564 Journal of Bangladesh Academy of Scinces, Vol. 37, No. 2, 219-229, 2013


2019 ◽  
Vol 31 (9) ◽  
pp. 2015-2021
Author(s):  
Ashok K. Singh ◽  
Suresh K. Patel ◽  
Asif Jafri

A series of eight Co(III) complexes [CoL1-8(H2O)2Cl] (I-1 to I-8) incorporating 4-(2-substituted phenylimino)-2-(4-substituted phenyl)-4H-chromen-3-ol, as a tridentate imino flavone ligands (L1 to L8, 2-sub. = NH2, SH, 4-sub. = OMe, OH, Cl, NMe2) have been synthesized, characterized and the geometry of the complexes were optimized by DFT. The chemical structure of synthesized imino flavone ligands and their complexes were characterized by elemental analysis, 1H NMR, 13C NMR, UV-visible, IR, ESI-mass spectral data, conductometric and magnetic measurements. The synthesized compounds have been screened for their in vitro antibacterial activities against bacteria Vibrio cholerae, Salmonella typhi, Staphylococcus aureus, Escherichia coli and antifungal activities against fungi Candida albicans and Aspergillus flavus by paper disc diffusion method. The complexes I-3, I-4, I-7 and I-8 showed good antimicrobial activities against pathogens.


2020 ◽  
Vol 12 (5) ◽  
pp. 695-701
Author(s):  
Sonika Sharma ◽  
Neeraj Sharma

The tris(nicotinohydroxamato) vanadium(III) complex of composition [V(C5H4NCONHO)3] have been synthesized by the reaction of VCl3 with three equivalents of potassium salts of nicotinohydroxamate in methanol medium under nitrogen atmosphere. The characterization of complex has been accomplished by elemental analyses, molar conductivity, magnetic moment measurements, IR, electronic and mass spectral studies. An octahedral geometry around vanadium, inferred from physicochemical and spectral studies has been proposed for complex. The antimicrobial activities of the newly synthesized complex, ligand and precursor VCl3 have been evaluated against some pathogenic bacteria as E. coli, S. aureus, S. typhi, S. paratyphi, S. epidermidis and K. pneumoniae and fungi such as A. niger, B. fulva and M. circinelloid by minimum inhibitory concentration method. The complex exhibited promising antimicrobial activity relative to free ligand and metal precursor.


Author(s):  
Priyanka Bhatt ◽  
S. Deepthi ◽  
Ch. Ravi Shankar Kumar ◽  
Anjali Jha

Objective: A facile synthesis of some novel Schiff base derivatives of 2-substituted-5-amino-thiadiazoles along with their Ni (II), Cu (II), and Pd (II) complexes were achieved by sonication and the conventional method. In addition to establish the structure by DFT studies and to explore antimicrobial and anticancer activities of these novel compounds.Methods: The precursor 2-substituted-5-amino-thiadiazoles (T1-T3), target ligands and their metal complexes were synthesized by ultra-sonication and conventional means. The isolated products were thoroughly characterized by physical and spectroscopic techniques including 1H-NMR, [13]C-NMR and IR spectroscopy. All characterized compounds were screened for antimicrobial activities using well diffusion method, and MTT assay was performed for cytotoxicity.Results: All novel compounds were synthesized by a green route i.e. ultra sonication and a noticeable improvement in yield with shorter reaction time than the conventional method were observed. The octahedral geometry was proposed for Ni (II)/Cu (II) complexes whereas square planar for Pd (II) complexes on the basis of the spectral techniques which were supported by DFT analysis by Gaussian03. On the analysis of antimicrobial activities, the compound T7 and T10 showed maximum antibacterial and antifungal activities respectively. However, compounds T25, T37, T31 found to be a potential cytotoxic compound with IC50 value 0.469, 0.865 and 1.131 μM respectively.Conclusion: Analysis of synthetic protocol, it could be concluded that ultra-sonication is the better method to synthesize these potential biological active moiety. On the whole Cu (II) and Ni (II) complexes showed promising activity towards all microorganisms while Pd (II) complex emerged an excellent moiety in carcinoma cell line.


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