Synthesis of Novel Oxazin Analogs of Thio-4-azaspiro[4.5]decan-3-one for their Antimicrobial Activity

2021 ◽  
Vol 6 (2) ◽  
pp. 116-120
Author(s):  
Raj Bahadur Singh ◽  
Krishna Srivastava ◽  
Ram Prakash Tiwari ◽  
Jyoti Srivastava
Keyword(s):  
Antimicrobial Activity ◽  
Hydrazine Hydrate ◽  
1H Nmr ◽  
Absorption Spectroscopy ◽  
Elemental Analysis ◽  
Spectral Studies ◽  
Good Activity ◽  
Mass Spectral ◽  
E Coli

The present work reports the synthesis of 4-(1-(substituted phenyl)-1H-naphtho[1,2-e][1,3]oxazin- 2(3H)-yl)-1-thia-4-azaspiro-[4.5]-decan-3-one IV(a-h) by 4-(((substituted phenyl)(2-hydroxynaphthalen- 1-yl) ethyl)amino)-1-thia-4-azaspiro[4.5]decan-3-one with formaldehyde in acetonitrile, containing a spiro ring obtained from the reaction of cyclohexylidene hydrazine and thioglycollic acid in DMF (cyclohexanone reacts with hydrazine hydrate in pyridine). The structures of the synthesized compounds have been established on the basis of elemental analysis, UV-vis absorption spectroscopy, IR, 1H NMR and mass spectral studies. The in vitro antimicrobial screening of all novel compounds was done against S. aureus, E. coli, P. aeruginosa and B. subtilis. The activity of compounds IVb, IVc, IVe and IVf compounds showed moderate to good activity against the tested microbes.

scholarly journals Synthesis and Antimicrobial Studies of Novel N-Glycosyl Hydrazino Carbothioamide

2020 ◽  
Vol 33 (1) ◽  
pp. 127-131
Author(s):  
Riddhi A. Nayak ◽  
Anvita D. Mangte
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
Medicinal Chemistry ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Mass Spectral ◽  
E Coli ◽  
Antimicrobial Studies ◽  
Antimicrobial Evaluation

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.

scholarly journals Green Synthetic Protocol for (E)-1-Aryl-3-(2-morpholinoquinolin- 3-yl)prop-2-en-1-ones and Their Antimicrobial Activity

2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
13C Nmr ◽  
Mass Spectral Data ◽  
In Vitro Antimicrobial Activity ◽  
Mass Spectral ◽  
Fungal Organisms

We report here an easy, efficient and green synthetic protocol for the (E)-1-aryl-3-(2-morpholinoquinolin-3-yl)prop-2-en-1-ones by the Claisen-Schmidt condensation of 2-morpholinoquinoline-3-carbaldehyde and different substituted acetophenones by using 1-butyl-3-methylimidazolium tetrafluoroborate (Bmim)BF4. The compounds were characterized by using 1H NMR, 13C NMR and mass spectral data and screened there in vitro antimicrobial activity against different bacterial and fungal organisms.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NEWER BENZIMIDAZOLE DERIVATIVES BY MANNICH REACTION

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (07) ◽  
pp. 16-22
Author(s):  
N. Kumar ◽  
D Pathak ◽  
Keyword(s):  
Salicylic Acid ◽  
Elemental Analysis ◽  
Mannich Reaction ◽  
Anthelmintic Activity ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Good Activity ◽  
Mass Spectral Data ◽  
Mass Spectral

O-phenylenediamine and salicylic acid were used for the synthesis of 2-(1-(substituted phenylamino) methyl-1H benzo[d] imidazol-2-yl) phenol (2a-2h) derivatives by using various substituted aniline. In the first step, reaction of o-phenylenediamine and salicylic acid yielded 2-(1H-benzo[d]imidazol-2-yl) phenol (1), which on Mannich reaction with substituted aniline gave compounds (2a-2h). The structures of these compounds were characterized by IR, 1H NMR, mass spectral data and elemental analysis. Each analogue was tested in vitro for various types of pharmacological activity of this class of drugs including antibacterial, antifungal and anthelmintic activity. Among the synthesized compounds 2a act as vermifuge and no compound was found to be a vermicide. The compound 2c was found to be most active against E.coli and P. aeurigenosa and 2e be most active against B.subtilis and S.aureus. The derivative 2h shows good activity against C.albicans and A.niger.

scholarly journals Microwave Irradiative Synthesis of Triazine Substituted Pyrazoles and Study of Antitubercular and Antimicrobial Activities

2019 ◽  
Vol 31 (5) ◽  
pp. 1087-1090 ◽  
Author(s):  
Pradip P. Deohate ◽  
Roshani S. Mulani
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Structural Investigation ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Gram Negative ◽  
Mass Spectral ◽  
The Relationship ◽  
Substituted Pyrazoles ◽  
Structure And Activity

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.

scholarly journals A Facial Synthesis and Antimicrobial Activity of Some Pyrazole Derivatives Carrying Indole

2010 ◽  
Vol 7 (3) ◽  
pp. 745-750 ◽  
Author(s):  
K. Narasimha Sarma ◽  
M. C. S. Subha ◽  
K. Chowdoji Rao
Keyword(s):  
Antimicrobial Activity ◽  
Acetic Acid ◽  
Carboxylic Acid ◽  
Hydrazine Hydrate ◽  
Elemental Analysis ◽  
Antimicrobial Activities ◽  
Subsequent Treatment ◽  
Spectral Studies ◽  
Pyrazole Derivatives

The title compounds (7a-h) were prepared by esterification of indole-5-carboxylic acid (1) and subsequent treatment with hydrazine hydrate in methanolviathe hydrazide (3). Finally hydrazide (3) condensed with different substituted aldol (6) in acetic acid / PTSA catalytic media produced (3,5-subsituted-4,5-dihydropyrazol-1-yl)(1H-indol-5-yl)methanone (7a-h) in good yields. All the newly synthesized compounds are by elemental analysis and spectral studies and evaluated for antimicrobial activities.

scholarly journals Synthesis, Characterization, and Thermal and Antimicrobial Activities of Some Novel Organotin(IV): Purine Base Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Reena Jain ◽  
Rajeev Singh ◽  
N. K. Kaushik
Keyword(s):  
Antimicrobial Agents ◽  
Rhizopus Oryzae ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Purine Base ◽  
Mass Spectral ◽  
E Coli ◽  
Kinetic And Thermodynamic Parameters ◽  
C Nmr

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.

scholarly journals Synthesis, antimicrobial and antimalarial activityof1, 4-benzothiazepine and pyrazolinederivatives incorporating carbazolemoiety

2019 ◽  
Vol 51 (2) ◽  
pp. 234-241
Author(s):  
V. A. Kadnor ◽  
S. N. Shelke
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
13C Nmr ◽  
Antimalarial Activity ◽  
Positive Control ◽  
Spectral Studies ◽  
Standard Drug ◽  
Mass Spectral ◽  
Ft Ir

A series of carbazole-based 1,4-benzothiazepine and pyrazoline derivatives were synthesized and the structures of the newly synthesized compounds were confirmed by FT-IR, 1H NMR, 13C NMR and mass spectral studies. All new derivatives 4(a-f) and 5(a-e) were screened for their in vitro antimicrobial activity, and also for their antimalarial activity. Compounds 4a, 4b, 4d, 5a, 5b and 5c exhibited promising antimicrobial and antimalarial activities as compared to positive control. Notably, compounds 4a, 4b and 4d showed excellent antifungal activity against Penicillium sp. comparable to that of a standard drug.

scholarly journals Synthesis and Antimicrobial Screening 6-Aryl-2-(Amino/Methoxy)-4-[(4′-Difluoro Methoxy) (3′-Hydroxy) Phenyl] Nicotinonitrile

2015 ◽  
Vol 50 ◽  
pp. 35-42 ◽  
Author(s):  
Vijay N. Bhadani ◽  
Piyush A. Patel ◽  
Heta D. Purohit ◽  
Dipak M. Purohit
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Sodium Methoxide ◽  
Ammonium Acetate ◽  
Mass Spectral Data ◽  
Antimicrobial Screening ◽  
Mass Spectral ◽  
Efficient Route

A series of an easy and efficient route for the synthesis of some new 2-amino-3-cyanopyridine (4a-4i) and 2-methoxy-3-cyanopyridine (5a-5i) derivatives were synthesized through the reaction of various chalcone (3a-3i) with malononitrile in presence of ammonium acetate and sodium methoxide, respectively. The constitutions of the all synthesized compounds have been established by the IR, 1H-NMR, Mass spectral data and Elemental analysis. Furthermore, all the synthesized products were screened for their antimicrobial activity.

Synthesis, Characterization and Evaluation of Azetidinylquinolines and Thiazolidinylquinolines as Antibacterial Agents

2014 ◽  
Vol 7 (3) ◽  
pp. 2536-2543
Author(s):  
Shalabh Sharma ◽  
Kuldeep K Saxena
Keyword(s):  
Antibacterial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Antibacterial Agents ◽  
Mass Spectral Data ◽  
Standard Drug ◽  
Mass Spectral ◽  
New Compounds

Several molecules were synthesized like 8-ethoxy-4-methyl-2-amino-(3’-chloro-2’-oxo-4’-substitutedaryl-1’-azeti-dinyl)-quinolines 8-12 and 8-ethoxy-4-methyl-2-amino-(2’-substitutedaryl-4’-oxo-1’,3’-thiazolidin-3’-yl)quinolines 13-17 from 8-ethoxy-4-methyl-2-(substitutedarylidenylimino amino)-quinolines 3-7, and screened to evaluate their antibacterial activity against numerous strains of bacteria        in vitro. The structures of new compounds were established on the basis of their elemental analysis, IR, 1H-NMR and mass spectral data. The results showed that three compounds 10, 11 and 16 were found to exhibit promising antibacterial activity as compared to the standard drug amphicillin.   

Synthesis, Characterization and in vitro Antimicrobial Evaluation of Pyrazole Based Oxothiazolidine Hybrids

2020 ◽  
Vol 5 (4) ◽  
pp. 295-300
Author(s):  
Yogesh J. Sanghani ◽  
Suresh B. Koradiya ◽  
Krushnakumar J. Jilariya
Keyword(s):  
Diffusion Method ◽  
Spectral Studies ◽  
Zone Of Inhibition ◽  
Disk Diffusion Method ◽  
Mass Spectral ◽  
E Coli ◽  
Antifungal Potential ◽  
Antimicrobial Evaluation ◽  
Antibacterial And Antifungal

In this work, pyrazole based oxothiazolidine hybrids, 4-{4-[2-(1- phenyl-3-(substituted)phenyl-1H-pyrazol-4-yl)-4-oxo-thiazolidin-3- yl]-phenyl}-morpholin-3-one (11a-l) were synthesized using molecular hybridization approach through Vilsmeier-Haack reaction. The titled compounds 11a-l were characterized by elemental analysis, IR, 1H NMR and mass spectral studies. The antibacterial activity of 11a-l was evaluated in vitro by agar cup plate method against B. cocous, B. subtillis, E. coli and P. vulgaris. The antifungal activity of compounds 11a-l was evaluated in vitro by agar based disk diffusion method against A. niger. The results of antibacterial and antifungal evaluation were reported in terms of zone of inhibition measured in mm. The synthesized compounds 11a-l exhibited moderate to good antibacterial and antifungal potential. Compound 4-{4-[2-(1-phenyl-3-(2-methoxyphenyl) phenyl-1H-pyrazol-4-yl)-4-oxo-thiazolidin-3-yl]-phenyl}- morpholin-3-one (11h) emerged as a most potent antimicrobial agent displaying zone of inhibition 21, 20, 21, 24 and 20 mm against B. cocous, B. subtillis, E. coli, P. vulgaris and A. niger, respectively.

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