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

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.

2010 ◽  
Vol 7 (3) ◽  
pp. 745-750 ◽  
Author(s):  
K. Narasimha Sarma ◽  
M. C. S. Subha ◽  
K. Chowdoji Rao

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.


2015 ◽  
Vol 70 (1-2) ◽  
pp. 45-50
Author(s):  
Asu Usta ◽  
Hacer Taşkıran

Abstract N-alkyl substituted 2′,3″-thiazachalcones {3-[(1E)-3-(4-methylthiophene-2-yl)-3-oxoprop-1-en-1-yl]-1-alkyl (C5–12,14) pyridinium bromides} were synthesized by a two-step reaction. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, elemental analysis and mass spectral studies. The synthesized compounds were tested for antibacterial activities and found to be more active against Gram-positive as compared to Gram-negative bacteria.


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.


2021 ◽  
Vol 6 (2) ◽  
pp. 116-120
Author(s):  
Raj Bahadur Singh ◽  
Krishna Srivastava ◽  
Ram Prakash Tiwari ◽  
Jyoti Srivastava

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.


2011 ◽  
Vol 4 (1) ◽  
pp. 183 ◽  
Author(s):  
R. V. Antre ◽  
A. Cendilkumar ◽  
R. R. Nagarajan ◽  
D. Goli ◽  
R. J. Oswal

Several 1-(substituted)-3-methyl-1H-pyrazol-5(4H)-one as RA1-RA9 were synthesized and compounds were screened for antitumor activity against Ehrlich ascites carcinoma (EAC) cells and antimicrobial activity. Elemental analysis, mass spectral data, 1H-NMR, and IR confirmed the structure of the newly synthesized compounds. Some of the tested compounds showed good antitumor and antimicrobial activity. Compounds RA1, RA4, and RA9 exhibit highest antitumor activity against EAC cells in comparison with 5-flurouracil as standard drug.Keywords: Ehrlich ascites carcinoma; Pyrazolone; Antitumor; N-substitution; Antimicrobial.© 2012 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi: http://dx.doi.org/10.3329/jsr.v4i1.7027 J. Sci. Res. 4 (1), 183-192 (2012)


2018 ◽  
Vol 69 (4) ◽  
pp. 815-822 ◽  
Author(s):  
Lucia Pintilie ◽  
Amalia Stefaniu ◽  
Alina Ioana Nicu ◽  
Maria Maganu ◽  
Miron Teodor Caproiu

A new series of fluoroquinolone compounds have been obtained by Gould-Jacobs method. The compounds have been characterized by physic-chemical methods (elemental analysis, FTIR, NMR, UV-Vis) and by antimicrobial activity against Gram-positive and Gram-negative microorganisms. For the synthesized compounds have been performed calculations of characteristics and molecular properties, using Spartan�14 Software from Wavefunction, Inc. Irvine, CA. and molecular docking studies using CLC Drug Discovery Workbench 2.4 software, to identify and visualize the most likely interaction ligand (fluoroquinolone) with the receptor protein.


Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2793 ◽  
Author(s):  
Ameen Abu-Hashem

Substituted-6-methyl-1-thioxo-1,2-dihydro-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-ones (5a,b) were synthesized from condensation of visnagenone (2a) or khellinone (2b) with 6-amino-thiouracil (3) in dimethylformamide or refluxing of (4a) or (4b) in dimethylformamide. Hence, compounds (5a,b) were used as the starting materials for preparing many new heterocyclic compounds such as; furo[3,2-g]pyrimido[1,6-a]quinazoline (6a,b), furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazolinone (7a,b), substituted-benzylidene-furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazoline-3,5-dione (8a–f), 3-oxo-furo[3,2-g]pyrimido[1,6-a]quinazoline-pentane-2,4-dione (9a,b), 1-(pyrazole)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (10a,b), 2-(oxo or thioxo)-pyrimidine-furo[3,2-g]pyrimido[1,6-a]quinazolinone (11a–d), 1-(methylthio)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (12a,b), 1-(methyl-sulfonyl)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (13a,b) and 6-methyl-1-((piperazine) or morpholino)-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-one (14a–d). The structures of the prepared compounds were elucidated on the basis of spectral data (IR, 1H-NMR, 13C-NMR, MS) and elemental analysis. Antimicrobial activity was evaluated for the synthesized compounds against Gram-positive, Gram-negative bacteria and fungi. The new compounds, furothiazolo pyrimido quinazolines 8a–f and 11a–d displayed results excellent for growth inhibition of bacteria and fungi.


2021 ◽  
Vol 68 (4) ◽  
pp. 1008-1015
Author(s):  
Yong Yuan ◽  
Xi-Kun Lu ◽  
Gao-Qi Zhou ◽  
Xiao-Yang Qiu

Three new copper(II) complexes, [Cu(LH)2]Br2 (1), [Cu(LH)2]NCS2 (2), and [Cu(LH)2](NO3)2 (3), where LH is the zwitterionic form of 2-bromo-6-((2-(isopropylamino)ethylimino)methyl)phenol (HL), were synthesized and characterized by elemental analysis, IR and UV-vis spectroscopy. The structures of the complexes were further confirmed by single crystal X-ray structure determination. All compounds are mononuclear copper(II) complexes. The Cu atoms in the complexes are coordinated by two imino N and two phenolate O atoms from two LH ligands, forming square planar coordination. The compounds were assayed for their antimicrobial activities.


2012 ◽  
Vol 9 (1) ◽  
pp. 481-486
Author(s):  
K. Anuradha ◽  
R. Rajavel

Novel Cu(II),Ni(II) and VO(II) complexes are synthesized with N1,N4-bis(2-aminobenzylidene)benzene-1,4-diamine (L). Complexes were characterized by elemental analysis, molar conductance, IR, UV and EPR. Spectral studies reveals a square planner geomentry for Cu(II), Ni(II) complexes and square pyramidal for VO(II) complex. The ligand and its complexes were also evaluated against the growth of gram positive bacteria and gram negative bacteria.


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