Synthesis and Antimicrobial Activity of Some Derivatives of 5‐Substituted Indole Dihydropyrimidines

Heda, Lalchand; Pareek, Chandresh; Chaudhari, P. B.

doi:10.1155/2009/893812

Cited by 17 publications

(13 citation statements)

References 3 publications

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“…The novel series of indole dihydropyrimidine derivatives ( 134 ) were synthesized by Heda et al and screened for their in vitro antibacterial activity against E. coli and P. aeruginosa and in vitro antifungal activity against A. niger and Fusiform oxyporum . The MIC was determined which showed promising results when compared with the standard drug [ 151 ]. The novel series of substituted 6-n-propyl thiouracils was synthesized by Prachayasittikul et al and screened for in vitro antibacterial, antimalarial activities and as cytotoxic agents.…”

Section: In Vitro Antimicrobial Activity Profilmentioning

confidence: 99%

Significance and Biological Importance of Pyrimidine in the Microbial World

Sharma

Chitranshi

Agarwal

2014

International Journal of Medicinal Chemistry

209

160

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Microbes are unique creatures that adapt to varying lifestyles and environment resistance in extreme or adverse conditions. The genetic architecture of microbe may bear a significant signature not only in the sequences position, but also in the lifestyle to which it is adapted. It becomes a challenge for the society to find new chemical entities which can treat microbial infections. The present review aims to focus on account of important chemical moiety, that is, pyrimidine and its various derivatives as antimicrobial agents. In the current studies we represent more than 200 pyrimidines as antimicrobial agents with different mono-, di-, tri-, and tetrasubstituted classes along with in vitro antimicrobial activities of pyrimidines derivatives which can facilitate the development of more potent and effective antimicrobial agents.

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Section: In Vitro Antimicrobial Activity Profilmentioning

confidence: 99%

Significance and Biological Importance of Pyrimidine in the Microbial World

Sharma

Chitranshi

Agarwal

2014

International Journal of Medicinal Chemistry

209

160

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“…Solvents were purified and dried before being used. The required substituted 2-phenyl- N -allyl-indole-3-carbaldehyde 1a–d was prepared by the Vilsmeier–Haack reaction according to the procedure in the literature [ 40 ]. All melting points were taken in open capillaries and are uncorrected.…”

Section: Methodsmentioning

confidence: 99%

An efficient synthesis of 4 H -pyrano quinolinone derivatives catalysed by a versatile organocatalyst tetra- n -butylammonium fluoride and their pharmacological screening

Prasad¹,

Shobhashana²,

Patel³

2017

R. Soc. open sci.

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A new series of indole-based pyranoquinoline derivatives P1–24 has been synthesized by a one-pot cyclocondensation reaction of 2-(4-substituted)phenyl-N-allyl-indole-3-carbaldehydes 1a–d; active methylenes 2a–c; and 4-hydroxy-1-substituted quinolin-2(1H)-one 3a–b catalysed by an organocatalyst tetra-n-butylammonium fluoride (TBAF) in aqueous ethanol. The easy experimental procedure of the reaction leads to excellent yields of pyranoquinoline derivatives. All the compounds were screened against a representative panel of bacteria and fungi. Some of the compounds are found to be equipotent or more potent than standard drugs as evident from the structural activity relationship study.

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“…The screening consequences revealed as the newly designed compounds (11a-g) containing halogen groups have shown significant antibacterial [17] and antifungal activity compared to corresponding standard drugs. It reveals that the metformin residue and the indole site attached to the compounds may increase the antimicrobial activities [18][19][20][21][22][23] of the entire compounds (11a-g).…”

Section: In Vitro Antimicrobial Activitymentioning

confidence: 99%

Synthesis, Characterisation, Molecular Docking, Anti-microbial and Anti-diabetic Screening of Substituted 4-indolylphenyl-6-arylpyrimidine-2-imine Derivatives

et al. 2017

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The purpose of the research is to synthesise a novel series of (E)-2-(4-(1H-indol-3-yl)-6-p-substituted phenylpyrimidin-2-yl)dimethylguanidine derivatives since 3-(1H-indol-3-yl)-1-p-substituted phenylprop-2-en-1-one and evaluate their molecular docking studies, antimicrobial, and anti-diabetic activities. Among all the synthesized compounds (), compound exhibits excellent CDOCKER energy (-11.36 kcal/mol). The entire compounds () confirm very good antimicrobial activity towards the tested microorganisms. In the in vitro anti-diabetic studies, compounds confirm higher alpha-amylase and alpha-glucosidase inhibition activity. In the in vivo anti-diabetic activities, the synthesized compounds (10 mg/kg, p.o.) investigated by the streptozotocin (60 mg/kg, ip) -nicotinamide (120 mg/kg, p.o.) - induced model in adult male albino Wistar rat and these derivatives show considerable fasting blood glucose level when compared to metformin hydrochloride a potent and well-known anti-diabetic drug as a reference.

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Synthesis and Antimicrobial Activity of Some Derivatives of 5‐Substituted Indole Dihydropyrimidines

Cited by 17 publications

References 3 publications

Significance and Biological Importance of Pyrimidine in the Microbial World

Significance and Biological Importance of Pyrimidine in the Microbial World

An efficient synthesis of 4 H -pyrano quinolinone derivatives catalysed by a versatile organocatalyst tetra- n -butylammonium fluoride and their pharmacological screening

Synthesis, Characterisation, Molecular Docking, Anti-microbial and Anti-diabetic Screening of Substituted 4-indolylphenyl-6-arylpyrimidine-2-imine Derivatives

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