In vitro antimicrobial activity screening of new Heterocyclic compounds derived from 5-bromo-2,3-di(furan-2-yl)-1h-indole

This article describes the antimicrobial activity evaluation of new heterocyclic compounds derived from 5-bromo-2,3-di(furan-2-yl)-1h-indole. Heterocyclic moiety serve as perfect framework on which pharmacophores can be effectively attached to produce novel drugs. New compounds were obtained on the basis of derivatives including 1H-indole-2,3-dione derivatives. Acid-catalyzed, three-component reaction (Belinelli synthesis) between 5-bromo-2,3-di(furan-2-yl)1H-indole, acetylacetone and semi carbazide, thiosemicarbazone, urea, thiourea, guanidine constitutes a rapid and facile synthesis of corresponding tetrahydro pyrimidines, which are interesting compounds with a potential for pharmaceutical application. Antimicrobial tests revealed high antibacterial activity of obtained derivatives. The synthesized compounds have been screened for their in vitro antimicrobial activity against various strains of bacteria and fungi. Keywords: Vitro; Heterocyclic Compounds; Antimicrobial

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Synthesis and in vitro antimicrobial activity of new steroidal hydrazone derivatives

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-021-00391-4 ◽

2022 ◽

Vol 8 (1) ◽

Author(s):

Shailesh Mistry ◽

Akhilesh Kumar Singh

Keyword(s):

Antimicrobial Activity ◽

Infectious Diseases ◽

Antimicrobial Agent ◽

Spectral Data ◽

Induced Resistance ◽

Antimicrobial Agents ◽

In Vitro Antimicrobial Activity ◽

Bacteria And Fungi ◽

New Compounds

Abstract Background For many years, various drugs have been used for the treatment of infectious diseases but some bacterial microorganisms have induced resistance to several drugs. In a search of new antimicrobial agents, a series of new steroidal hydrazones were designed and synthesized. Result The structures of the compounds were established based on the spectral data. The in vitro antimicrobial activity of some newly synthesized compounds against bacteria and fungi was studied. Conclusion New compounds showed better or similar antimicrobial activity. Designing more efficient steroidal hydrazones from ketosteroid based on the current study may successfully lead to the development of antimicrobial agent. Graphical abstract

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Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening

Applied Sciences ◽

10.3390/app11031180 ◽

2021 ◽

Vol 11 (3) ◽

pp. 1180

Author(s):

Kinga Paruch ◽

Łukasz Popiołek ◽

Anna Biernasiuk ◽

Anna Berecka-Rycerz ◽

Anna Malm ◽

...

Keyword(s):

Antimicrobial Activity ◽

Carboxylic Acid ◽

Bacterial Infections ◽

Acid Hydrazide ◽

Antimicrobial Effect ◽

In Vitro Antimicrobial Activity ◽

Research Goal ◽

New Compounds ◽

Derivatives Of

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

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Synthesis of New Furothiazolo Pyrimido Quinazolinones from Visnagenone or Khellinone and Antimicrobial Activity

Molecules ◽

10.3390/molecules23112793 ◽

2018 ◽

Vol 23 (11) ◽

pp. 2793 ◽

Cited By ~ 7

Author(s):

Ameen Abu-Hashem

Keyword(s):

Antimicrobial Activity ◽

Growth Inhibition ◽

Spectral Data ◽

Elemental Analysis ◽

13C Nmr ◽

Heterocyclic Compounds ◽

Gram Negative Bacteria ◽

Gram Negative ◽

Bacteria And Fungi ◽

New Compounds

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.

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PTSA-Catalyzed One Pot Domino Synthesis of Dihydropyrido[2,3-d]pyrimidine Derivatives and their Antimicrobial Activity

Asian Journal of Organic & Medicinal Chemistry ◽

10.14233/ajomc.2021.ajomc-p340 ◽

2021 ◽

Vol 6 (3) ◽

pp. 222-227

Author(s):

Krishna A. Bhensdadia ◽

Prakash L. Kalavadiya ◽

Nilam H. Lalavani ◽

Shipra H. Baluja

Keyword(s):

Antimicrobial Activity ◽

Spectral Analysis ◽

Pyrimidine Derivatives ◽

One Pot ◽

In Vitro Antimicrobial Activity ◽

Aryl Aldehydes ◽

Three Component Reaction ◽

The One

A novel series of dihydropyrido[2,3-d]pyrimidine derivatives were synthesized by multicomponent domino cyclization via the one-pot three component reaction of 6-amino uracil, substituted aryl aldehydes and N-methyl-1-(methylthio)-2-nitroethenamine in the presence of PTSA 10 mol% as a catalyst. The structures of these synthesized compounds were characterized by spectral analysis. Further the synthesized compounds screened for in vitro antimicrobial activity. Among all the compounds, compound 4b containing flouro substitution exhibited good inhibition against the tested species.

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