The synthesis, computer prediction of the biological activity and the acute toxicity of 1-Ar-4-R-[1,2,4]triazolo[4,3-a] quinazolin-5(4H)-ones

Danylchenko, S. Yu.; Drushlyak, O. G.; Kovalenko, Sergiy M.

doi:10.24959/ophcj.15.853

Cited by 2 publications

(2 citation statements)

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“…Similar studies were performed by S.M. Kovalenko group on [1,2,4]triazolo[4,3‐α]quinazolin‐5(4H)‐one derivatives and they also observed non‐toxicity of different compounds in different modes of administration …”

Section: Figurementioning

confidence: 99%

“…Kovalenko group on [1,2,4]triazolo[4,3-α]quinazolin-5(4H)-one derivatives and they also observed non-toxicity of different compounds in different modes of administration. [25] In summary, eight new N-glycoconjugates containing amino acids with hydrophobic side chain and mefenamic acid have been synthesized and their in vitro COX-2 inhibition activity has been explored. All the molecules exhibited a fair amount of enzyme inhibition and this was also supported by in silico studies.…”

Section: Absorbance α [Bound Pg Tracer] α 1/pgsmentioning

confidence: 99%

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Synthesis of Mefenamic Acid Containing N ‐Glycoconjugates and Their Evaluation as Human COX‐2 Enzyme Inhibitor

Madduluri

Sah

2020

ChemistrySelect

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A series of d‐glucose derived N‐glycopeptides containing mefenamic acid have been synthesised and in vitro evaluation of all these molecules have been performed as COX‐2 (human) enzyme inhibitor using Enzymes Immuno Assay kit. These studies were further supported by docking experiments on human COX‐2 enzyme (PDB ID: 5IKR). All the compounds exhibited a fair amount of COX‐2 enzyme inhibition during both the modes of study and tryptophan derivative showed the best activity. Acute toxicity (LD50) in rat has also been evaluated using General Unrestricted Structure‐Activity Relationships (GUSAR) software, where acute oral toxicity for most of the molecules was found to be less than the pure mefenamic acid.

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Section: Figurementioning

confidence: 99%

Section: Absorbance α [Bound Pg Tracer] α 1/pgsmentioning

confidence: 99%

Synthesis of Mefenamic Acid Containing N ‐Glycoconjugates and Their Evaluation as Human COX‐2 Enzyme Inhibitor

Madduluri

Sah

2020

ChemistrySelect

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Primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives

Danylchenko¹,

Drushlyak²,

Коваленко³

et al. 2016

ScienceRise

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Otsenka adgezivnykh svoystv spor vaktsinnykh shtammov Bacillus Anthracis na eritrotsitakh mlekopitayushchikh s pomoshch'yu fotokolorimetrii [Evaluation of adhesive properties of spore vaccine strains of Bacillus Anthracis on erythrocytes of mammals using photocolorimetry]. Problemy osobo opasnykh infektsiy, 110, 41-43. 11. Makhrova, T. V., Zaslavskaja, M. Y., Majanskyj, A. N. (2004). Vliyanie metabolitov stafilokokkov na adgezivnye reaktsii v sisteme «Candida albicansbukkal'nye epiteliotsity» [Influence of staphylococcal metabolites on reaction adhesive system "Candida albicansbuccal epithelial cells]. ZhMEI, 5, 4-7. 12. Khyzhnyak, O. S. (2015). Vyvchennya adhezyvnykh vlastyvostey bifidobakteriy ta laktobatsyl pry sumisnomu kul'tyvuvanni [Study of adhesive properties of bifidobacteria and lactobacilli in the joint cultivation]. Farmakom, 1, 71-74. 13. Anisimov, T. I., Bukovskaja, S. N. et. al (1989). Rukovodjashhij dokument po standartizacii. rD 42-28-8-89 / Doklinicheskie ispytanija novyh medicinskih immunobiologicheskih preparatov [Guidance document on standardization. 42-28-8-89 pA / Pre-clinical testing of new medical immunobiological preparations]. Moscow, 31. 14. Khyzhnyak, O. S. (2015). Rozrobka skladu kapsul'noyi masy profilaktychnoho zasobu na osnovi probiotychnykh bakteriy [Development of the capsule mass of drug based on probiotic bacteria]. Farmakom, 3-4, 43-48.

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The synthesis, computer prediction of the biological activity and the acute toxicity of 1-Ar-4-R-[1,2,4]triazolo[4,3-a] quinazolin-5(4H)-ones

Cited by 2 publications

References 8 publications

Synthesis of Mefenamic Acid Containing N ‐Glycoconjugates and Their Evaluation as Human COX‐2 Enzyme Inhibitor

Synthesis of Mefenamic Acid Containing N ‐Glycoconjugates and Their Evaluation as Human COX‐2 Enzyme Inhibitor

Primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives

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