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Record W2165499869 · doi:10.1139/v02-124

The antimicrobial nalidixic acid as a probe for molecular recognition of α- and β-cyclodextrins

2002· article· en· W2165499869 on OpenAlexvenueno aff
Ibrahim Shehatta, Mohamed Ibrahim, Mahmood Sultan

Bibliographic record

VenueCanadian Journal of Chemistry · 2002
Typearticle
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicDrug Solubulity and Delivery Systems
Canadian institutionsnot available
Fundersnot available
KeywordsChemistryNalidixic acidHydrogen bondAbsorption (acoustics)Gibbs free energySolubilityCrystallographyCyclodextrinAbsorption spectroscopyStability constants of complexesStereochemistryPhysical chemistryAqueous solutionMoleculeOrganic chemistryThermodynamicsAntibioticsTetracyclineBiochemistry

Abstract

fetched live from OpenAlex

The inclusion of the antibacterial drug nalidixic acid (NAL) in α- and β-cyclodextrin (CD) cavities was studied using UV–vis absorption and voltammetric methods. It was corroborated that the UV absorption bands of NAL are intensified in the presence of α- and β-CDs. A pronounced decrease in the peak currents of NAL was also noticed upon the addition of α- and β-CDs. From the changes in the peak currents, it was concluded that NAL forms 1:1 inclusion complexes with the various hosts, which is also revealed in the phase solubility profile of the NAL–β-CD system, as a representative example. From voltammetric data, the logarithm of the binding constants were calculated to be 2.60 and 3.20 for α- and β-CDs, respectively. The magnitude of the formation constants, as well as the Gibbs free energies for NAL with α- and β-CDs, shows that NAL is bound more strongly to β-CD, with a more apolar cavity, than to α-CD. These observations suggest that hydrophobic interaction is the most important recognition element in the binding process. All orientations of entering NAL into the cavity have been considered herein, with the purpose of characterizing the inclusion complex of NAL with CD. Combining the experimental results and molecular modeling and energy calculations on the inclusion complexes yielded a more detailed picture of the solution structure of the complex formed between NAL and either α-CD or β-CD. It was inferred that the inclusion process can occur through the 2-methylpyridine side. An additional hydrogen bond was also found to be formed between the carboxyl group of NAL, which remains outside the β-CD cavity, and the secondary hydroxyl group of β-CD. This hydrogen bond should, therefore, be operating as an important second recognition element in the NAL–β-CD system. Key words: cyclodextrins, host–guest association, inclusion complexes, nalidixic acid, solubility, voltammetry.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.001
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.120
Threshold uncertainty score0.330

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.077
GPT teacher head0.335
Teacher spread0.258 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations11
Published2002
Admission routes1
Has abstractyes

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