NEW PHENOTHIAZINE DERIVATIVE DESIGNED ACCORDING TO LIPINSKI’S RULE OF FIVE AND ITS VARIANTS

doi:10.21065/19204159.5.34

Paper

NEW PHENOTHIAZINE DERIVATIVE DESIGNED ACCORDING TO LIPINSKI’S RULE OF FIVE AND ITS VARIANTS

Published Apr 1, 2013 · Bint-e-Haider, M. Qaiser, H. Faizi

Journal of applied pharmacy

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Abstract

Some of the new 10H phenothiazine derivatives had been synthesized for their anti psychotic activity as dopamine antagonists. They had been synthesized with the help of software Marvin sketch. 10 parameters were analyzed for each of them which could make them drug like molecule. All parameters were found to be within range. Newly designed structures justify all the aspects of anti psychotic activity by satisfying Lipinski’s Rule. Three carbon distance from two amine atoms keeps the polar surface area within range (>10). Log P value and conformational energy of these derivatives shows that they are structurally constrained molecules. They have also satisfied the stereo chemistry and hence safer derivatives. The limit for total numbers of atoms and H-bond donor and Acceptor are also seem to be fulfilled. So these derivatives have maximum chances that they could be drug like molecules which may have valuable anti psychotic activity. They could be investigated further for clinical use in conditions like schizophrenia, mania and other psychotic disorders.

Study Snapshot

New 10H phenothiazine derivatives show potential as antipsychotic drugs by satisfying Lipinski's Rule and meeting other criteria, making them potentially useful for treating schizophrenia, mania, and other psychotic disorders.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

NEW PHENOTHIAZINE DERIVATIVE DESIGNED ACCORDING TO LIPINSKI’S RULE OF FIVE AND ITS VARIANTS

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References

Synthesis of New 10-Substituted Phenothiazines as Antiinflammatory and Analgesic Agents

New 10-substituted phenothiazines show potent antiinflammatory and analgesic properties, with compound 4a' showing the most potent analgesic activity and compound 4a showing good ulcerogenic liability.

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