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Pharmacological Study and Liposomal Formulation Evaluation of Novel 4-Aminoquinaldine Derivatives and Generic Drugs as Antileishmanial, Anti Cancer and Antimicrobial Agents

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Title Pharmacological Study and Liposomal Formulation Evaluation of Novel 4-Aminoquinaldine Derivatives and Generic
Drugs as Antileishmanial, Anti Cancer and Antimicrobial Agents
 
Creator Palit, Partha
 
Subject Infectious Diseases and Immunology
 
Description Leishmania parasites are the causative agents for cutaneous and visceral leishmaniasis affecting approximately 12 million cases annually. Pentavalent antimonials (Sb), though
toxic, remain the first-line drug for leishmaniasis. Emergence of drug-resistance has campaigned in second-line drugs like Amphotericin B (AmB) and pentamidine, and
miltefosine as an oral drug which cause toxic side effects and/or relapse of disease. Prolong biological half life of miltefosine can cause drug resistance, and is thus a barrier in its therapeutic use. Moreover, the convergence of visceral leishmaniasis with Human immunodeficiency virus (HIV) has turned the treatment regimen into worse condition.
Antileishmanial treatment with a new safe molecule with short course of treatment executing newer mode of action are the only solution to combat this neglected and fatal disease. In the first Chapter, PP-9 and PP-10 were evaluated for pre ADME and in vitro pharmacokinetic investigation whether they could be good candidates for oral
antileishmanial therapy. Data herein reveals that PP-9 and PP-10 have good permeability in PAMPA model. pKa value (8.128) suggests that the lead molecule, PP-10 may be absorbed by the lower intestine. Log P and Log D values are optimum for PP-10 which may be developed as an oral drug. High lipophilicity may aid it for good oral absorption. Molecular formulas and other physicochemical parameters convey that these molecules strongly adopt the Lipiniski rule of 5 to become a good oral drug. Furthermore, PP-10 contains the basic 4-amino quinaldine pharmacophore scaffold modified with dichloro anilide side chain. It
cannot be precipitated in the blood during distribution.
 
Date 2008
 
Type Thesis
NonPeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/1574/1/Partha_Palit_PDF.pdf
Palit, Partha (2008) Pharmacological Study and Liposomal Formulation Evaluation of Novel 4-Aminoquinaldine Derivatives and Generic Drugs as Antileishmanial, Anti Cancer and Antimicrobial Agents. PhD thesis, Jadavpur University.
 
Relation http://www.eprints.iicb.res.in/1574/