Browsing by Author "Patil, Jayshree P."

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    Review on Advances in the Synthesis and Bioactivity of Quinazolinone Derivative
    (International Journal for Pharmaceutical Research Scholars (IJPRS), 2014) Patil, Jayshree P.
    Owing to the significant biological activities, quinazoline derivatives have drawn more and more attention in the synthesis and bioactivities research. Many of the literature synthetic methods for elaboration of this simple ring structure are, however, time consuming, tedious and often low yielding. This review summarizes the recent advances in the synthesis investigations for the construction of the 4(3H)-quinazolinone and quinazoline skeletons. The synthetic methods were divided into five main classifications, including Aza-reaction, Microwave-assisted reaction, Metal-mediated reaction, Ultrasound-promoted reaction and Phase-transfer catalysis reaction. Literature studies on quinazolinones have shown that these derivatives possess a wide variety of biological activities. This review also focused on the few novel biological activities of quinazolinones but emphasis is specified for synthetic methods.
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    A review on polymer drug conjugate - what, why and how?
    (International ournal of Pharmaceutical Sciences and Research, 2015-11-01) Patil, Jayshree P.
    ABSTRACT: It is well known that polymeric prodrug or polymer-drug conjugate is an effective and fast growing technique for improved use of drugs for therapeutic applications. Polymer conjugated drugs generally exhibit prolonged half-life, higher stability, water solubility, lower immunogenicity and antigenicity and specific targeting to tissues or cells. Polymers are used as carriers in polymeric prodrugs/macromolecular prodrugs for the delivery of drugs, proteins, targeting moieties, and imaging agents. The potential of the polymer-drug conjugates have already been proved by success of many products in the market for the treatment of different diseases. The polymeric pro-drug can be regarded as drug delivery systems that exhibit their therapeutic activities by means of releasing smaller therapeutic drug molecules from a polymer chain molecule for a prolonged period of time which results in enhanced pharmacokinetic behaviour by increasing the t 1/2 , bioavailability, and hence prolonged pharmacological action. This review deals with the Rational for design of polymer-drug conjugates (PDC), requirements for selection of drug candidate for polymeric prodrug, requirements for selecting polymers as candidate drug carriers, classification of polymers, design and synthesis of polymeric prodrugs and strategies to enhance the reactivity of polymer and the drug by incorporation of spacers.
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    SYNTHESIS AND ANXIOLYTIC ACTIVITY OF 2-METHYL-3-AMINO-4- QUINAZOLINONE ACETAMIDE DERIVATIVES
    (Coden HLEEAI, 2014) Patil, Jayshree P.
    Medicinal Chemistry plays a vital role in the eradication of fatal diseases in human being. Quinazolin-4-one is versatile lead molecule. The synthesis of its derivatives has been the focus of great interest for the development of newer bioactive agent. The present study involves the synthesis, purification and characterisation of various acetamide derivatives of 3-aminoquinazolinone. Methyl Anthranilate on condensation with acetic anhydride in presence of pyridine and hydrazine hydrate form 2-methyl-3-amino-4-quinazolinone. The purity of synthesized compound was checked by Thin Layer Chromatography. The melting point of synthesized compounds were analysed with an open ended capillary tube method. Structures of synthesized compounds were elucidated by FT-IR, GC-MS, and NMR spectral analysis. The synthesized compounds were evaluated for anxiolytic activity by Elevated plus Maze Test and Light and Dark Test using Diazepam as standard.