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ISSN (Online): 0975-8232,
ISSN (Print): 2320-5148

International Journal Of
Pharmaceutical Sciences And Research

IJPSR is indexed with Embase

An International Journal published monthly
An Official Publication of Society of Pharmaceutical Sciences and Research

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Posted by on Dec 31, 2015 in | 0 comments

QUINOLINE: A DIVERSE THERAPEUTIC AGENT

Quinoline and its derivatives are diverse pharmacological agents. They play a vital role in the development of new therapeutic agents. Many new therapeutic agents have been developed by using quinoline nucleus. Hence quinoline and its derivatives constitute an important class of heterocyclic compounds for the new drug development. Quinoline is also known as 1-azanapthalene and many researchers have synthesized large number of quinoline derivatives. Different synthetic routes have been developed by these researchers for the synthesis of quinoline derivatives. These derivatives have also been evaluated for the relevant biological activity by in vitro as well as in vivo methods. The present review focuses on detailed work done so far on the quinoline and its derivatives in the search of new therapeutic agents. The review covers the synthesis as well as biological activities of quinoline derivatives such as antimalarial, anticancer, antibacterial, anthelmintic, antiviral, antiprotozoal, antifungal, anti-inflammatory, analgesic, cardiovascular, reproductive, central nervous system activity, hypoglycemic and miscellaneous...

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PHILADELPHIA CHROMOSOME IN PRETHERAPEUTIC CASES OF CHRONIC MYELOGENOUS LEUKEMIA

Chronic myeloid leukemia (CML) is a clonal myel0 proliferative disorder due to neoplastic transformation of myeloid stem cells. The characteristic Philadelphia Chromosome translocation t(9:22) (q 34: q11) juxta poses the c-abl oncogene from chromosome 9 with break point cluster region (bcr) on chromosome 22 resulting in the generation of aberrant bcr/abl transcripts. The abnormal bcr/abl tyrosine kinase gene product has enhanced activity compared to the wild type c-abl tyrosine kinase and is believed central to the pathogenesis of CML. Most of the patients in chronic phase who are treated with cytotoxic agents eventually develop a fatal blast phase that is the end stage in which the patient usually fails to respond combination chemotherapy and only treatment remain after that is allogenic bone marrow transplantation. Since the philadelphia chromosome is the most consistant abnormality in CML patients and as it possess both diagnostic as well as prognostic importance, it’s detection is mandatory to establish the diagnosis of CML and for planning of chemotherapy. Our study is a preliminary work to...

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PHYTOCHEMICALS AND COMPLICATIONS IN TYPE 2 DIABETES-AN UPDATE

Type 2 diabetes is a serious health problem globally. In type 2 diabetes insulin resistance in various tissues such as liver, muscle and β-cell is the major pathophysiological defects. People with long term uncontrolled hyperglycemia are at risk of developing a number of serious and life-threatening complications which mainly affect the heart and blood vessels, eyes, kidneys, and nerves. Current drug development strategy has focused towards the control of hyperglycemia but the treatment of severe complications has been neglected. Many herbs including Momordica charantia, Coccinia indica, Ficus carica, Gymnema sylvestre, Ocimum santum and many more have traditionally been used for the treatment of diabetes and associated complications. Natural products have been reported to have their efficacy in diabetes and its complications by protecting pancreatic β-cells, increasing insulin sensitivity, reducing oxidative stress and by targeting various proteins. Thus, now a day plant based natural product (phytoconstituents) have been the basis of drug development program for the treatment of various diseases. The present review summarizes the latest updates on phytochemicals from...

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SYNTHESIS OF HETEROCYCLIC NITROGEN COMPOUNDS BY CLOSURE REACTIONS USING TETRAACETYLETHANE WITH VARIOUS PRIMARY AMINES

This work includes synthesis of new five, six, and seven-heterocyclic nitrogen compounds by closure reactions of tetraacetylethane (3) with primary amines in refluxing ethanol and acetonitrile as solvents and without using any catalysts. The tetraacetylethane melting point 184-189 ºC was prepared by condensation of two anhydrous molecules of sodium salt of acetylacetone and in the presence of dry ether as solvents and Iodine as a catalysts. The heterocyclic nitrogen compounds as: 1,4,5,8-tetramethyl-4a,8a-dihydropyridazino[4,5-d]pyridazine (11), 3,7-bis (2,4-dinitrophenyl)1,4,5,8-tetramethyl-4a,8a- dihydropyridazino [4,5-d]pyridazine (12), 1,4,5,8-tetramethyl-1,4a,5,8a-tetrahydro-oxazino[4,5-d]oxazine (13), 4,4′,6,6′-tetramethyl-[5,5′-bipyrimidine]-2,2′(5H,5H’)-dione (14), 2,2′,4,4′-tetramethyl-3H,3H’-3,3′-bibenzo[b][1,5]diazepine (15), (4,6-dimethyl-1, 3 dimethyl enepyrrolo[3,4-c]pyrrole-2,5-diyl)bis(ethan-1-amine) (16), 4,4′-(4,6-dimethyl-1,3-dimethylene pyrrolo[3,4-c]pyrrole 2,5-diyl) dibenzoic acid (17), 2,5-bis(4-bromophenyl)-4,6-dimethyl-1,3-dimethylene-pyrrolo[3,4-c] pyrrole (18), 1,1′-((4,6-dimethyl-1,3-dimethylenepyrrolo[3,4-c] pyrrole -2,5-diyl) bis (4, 1-phenylene)) bis (ethan-1-one) (19), were prepared via condensation of compound (3) with primary amines (e.g. , hydrazine hydrate and primary aromatic amines) in 1:2 molar ratios. The compounds (11-19) were also synthesized by microwave irradiation of starting materials without using any solvent to give excellent yields of these compounds ranging between 80-95. Compounds (11-19) have been identified by spectroscopic methods, IR, UV, 1H-NMR, 13C-NMR (DEPT. 90...

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SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NOVEL α-AMINOPHOSPHONATES BEARING A QUINOLINE MOIETY

A novel aminophenylaminoquinoline analogues have been synthesized starting from 4,7 dichloroquinloine and (p-phenylenediamine 2a, o-phenylenediamine 2b or m-phenylenediamine 2c). The one pot reaction with aldehydes and triphenylphosphite in presence of LiClO4 as a Lewis acid catalyst led to the formation of novel α-aminophosphonate derivatives bearing quinoline moiety in good yields. The synthesized compounds have been characterized on the basis of the spectral analysis.  All the synthesized compounds were screened for in vitro antibacterial activity and most of them showed a potency against both gram positive and gram negative...

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