Chemistry Articles

16 December 2012

CONDENCED HETEROCYCLIC SYSTEM - QUINOLINE WITH THEIR NUMEROUS BIOLOGICAL ACTIVITY

About Authors:
C.P.Meher*, D.V.Charan, S.P.Sethy
Asst. Professor
Maheshwara Institute of Pharmacy,
Chitkul, Patancheru, Medak, A.P
*chaitanyameher84@gmail.com

ABSTRACT
Heterocyclic chemistry is the branch of chemistry dealing with structure,synthesis, properties, and applications of heterocycles. heterocyclic compounds may be inorganic, most contain at least one carbon. Since in organic chemistry non-carbons usually are considered to replace carbon atoms, they are called heteroatoms, meaning 'different from carbon and hydrogen' (rings of heteroatoms of the same element are homocyclic). The IUPAC recommends the Hantzsch-Widman nomenclature for naming heterocyclic compounds.The present review article is based on the condenced heterocyclic system quinoline derivatives with their tremendous pharmacological activities.
2 December 2012

IMPURITIES AN OVERVIEW

About Authors:
Lila dhar^*, Prof. Sanjeev Thacker, Jatin Patel
Seth G. L. Bihani S.D. College Of Technical Education, Institute Of Pharmaceutical Sciences & Drug Research,
Gaganpath, Sri Ganganagar, Rajasthan 335001
*ldbudania@gmail.com

ABSTRACT
Impurities is defined as an entity of drug substances or drug product that is not chemical entity defined as drug substances an excipients or other additives to drug product. In pharmaceutical world, an impurity is generally considered as an other organic material beside the other drug substances that is arises out of the synthesis most of the time, inorganic contaminants are not considered as an impurity unless they are toxic, such as heavy metal or arsenic. There are numerios source of impurities and many different common terms are use for impurities such as by product, intermediate, transformation on product, related product, interaction product and degradation products.
29 November 2012

REVIEW ON THE LEAD OPTIMIZATION TECHNIQUES (PHASE-I)

About Authors:
Kambham Venkateswarlu*, D.Z.Suhasini
Department of Pharmacology,
Sri Lakshmi Narasimha College of Pharmacy (JNTUA), Pallur,
Chittoor, Andhra Pradesh, India.
*k.v.reddy9441701016@gmail.com

ABSTRACT:
Lead optimization techniques are deals that new discovery is to choose the compounds with a known pharmacological action and proceed to modify the molecular structure of the compound systemically to get a drug with desired properties pharmacological action and pharmacokinetics. The compounds of the drugs are choosing for the study is called as lead.

Generally the identification and synthesis of compounds which are structurally related to the lead compound and testing their pharmacological activity. In the process it is possible to find a better drug than the lead compound.

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28 November 2012

PYRROLE, FURAN, THIOPHENE DERIVATIVES & PHARMACOLOGICAL ACTIVITIES: A REVIEW

About Authors:
C.P.Meher*, S.P.Sethy, M.Madhavi
^*Asst. Professor
Maheshwara Institute of Pharmacy,
Chitkul, Patancheru, Medak, A.P
*chaitanyameher84@gmail.com

ABSTRACT:
Medicinal chemistry and pharmaceutical chemistry are disciplines at the intersection of chemistry, especially synthetic organic chemistry, and pharmacology and various other biological specialties, where they are involved with design, chemical synthesis and development for market of pharmaceutical agents, or bio-active molecules (drugs).Very important part of above is the heterocyclic-chemistry. Now a days so many investigation are carried out for developing new chemical entities having suitability for human life. A lot of research work is going on presently for development of new heterocyclic derivatives.The present review article is concern with the three, five-membered heterocyclic compound pyrrole, furan & thiophene derivatives that show diverse pharmacological activities.
20 September 2012

STRUCTURE BASED DRUG DESIGN OF PIPERAZINE LINKED HYDROXAMIC ACID DERIVATIVES AS HDAC INHIBITOR

About Authors:
Avisek Mukhopadhyay*, Subhasis Banerjee
Gupta College Of Technological Sciences
M.Pharm(Bit Mesra, Ranchi)
*avisekmukhopadhyay7@gmail.com

INTRODUCTION
Urbanization, industrialization, changes in lifestyles, population growth and ageing all have contributed for epidemiological transition in the country. The absolute number of new cancer cases is increasing rapidly, due to growth in size of the population, and increase in the proportion of elderly persons as a result of improved life expectancy following control of communicable diseases. In India, the life expectancy at birth has steadily risen from 45 years in 1971 to 62 years in 1991, indicating a shift in demographic profile. It is estimated that life expectancy of Indian population will increase to 70 years by 2021–25. Such changes in the age structure would automatically alter the disease pattern associated with ageing and increase the burden of problems such as cancer, cardiovascular and other non-communicable diseases in the society.The latest global figures show that in 2004, there were 11.4 million cases of cancer diagnosed worldwide, and 75% of these were in Europe, the Americas and the Western Pacific Region. The Western Pacific Region includes China, Malaysia, Japan, Australia and New Zealand. The lowest numbers of cases were diagnosed in the Eastern Mediterranean region (includes Saudi Arabia, Egypt Iraq, Morocco, Tunisia) and Africa.
There were differences in the top three most common cancers in each region. The top three included lung cancer in all regions except Africa and included breast cancer in all except for the Western Pacific region. Cervical cancer was in the top three in Africa and South-East Asia only and bowel cancer in the top three for Europe only. Prostate cancer was in the top three in Africa and the Americas.Let us discuss one of the most promising targets of these days, which when overexpressed may cause cancer, i.e.;HISTONE DEACETYLASE.

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28 August 2012

SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL HETEROCYCLES DERIVED FROM 2-ARYLIDENE-1-TETRALONES

About Authors:
Roshni Patel*, Prof. Arun Parikh, Prof. Vijayalakshmi Gudaparthi
Department of Pharmaceutical Chemistry, L.J.Institute of Pharmacy,
S.G.Highway, Ahmedabad-382210
*roshanimpharm@gmail.com

ABSTRACT
Medicinal chemistry involves chemical aspects of identification, and then systematic, thorough synthetic alteration of new chemical entities to make them suitable for therapeutic use. Indazoles have an important role in medicinal chemistry. Indazole nucleus is an important class of nitrogen containing heterocyclic widely used as key building block for the synthesis of various pharmaceutically important agents. Indazole possess wide range of biological activities such as bactericidal, fungicidal, analgesic, antihypertensive, anti-inflammatory and antitumor. In the present study we have synthesized some novel 3,3a,4,5-tetrahydro-2-(substituted benzenesulphonyl)-3-(substituted phenyl)-2H-benzo[g]indazoles, by condensation of 1-tetralone with different substituted aromatic aldehydes and the resulted 2-(substituted benzylidene)-3,4,-dihydronaphtalen-1-ones on reaction with hydrazine hydrate in methanol followed by treatment with different substituted sulfonyl chlorides in pyridine gave the titled compounds.The synthesized compounds were characterized by IR, NMR and Mass spectral analysis. All newly synthesized derivatives were evaluated for antibacterial activity against gram + ve and gram-ve bacteria B.cereus, S.aureus and E.coli respectivelyand antifungal activity againstC.albicans and all the synthesized compounds showed significant antibacterial and antifungal activity.

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25 August 2012

SIMULTANEOUS ESTIMATION OF FUROSEMIDE AND SPIRONOLACTONE IN COMBINED PHARMACEUTICAL DOSAGE FORM BY RP-HPLC

About Author:
Hardik Patel^*, Sagar Solanki
Department of Pharmaceutical Chemistry,
K.B.Raval College of Pharmacy, Shertha,
Gandhinagar-382423, Gujarat, India.
*patel1928@yahoo.in

ABSTRACT
A new, simple, rapid, accurate, precise and sensitive method has been developed for the simultaneous estimation of Furosemide and Spironolactone in their combined tablet dosage form. The method was carried out on a Hiber C₁₈ column (250 mm×4.6mm, i.d.5 μm) with a mobile phase consisting of acetonitrile: water at a flow rate of 1 ml/min and the detection was carried out at 237 nm. The retention time of Furosemide and Spironolactone was 3.81 min and 7.28 min. respectively. Linearity for Furosemide and Spironolactone were found in the range of 2-10 μg/ml and 5-25 μg/ml respectively. The developed method was validated in terms of linearity, accuracy, and precision, limit of detection (LOD) and limit of quantification (LOQ). The proposed method can be used for estimation of both drugs in their combined dosage form.
20 July 2012

Synthesis and Antimicrobial activity of Bulky molecules comprising Benzothiazole and Sulphonamide moieties

About Authors:
Pritesh R. Patel^*, Priyank Patel, Jagath Pillai, Nilesh Darji, Bhagirath Patel
Department of Pharmaceutical Chemistry,
Sat Kaival College of Pharmacy, Sarsa,
Ta & Dist: Anand (Gujarat), India-388365
*prit.pharma@gmail.com

ABSTRACT
As part of ongoing studies in developing new antimicrobials, a novel series of 4-acetamido-N-(substituted 1, 3-benzothiazol-2-yl) benzenesulphonamide and N-(substituted 1, 3-benzothiazol-2-yl)-4-(substituted aryl diazenyl) benzenesulphonamide were synthesized in order to determine their antibacterial and antifungal activity. The synthesized compounds were tested in vitro against two Gram-positive bacteria like Staphylococcus aureus, Bacillus subtilis; two Gram-negative bacteria like Escherichia coli, Pseudomonas aeruginosaand one fungal strain Candida albicans in comparison with standard drugs. Microbiological results showed that the synthesized compounds possessed a broad spectrum of antibacterial and antifungal activity against the tested microorganisms. The compounds with a 6-chloro (SK5b), 7-chloro-6-fluoro(SK5d) and 6-nitro (SK5e) on 2-amino benzothiazole ring possessing azo linkage showed better antimicrobial activity; almost similar or less to that of standard drugs thus they could be promising candidates for novel drugs. The novel heterocyclic derivatives were characterized by Physical characterization (Melting point, TLC) and different Spectroscopy techniques (IR, ¹H NMR and Mass spectroscopy).
19 July 2012

A REVIEW ON ROLE OF MOLECULAR DESCRIPTORS IN QSAR: A COMPUTATIONAL METHODS APPROACH

About Authors:
Rakesh Bhatia*
School of Pharmaceutical Sciences,
Department of Pharmaceutical Chemistry,
Jaipur National University,
Jaipur-302025 (Rajasthan), India
*rakesh.mpharm1304@yahoo.com

Abstract
Chemical synthesis data and their biological screening have provided a vast amount of experimental data. As a result of that, availability of large amount of biological data information through molecular biology has made drug discovery and development a more complex method. To combat these problems, Quantitative structure-activity relationships (QSAR) emerged as a very useful tool in drug design. QSAR has been applied extensively and successfully over several decades to find predictive models for activity of bioactive agents. QSAR have brought revolution in drug discovery process by thedevelopment of mathematicalrelationships linking chemical structures and pharmacological activity in quantitative manner of series of compounds. Description of the molecular structure, electronic orbital reactivity and the role of structural and steric components has been the subject of mathematical and statistical analysis. Computational drug design method in QSAR is a rapidly growing field which is now a very important component in the discipline of medicinal chemistry. Virtual filtering and screening of combinatorial libraries have recently gained attention as methods complimenting the high-throughput screening and combinatorial chemistry. These chemoinformatic techniques rely heavily on quantitative structure-activity relationships (QSAR) analysis, a field with established methodology and successful history.By characterize a specific aspect of a molecule that is numbers containing structural information derived from the structural representation used for molecules under study called “Molecular descriptors” to find appropriate representations of the molecular structure of drug compoundsto obtain the structure-activity relationships in which these theoretical and computational methods are based, the ability to predict physicochemical, pharmacokinetic and toxicological properties of these leads are becoming increasingly important in reducing the number of expensive methods and late development failures. Thus thereby, QSAR certainly decreases the number of compounds to be synthesized by easing the selection of the most promising candidates. This review seeks to provide a review on role of molecular descriptors in the drug design in QSAR.

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1 July 2012

IONTOPHORETIC DRUG DELIVERY SYSTEM- A BUNCH OF POSSIBILITIES

About Authors:
^1*Ajeet, ²Shelly Singh
¹Department of Medicinal Chemistry, S. D. College of Pharmacy and Vocational Studies,
Bhopa Road, Muzaffarnagar, U.P., India, PIN-251001
²Department of Pharmaceutics, Mahatma Gandhi College of Pharmaceutical Sciences,
Jaipur, Rajasthan, India.
* ajeet_pharma111@rediffmail.com

Abstract
Iontophoresis, a 250 years old technology for delivering the drug is simply based on the use of electrical potential. Being so old, it is still having too popped up just because of its unlimited aspects to work with. In the present review, I tried to compile the vast aspects of a drug delivery system termed as iontophoresis. Iontophoresis is one of the most interesting and challenging endeavors facing the pharmaceutical scientist. The systemic drug delivery systems often require large dose and are associated with gastrointestinal side effects, while topical application of solutions, suspensions, and ointments show variability in absorption patterns. Iontophoresis technique is capable of expanding the range of compounds that can be delivered through ocular, transdermal, ural, transungual, buccal or by nasal route.