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SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL 3-(2-(1H-INDOL-2-YL) PHENYL)-2-ARYLIMIDAZO[4,5-b]INDOLES

About Authors:
Aditya Dixit1, Gyanendra Kumar Sharma2, Devender Pathak*3
1M. Pharmacy (Pharmaceutical Chemistry)
2Associate Professor (Pharmaceutical chemistry)
3Director, Professor and Head of the Dept. (Pharmaceutical Chemistry)
Rajiv Academy for Pharmacy, Mathura,
Delhi-Mathura Highway, Chhattikara, 281006, India
dev_15@rediffmail.com*, adixit70@gmail.com

ABSTRACT
A traditional but effective method of developing new targets is lead molecule modification, where an existing popular drug from the market is taken as a lead and similar derivatives are synthesized. With the advent of modern techniques conventional methods have lost their gleam but, reactions are still best understood when performed by the conventional techniques. One such endeavor has been made here where indole has been used as a parent moiety and by adding some functional groups some novel indole derivatives were synthesized and screened for their in vitro antitubercular, and anticancer activity. This synthesis of some fresh indole derivatives was done by using various benzaldehyde derivatives and 2-(o-Aminophenyl)indole in acidic condition then with ammonium acetate and isatin in presence of glacial acetic acid.. The structures of newly synthesized compounds were characterized by IR, 1H NMR, MASS and elemental analysis.Compounds 3h & 3i showed good antitubercular activity and 3d, 3e & 3g showed good anticancer compared to the standard drug.



FOOD CONTAMINANTS: BANGLADESH PERSPECTIVE

About Authors:
Zubair Khalid Labu1; AK Mohiuddin1; M.A Bake*2
1Department of Pharmacy, World University of Bangladesh (WUB), Dhaka-1215, Bangladesh
*2Product Development officer, Gonoshasthaya Pharmaceuticals Ltd., Mirzanagar, Savar, Dhaka-1344.
zubairlabu@yahoo.com; *abdul.bake@yahoo.com

Abstract
Food is the major source of energy in humans as well as animals. Foods are materials taken into the body by different route which provide nourishment in the form of energy or in the building of tissues. Food contaminants are substances that make food unfit for human consumption. Examples include bacteria, toxic chemicals, carcinogens, teratogens and radioactive materials. The purpose of these studies is to find out the food contaminants which are used in different purposes available in Bangladesh and contaminants detection method. After survey we found that Dhaka is the main city where food contamination by various contaminants in higher percentage. This contamination done by manmade, industrial discharge, poisonous water etc. Government of Bangladesh taking various necessary steps to stop this contamination.


REVIEW OF A REAL VERSATILE MOLECULE

About Authors:
C.P.Meher
Asst. Professor
Maheshwara Institute of  Pharmacy,
Chitkul, Patancheru, Medak, A.P
chaitanyameher84@gmail.com

ABSTRACT
Pyrazole, a 5-membered heterocyclic diazole alkaloid composed of three carbon atoms and two nitrogen atoms in adjacent positions, is a prevalent scaffold in drug discovery programs. The aim of this review is to provide an overview of diverse pharmacological activities of pyrazole moiety.This review highlighted recent reports of antimicrobial, anticancer, ACE inhibitory, antiviral as well as anti-inflammatory activities of pyrazole. The purpose of this review was to collate literature work reported by researchers on pyrazole for their varoius pharmacological activities and also reported recent efforts made on this moiety.


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.


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.


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.


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.


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.



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.


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.


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