Chemistry Articles

20 July 2011

A Review of High - Throughput Screening Approaches for Drug Discovery

About Authors: Ashwini K. Reddy, Swetha, Gauthami, Srivally, Masoom - M.Pharm, Helen Sheeba - Assistant Professor. Malla Reddy Institute of Pharmaceutical Sciences, Hyderabad.

Reference ID: PHARMATUTOR-ART-1076

HIGH - THROUGHPUT screening (HTS) is an approach to drug discovery that has gained widespread popularity over the last three or four years. HTS is the process of assaying a large number of potential effectors of biological activity against targets (a biological event). The methods of HTS are applied to the screening of combinatorial chemistry, genomics, protein, and peptide libraries. The goal of HTS is to accelerate drug discovery by screening large libraries often composed of hundreds of thousands of compounds (drug candidates) at a rate that may exceed 20,000 compounds per week. This paper will focus on assay adaptations, robotic equipment, and implementation strategies that allow HTS programs to be successful. Ultrahigh throughput screening (UHTS) issues (testing of 100,000 compounds / day) will also be discussed.
2 May 2011

Click chemistry - A New Approach for Drug Discovery

About Author: Shekh Yunus1, Nirmal Das Adhikary2 and Partha Chattopadhyay*
National Institute of Pharmaceutical Education and Research
at IICB, Jadavpur, 4 Raja S.C. Mullick Road, Kolkata-700032, India

Source of Support: NIPER Kolkata and IICB

ABSTRACT:
Click chemistry is a modular approach that uses only the most practical and reliable chemical transformations. Its applications are increasingly found in all aspects of drug discovery, ranging from lead finding through combinatorial chemistry and target-templated in situ chemistry, to proteomics and DNA research, using bioconjugation reactions. The copper-(I)-catalyzed 1,2,3-triazole formation from azides and terminal acetylenes is a particularly powerful linking reaction, due to its high degree of dependability, complete specificity, and the bio-compatibility of the reactants. The triazole products are more than just passive linkers; they readily associate with biological targets, through hydrogen bonding and dipole interactions.
19 April 2011

Synthesis & Evalution Of Triazolo Phthalazine Derivatives As Anticonvulsant Agents

About Author:
ANAND GAURAV, SMITA SINGH
M.Pharm,
Assistant Professor

Abstract:
The importance of the phthalazine as a nucleus with medicinal properties is well established, since many decades. This nucleus possess potent anticonvulsant activity with high protection index value that why this property is use for the treatment that are related to mental disorder, like seizures. Phthalazine and its derivatives possessing triazines nucleus has attracted great attention in recent years due to wide variety of biological activity particularly anticonvulsant activity keeping in view the continuing interest in phthalazine and its derivatives. The present study is aimed at synthesizing safer and effective anticonvulsant triazolo-phthalazine derivatives to evaluate them for anticonvulsant activity.
9 April 2011

Synthesis and biological evaluation of newer analogues of 2,5-disubstituted 1,3,4-oxadiazole as antioxidant and anticonvulsant agents

About Authors: Arun Dureja*, Kalpana Divekar and M.S.Sandhyavali
Department of Pharmaceutical Chemistry,
Dayananda Sagar College of Pharmacy,
Kumaraswamy Layout,
Bangalore

Abstract
A series of 3-(4-acetyl-5H-5-phenyl-4,5-dihydro-1,3,4-oxadiazol-2-yl)- 2H-chromen-2-one derivatives were synthesized and evaluated for their anticonvulsant and antioxidant activities. Initially Ethyl-2-oxo-2H-chromene-3-carboxylate was prepared by reacting Salicylaldehyde with Diethyl malonate in presence of piperidine. This compound was treated with hydrazine hydrate to give aromatic hydrazides. Those hydrazides were refluxed with different aldehydes to form arylidines, which were then treated with acetic anhydride to form 3-(4-acetyl-5H-5-phenyl-4,5-dihydro-1,3,4-oxadiazol-2-yl)- 2H-chromen-2-one derivatives. The structures of synthesized compounds were characterized and confirmed by IR and ¹HNMR and then screened for antioxidant activity by DPPH reduction method and anticonvulsant activity by MES method. The investigation revealed that out of eight newly synthesized derivatives five were found to possess significant anticonvulsant activity but none of the derivative was found with antioxidant activity.
31 March 2011

Chemistry of Tamsulosin HCl and Estimation of Tamsulosin HCl by high performance liquid chromatography.

About Authors: Kollu Varuni, B.pharm
Vathsalya college of pharmacy,
J.N.T.U University

Introduction:
Tamsulosin is a selective, potent and competitive a 1 – adrenoreceptor antagonist and has a greater affinity for these receptors, predominantly present in the human prostate. Literature survey reveals that several methods like HPLC,HPLC-MS and LC-MS were reported for the estimation of Tamsulosin hydrochloride in combination with other drugs as well as in biological fluids [1- 3]
29 March 2011

RESEALED ERYTHROCYTES AS DRUG CARRIERS

About Authors: Varun Raj Vemula*¹, Swathi Thakkalapally², Chaitanya Kumari Bairi^3

1DepartmentofPharmaceutical Chemistry, Vikas College of Pharmacy, Jangaon, Warangal. Affiliated to Kakatiya University.
²Department of Pharmaceutics, Care College of Pharmacy, Warangal. Affiliated to Kakatiya University.
³Department of Pharmaceutics, TallaPadmavathi College of pharmacy, Warangal. Affiliated to Kakatiya University.

Abstract:
Carrier erythrocytes have been evaluated in thousands of drug administration in humans proving safety and efficacy of the treatments. Carrier erythrocytes, resealed erythrocytes loaded by a drug or other therapeutic agents, have been exploited extensively in recent years for both temporally and spatially controlled delivery of a wide variety of drugs and other bioactive agents owing to their remarkable degree of biocompatibility, biodegradability and a series of other potential advantages. Biopharmaceuticals, therapeutically significant peptides and proteins, nucleic acid-based biologicals, antigens and vaccines, are among the recently focused pharmaceuticals for being delivered using carrier erythrocytes. In this review article, the potential applications of erythrocytes in drug delivery have been reviewed with a particular stress on the studies and laboratory experiences on successful erythrocyte loading and characterization of the different classes of biopharmaceuticals.

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26 March 2011

Synthesis and evaluation of carbodithioic acid esters of naphthylmethylamine, a novel class of spermicides

About Authors
M. M. Singhal, Monica Gupta
Department of chemistry,
Delhi Institute of Pharmaceutical science & Research,
New Delhi, India

Affiliation Affiliated from Govt. of NCT Delhi

Abstract :
Carbodithioic acid esters of naphthylmethylamine prepared by replacing the amino function in amino methyl side chain with carbodithioic acid ester group and by adding various S-2-hydroxy propyl ester of dialkyl carbodithioic acid at amino group. Some of these compounds showed better spermicidal activity. The study revealed that incorporation of carbodithioic acid residue directly into naphthylmethylamine leads to compounds with better spermicidal activity and naphathalene-1-yl-methyl-carbodithioic acid-3-dialkyl amino-2-hydroxy-propyl ester has shown better profile than nonoxynol-9. Further, lead optimization may yield a potent spermicide.

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A Review of High - Throughput Screening Approaches for Drug Discovery

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