THE EFFECTS OF ACTIVE AND INACTIVE RECOVERY AFTER EXERCISE HIIT ON HSP72 AND PLASMA CORTISOL RESPONSE

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ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6220 ]

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2016- VOLUME 5, JUNE ISSUE 6

Research Article

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Othman A. Gubara*, Tariq O.A. Gubara, Mohammed O. Ayoub, Shayoub M. El. A., Ali M. EL. Hassan., Abd Alla Ah. M. El. A, Ali. M. El. A., Asma Nour Eldim Mahmmoud

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Sumya Afroze, Mohammad Shah Hafez Kabir*, Md. Saiful Islam Arman, Belkis Fatama, Md. Shohel Hossain, Fahmida Abdullah Tuly, Mosarrof Hossain, Md. Najem Uddin, Md. Mominur Rahman

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Mohammad Shah Hafez Kabir*, Md. Saiful Islam Arman, Sumya Afroze, Md. Shohel Hossain, Fahmida Abdullah Tuly, Mosarrof Hossain, Md. Najem Uddin, Hosna Banu, Md. Mominur Rahman

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Haifa M. Fahad*

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Bambang Tri Purwanto*

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Arhoghro E. M.*, John T. R.1, Eboh A.S., Prohp T. P. and Angalabiri-Owei B. ABSTRACT PDF [ DOI : 10.20959/wjpr20166-5835 ]

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D. H. D Mohmoud, As. N. Hisham Osman

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M. González-Pérez*

POLYMORPHISM IN ENDOPLASMIC RETICULUM AMINOPEPTIDASE-L (ERAP1) GENE IN IRAQI PATIENTS WITH ANKYLOSING SPONDYLITIS

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Ahmed Yaseen AL-Tarboolii*, Hameed Majeed Jassim, Mohammed Hadi Alosami, Saleh Ahmed Wohaieb

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M.R.A. Mollah*, M. A. Ali, M.M. Rahman, M.Z.H. Prodhanand T. Hasan ABSTRACT PDF [ DOI : 10.20959/wjpr20166-5559 ]

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Danladi Chiroma Husaini*, Diomar Salazar, Roberta Thimbriel, Innocent Ejiofor Nwachukwu and Augustine 'Dele Domingo

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Kiran C. Nilugal*, Santosh Fattepur, Hamid Ali Kazi, May Florence Dela Cruz Bacayo, Mohd. Fadli Asmani and Asif Iqbal Chittur

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Deepak Chandra*, Gunjan Kohli, Kundan Prasad, G.Bisht, Vinay Deep Punetha, Amit Panwar and Veena Pande

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Dr. Akanksha Mahajan*, Dr. Anita K. Gupta, Dr. Gursatinder Singh ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6191 ]

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N. Shivakrishna*, G. Venkateshwarlu, H. Ramana, M. Rajeshwari, B. Balakrishna, S. Sathish

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Divya Bade*, Shivashankaramurthy K. G., Apoorva B. M., Sonali Mohanty, Nayana M. R. ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6253 ]

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Rupashree Salvi, Nikita Naik and Arati Potphode*

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Neha Atwal*, Chanpreet Singh Bindra and Upendra K. Jain ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6266 ]

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Vasava Shilpa N.1 and Rajashree C. Mashru*

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Kumar Manendra*

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T. Ananthi* and R. Kalaiselvi

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Napa Lakshmi Priya, Gopinath S.*, Shanmuganathan S. and Thameemul Ansari L. H. ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6315 ]

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K. Sudhakar Babu, V. Prabhakar*, L. K. Ravindranath, S. Shabhari Prasad, J. Latha ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6316 ]

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M. Chandana Priya, M. Manasa, S. Jakriya, C. Kavya, G. Upendra Sai, S. S. Somanathan* and D. Ranganayakulu

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Dr. C. Jayabhaskar, Dr. M. Ramadevi* and Dr. K. Raghavendhra ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6323 ]

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Santosh Raveendra Karajgi*, Ramaling Bhagavantrao Kotnal, Amruta Shankar Patil, Navanath Vishwanathappa Kalyane

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Vijakumar L. Chavan* and Rajendra R. Rane

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R. Rajapandi*, Aswathy S. R. and B. Sreedharran

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Chandrakant D. Pawar, Dattatraya N. Pansare, Rohini N. Shelke, Devanand B. Shinde*

KINETIC SPECTROPHOTOMETRIC DETERMINATION OF DRUGS BASED ON OXIDATION BY ALKALINE KMnO4

M. Prashanthi and G. Venkateshwarlu*

NEUROPROTECTIVE ACTIVITY OF SEEDS OF CAESALPINIA BONDUCELLA (ROXB) IN OXIDATIVE STRESS INDUCED RATS

Shamabai D. Hosamani*, Dr. Shivakumar S. Inamdar, Ravi Ranjan Kumar Pandey, Pallavi P. Kulkarni and Harika Vatikuti

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Sangeeta A. Pingale*

DETERMINATION OF HERBAL PRODUCT CARDIOL VATI BY ICPMS VALIDATION AND APPLICATION

Raju P. Suryawanshi* and Sudhir S. Kamat

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Rehana Parveen* and Ranjeet Kumar Bhargav

OPTIMIZED DEVELOPMENT AND EVALUATION OF MICROBIALLY TRIGGERED BASED ORNIDAZOLE MICROSPHERES FOR COLON TARGETING

Verma Surender*, Bhalla Gaurav and Goyal Gourav ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6338 ]

FLOURESCENCE ANALYSIS OF MUSA PARADISIACA L. OF SUBFAMILY MUSACEAE

Meenakshi Vaidya*

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Mable Babu* and Raghu M. T.

EXPERIMENTAL STUDIES ON WOUND HEALING PROPERTIES OF ANDROGRAPHIS ECHIOIDES (L.) NEES IN WISTAR ALBINO RATS

Mohd Rafiq* and Dr. Sadath Ali

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Sujay Patil*, Richa Bhardwaj and Merlyn Gomes

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M. Krishnaveni*, Sreerenjini V. M. and J. Santhoshkumar ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6349 ]

EFFICACY OF PLANTAR IONTOPHORESIS WITH AQUEOUS SOLUTION OF GUGGULU RESIN IN THE MANAGEMENT OF PADAKANTAKA (PLANTAR FASCIITIS): A PILOT STUDY

*Dr. Alpona Ray, Dr. Alok Kumar, Dr. Narinder Singh, Dr. Ashok Kumar, Dr. J. P. Verma and Dr. P. Hemantha Kumar

AIR POLLUTION TOLERANCE INDEX AND ANTIOXIDANT ACTIVITY OF PLANT LEAVES COLLECTED AT SAGO SERVE INDUSTRY, SALEM, TAMIL NADU, INDIA.

M. Krishnaveni*, Harsha V. Rari and Santhosh Kumar J. ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6360 ]

SYNTHESIS, CHARACTERIZATION AND INVITRO ANTIMICROBIAL ACTIVITY OF MIXED ‘TRANSITION METAL - BARIUM TARTARATE’ COMPLEXES

Milind B. Ubale*, Murlidhar A. Betallu, Vijay B. Tadke, Shridhar M. Vhankate and Girish R. Pathade ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6361 ]

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PROTECTIVE EFFECT OF CALENDULA OFFICINALIS L. AGAINST POLLUTED WATER INDUCED HEPATOTOXICITY IN ALBINO RATS.

Ab Rashid Wani, Sheeraz Ahmad Wagay*, Ghulam Mohammad jan, Sudhanshu Dhar Dwivedi and Syed Zeenat khurshid

PHYTOCHEMICAL SCREENING AND ANTIMICROBIAL ACTIVITY OF SENNA UNIFLORA (MILL.) H.S. IRWIN & BARNEBY

Thangarathinam Jothirathinam* and Violet Dhayabaran Victor ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6370 ]

STUDY ON INCREASE IN PRACTICE OF NON-PRESCRIBED ANTIBIOTIC USE IN TAMILNADU STATE, INDIA.

R. Naveenkumar*, R. Kamalraj and K. Velmurugan ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6371 ]

EVALUATION OF SERUM ALBUMIN AND OTHER BIOCHEMICAL PARAMETERS IN PATIENTS WITH CHRONIC PERIODONTITIS

Dr. Reshama Y. Sawant* and Dr. Chitra Y. Dhume

PHYTOCHEMICAL AND ANTIMICROBIAL ACTIVITY OF ORYZA RUFIPOGON GRIFF. FROM NALLAMALAI FOREST AREA.

Lakshmi Devi A. and Yasodamma N.*

PLEOROTUS SPS. MUSHROOM CULTIVATION WITH DRIPPING SYSTEM IN ODD SEASONS

Priyam Singh*, Rajendra Vishwakarma, Pramod Bhartiya, Rajni Shrivastava and Padma Shrivastava

EVALUATION OF SAFETY OF ARIFLEX TABLET - A POLYHERBAL FORMULATION IN SPRAGUE DAWLEY RATS

Vasant E. Narke*, Nitin V. Athavale, Ujwala V. Khisti, Sanjay U. Nipanikar ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6384 ]

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Sheeraz Ahmad Wagay*, Ab Rashid Wani, Ghulam Mohammad Jan, Tawseef Ahmad Bhat and Surayakant

EVALUATION OF NOOTROPIC ACTIVITY OF DIFFERENT EXTRACTS OF VIGNA MUNGO (LINN) IN RATS

Saleem Ahmed and Zeeshan Afsar*

STUDY ON ANTICONVULSANT AND ANXIOLYTIC ACTIVITIES OF LEAVES EXTRACTS OF ACORUS CALAMUS LINN. IN MICE

Ravi Ranjan Kumar Pandey*, Dr. Shivakumar S. Inamdar, Shamabai D. Hosamani, Prateek Reddy and Anil S. Rathod

RENAL PROTECTIVE ACTIVITY OF HELIOTROPIUM INDICUM IN RIFAMPICIN INDUCED NEPHROTOXICITY RATS

Mokhalad Waheeb Abdullah, Jaffar S. K., Ghousia Begum and Balasubramanian Sathyamurthy* ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6393 ]

EFFECT OF MALATHION ON THE BLOOD GLUCOSE LEVEL IN THE INDIAN LIZARD CHAMELEON ZELENICUS.

Dr. Bishnu Charan Pradhan*

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Dr. Reshama Y. Sawant* and Dr. Chitra Y. Dhume

A COMPARATIVE STUDY OF TREATMENT DURATION FOLLOWUP AND INCLINATION TOWARDS TREATMENT FROM GOVERNMENT HOSPITALS OR PRIVATE CLINCS BY GERIATRIC PATIENTS WITH MENTAL HEALTH DISORDERS IN GUJARAT.

*Michael W. D’Souza and Rajesh Mehrotra

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Kolluri Ramesh* and P. Thriveni

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K. Lakshmi Surekha*, N. N. Srinivas Rao, C. Murali Krishna Goud, K. Ramya, U. Srikanth, G. Rajeswari, A. Sudha Rani, G. Keerthi, K. Shiva Durga Prasad, Dr. H. Ramana

IMPACT OF MICROWAVE HEATED WATER ON GERMINATION OF SEEDS AND GROWTH OF PLANT SYSTEMS

Dr. K. Radha, Dr. B.V. Mrudula Rao1, M. Sujatha, *Dr. D. Sirisha ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6418 ]

DEVELOPMENT AND EVALUATION OF METOPROLOL SUCCINATE MICROPARTICLE-HYDROCHLOROTHIAZIDE SUSTAIN RELEASE MATRIX TABLET

Prajakta A. Ahire*, Harshada Deoghare, Rajendra Surawase, Avish Maru ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6428 ]

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*Neelam Parab and Sharda Vaidya

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TO EVALUATE THE ANTI-DIABETIC ACTIVITY OF COMMERCIALLY AVAILABLE EXTRACT OF TINOSPORA CORDIFOLIA IN ANIMAL MODEL

Nishant Pathak, Arkapal Bandyopadhyay*, Rakesh Chandra Chaurasia, Kachnar Verma ABSTRACT PDF [ DOI : 10.20959/wjpr20166-6430 ]

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www.wjpr.net

Vol 5, Issue 6, 2016.

271 Purwanto

.

World Journal of Pharmaceutical Research

THE BENZOYLSALICYLAMIDE AND THE

4-FLUOROBENZOYLSALICYLAMIDE, THE NOVEL SALICYLAMIDE

DERIVATIVES AND THE ANALGESIC ACTIVITIES COMPARATIVE

Bambang Tri Purwanto*

Departement of Pharmaceutical Chemistry Faculty of Pharmacy, Universitas Airlangga

Surabaya, Indonesia.

ABSTRACT

The benzoylsalicylamide and the 4-fluorobenzoylsalicylamide as the

novel salicylamide derivatives had been synthesized. The novel

compound benzoylsalicylamide and the 4-fluorobenzoylsalicylamide

were synthesized by The Schotten Baumann method, where the

reaction were between salicylamide and benzoyl chloride also

4-fluorobenzoyl chloride. The analgesic activity test was done for the

benzoylsalicylamide and the 4-fluorobenzoylsalicylamide compound

by writhing test and compared with salicylamide as the standard

compound. The benzoylsalicylamide compound yield was 58%, had a

crystal shiny white needles and gave one spot in Thin Layer

Chromatography with three different eluents. The compound melting

point was different from the salicylamide and showed greater. The

structure identification from the new compound was analysed by UV, IR,

1-

H-NMR, the

result showed that the novel compound was benzoylsalicylamide

.

The analgesic activity test

from benzoylsalicylamide had a greater activity if compare with the standard compound

salicylamide. The 4-fluorobenzoylsalicylamide compound yield was 64% had a white powder

and gave one spot in Thin Layer Chromatography with three different eluents. The compound

melting point was different from the salicylamide and showed greater. The structure

identification from the new compound was analysed by UV, IR,

1-

H-NMR, the result showed

that the novel compound was 4-fluorobenzoylsalicylamide

.

The analgesic activity test from

4-fluorobenzoylsalicylamide had a greater activity if compare with the standard compound

salicylamide also from the benzoylsalicylamide. The benzoylsalicylamide and

4-fluorobenzoylsalicylamide had been synthesized as the novel salicylamide derivatives and the

World Journal of Pharmaceutical Research

SJIF Impact Factor 6.805

Volume 5, Issue 6, 271-277. Research Article

ISSN 2277

–

7105

*Corresponding Author

Dr. Bambang Tri

Purwanto

Departement of

Pharmaceutical Chemistry

Faculty of Pharmacy,

Universitas Airlangga

Surabaya, Indonesia.

Article Received on

06 April 2016,

Revised on 26 April 2016,

Accepted on 16 May 2016

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www.wjpr.net

Vol 5, Issue 6, 2016.

272 4-fluorobenzoylsalicylamide had a higher analgesic activity if compare with salicylamide as

the standard compound also from the benzoylsalicylamide.

KEYWORDS:

Benzoylsalicylamide; 4-fluorobenzoylsalicylamide; Synthesis; analgesic

activity test.

INTRODUCTION

In this periode the existing of the new compound which will be use as a drug is a challenges.

The develop the structure of the existing drug molecules were made by the scientific

researches or searching and finding the new drug candidate compounds that have potent

pharmacological activity.

[2]

To obtain a new compound that has the potential as a new drug candidate, the modification of

the drug molecul (by chemical synthesis process) is needed, with the consideration that new

compounds which will be obtained had a relatively pure compounds and has higher

pharmacological activity than the parent compound.

[7]

The analgesics are the drugs which be use as a relieve pains and were always required by the

hospitals, the clinicians and the individuals. The circulation of the analgesic drugs were used

in the hospital is 43% while 32% in the pharmacies and 27% in the drug store, so these

indicate that the analgesic drugs are needed and has great opportunities for further

development.

Salicylamide is one of the analgesic compounds of the salicylic acid derivatives which was

used by the publics. Pharmacological activity as pain relievers like aspirin, but salicylamide

not have the pharmacological activity as the anti-inflammatory and the anti-rheumatic.

[1]

To enhance the analgesic potency owned by salicylamide it is necessary to modify the

structure so that it will be obtained the novel salicylamide derivatives which be predicted

would have a higher analgesic potency than salicylamide.

[15]

Salicylamide pharmacological activity is highly dependent on the physical chemical

properties, an increase in the value of the log P from the novel compounds salicylamide

derivatives is expected to increase the potential for the pharmacological activity as an

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Vol 5, Issue 6, 2016.

273 To produce a novel compound, the synthesis reactions carried salicylamide derivative with

Schotten-Baumann method, whereas for the analgesic activity test was conducted by the

writhing test method.

[4, 8, 14]

In the novel compounds salicylamide derivatives which have been synthesized, looks have

the same chromophore moities with salicylamide as the parent compound, but an increase in

the value of the liphophylic parameter, so the novel compounds salicylamide derivatives

expected will have a higher analgesic potency than the salicylamide.

METHOD

1. Synthesis benzoylsalicylamide and 4-fluorobenzoylsalicylamide

Siswandono

[11]

has been synthesized the new derivatives benzoylurea which had the central

nervous system acitivties by the Schotten Baumann method.

Bambang Tri Purwanto

2

has been successfully used the Schotten Baumann method to

synthesized the N-bromobenzoylampicillin.

Bambang Tri Purwanto

[3]

also used the Schotten Baumann method to synthesized the

benzoylphenylurea derivatives.

Hardjono

[6]

has been successfully by using the method Schotten Baumann to modified urea

structure became benzoyloxyurea derivatives.

Synthesis reaction to obtain the novel salicylamide derivatives performed by reacting the

salicylamide (0.015 mol) with some derivative benzoyl chloride, among others, benzoyl

chloride, 4-fluorobenzoyl chloride (0.0125 mol) were dissolved in acetone. The reaction was

performed at a temperature of 5°C for 2 hours slowly while stirring, to maintain stability and

the need to accelerate the reaction was added a solution of pyridine as a catalyst. After the

reaction was finished the sodium bicarbonate solution is added to the reaction until a neutral

reaction. The crystals that occur was filtered, then was made recrystallization with hot

methanol solvent.

[4, 8, 13]

2. The purity test and the structure characterization

a.

The purity test of the compounds which were synthesized performed by thin layer

(20)

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Vol 5, Issue 6, 2016.

274 (ethyl acetate: n-hexane = 7: 3; chloroform: ethyl acetate = 7: 3 and n-hexane: ethyl

acetate: methanol = 8: 3: 1)

b.

Characterization of the structure of the new compounds synthesized were done by using

an infrared spectrophotometer (KBR pellet) and spectrometer

1

-HNMR (solvent

DMSO-d

6

).

[9, 10]

3. The analgesic activity test

The analgesic activity test from the O-benzoylsalicilic acid by the writhing test method was

done by Dyah

et.al

.

[5]

The analgesic activity test using writhing test method with the experimental animals

(Mus

musculus

) aged 2-3 months, Blab C strain, weighing 20-30 grams and physically showed no

disability. Doses used in trials of analgesic activity of the novel derivatives salicylamide was

10, 25, 50, 100 and 200 mg / kg BW and administered by intra-peritoneal, the preparations

were made in the form of a suspension in a solution of sodium carboxy methyl cellulose.

Salicylamide used as a comparison agent with the same dose.

RESULT AND DISCUSSION

1. The compound benzoyl salicylamide (C

14

H

11

NO

3

)

These compounds form is crystal shiny white needles, odorless and has a yield of 58%.

Melting point 119

o

C. Characterization of the structure, IR (KBr pellet): 3546 cm

-1

(OH),

3232 cm

-1

(NH), 1712 cm

-1

, 1671 cm

-1

(CO amide), 1480 cm

-1

(C = C aromatic);

1

H-NMR

(DMSO-d

6

) 12.02, s (OH); 6.4, s, (NH); 6.8-8.2 m, (C

6

H

5

).

2. The compound 4-fluorobenzoyl salicylamide (C

14

H

10

FNO

3

)

This compound is in the form of white powder, odorless and has a yield of 64%. The melting

point was 216

o

C. Characterization of the structure, IR (KBr pellet): 3218 cm

-1

(NH

secondary), 1717 cm

-1

(CO amide), 1484 cm

-1

(C = C aromatic), 1273 cm

-1

(CF);

1

H-NMR

(DMSO-d

6

): 12.98, s (OH); 6.92-8.30, m (C

6

H

5

).

All of the compounds synthesized showed only 1 different spot and the Rf value for each

compound different with the Rf of the salicylamide as the parent compound, using thin layer

chromatography for the purity analysis with 3 different eluent solvent. Besides that, this

result is reinforced by differences in melting point the compounds synthesized by the parent

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Vol 5, Issue 6, 2016.

275 been formed and were different from the parent compound salicylamide, also means all the

compounds synthesized can be said to be pure and not contaminated by other materials.

Based on the results the yield of each compound synthesized was seen that the results of the

yield above 50%, indicating that the Schotten Baumann method was the chosen method to

carry out the synthesis of derivatives salicylamide by means of molecular modifications from

the parent compound salicylamide by substitution with a moety of benzoyl (benzoylation).

The characterization of the structure which were analysed by the spectrophotometer IR

shown that the compounds synthesized have been different with a parent compound

salicylamide particularly evident from the specific carbonamide bond (CO amide) and

reinforced by the results of spectra

1

H-NMR, which showed the number of the hydrogen

atoms of each compound derivatives of salicylamide has different from the salicylamide

compound.

So based on the data above, it can be concluded that the compounds synthesized were

benzoylsalicylamide and 4-fluorobenzoylsalicylamide.

The analgesic activity test from the novel derivatives salicylamide can be seen in the figure

below.

Fig 1: % effect inhibitory analgesic activity from the novel salicylamide derivatives.

Based on the analgesic activity which was shown by the percentage of inhibition of the pain

in the figure 1 above, showed the curve that all new salicylamide derivative compounds have

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Vol 5, Issue 6, 2016.

276 The addition of benzoyl group at salicylamide derivates will increase the liphophylic

parameter value so the novel salicylamide derivative compounds have the capability of

penetration into larger biological membrane and harmony in binding with the receptor

molecule will be higher. The highest analgesic activity was shown by the novel

4-fluorobenzoylsalicylamide compound at the dose 200mg/kg BW. The fluoro moeity at para

position

showed

that

the

4-fluorobenzoylsalicylamide

more

lipophylic

than

benzoylsalicylamide or salicylamide, so the 4-fluorobenzoylsalicylamide had a higher

analgesic activity than both.

CONCLUSION

The novel salicylamide derivatives, benzoyl salicylamide and 4-fluorobenzoyl salicylamide,

has been succeesfully synthesized and all have higher analgesic activities than the

salicylamide compound. The 4-fluorobenzoylsalicylamide had a highest analgesic activity.

REFERENCES

1. Abraham, DJ. 2003. Burger's Medicinal Chemistry and Drug Discovery, Sixth Edition,

Volume 1: Drug Discovery, John Wiley and Sons, Inc., New York.

2. Bambang Tri Purwanto, 1991, Synthesis and the antibacterial activity test from

N

-para-bromobenzoylampicilin against

S.aureus

ATCC 7500 and

E.coli

ATCC 7500, 1991,

Unpublished Master Thesis, Universitas Gadjah Mada, Yogyakarta, Indonesia.

3. Bambang Tri Purwanto, 2010, QSAR, Synthesis the benzoylphenylurea derivatives and

the central nervous system activity test on mice, Dissertation, Airlangga University,

Surabaya Indonesia.

4. Clayden, G., Warren, Wothers, 2001, Organic Chemistry, Oxford University Press, New

York: 279-303.

5. Diyah, N.W., Purwanto, Siswandono, Hardjono, S., Purwanto, B.T., Susilowati, R. 2007.

The Structure Modification And Analgesic Activities Of

O

-Benzoylsalicylic Acid

Derivatives. USM

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