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V. Sai Saraswathi ¹, D. Saravanan ², J. Padmavathy ², I. Aparna Lakshmi ², D. Raju ³, Ch. Praveen kumar ², C. R. Prakash ⁴

Affiliations
1 Vellore Institute of Technology, Vellore – 632 007, Tamil Nadu, IN
2 Ratnam Institute of Pharmacy, Pidathapolur, Nellore – 524 346, Andhra Pradesh, IN
3 SRM College of Pharmacy, SRM University, Kattankulathur, Chennai-603203, TamilNadu, IN
4 DCRN College of Pharmacy, Ilkollu, Andhra Pradesh, IN

Abstract

Naproxen suffers from the general side effects of NSAIDs, owing to presence of free carboxylic acid group. The study aimed to retard the adverse effects of gastrointestinal origin. Ten prodrugs of Naproxen were synthesized by amidation with N-Substituted-2-chloroacetamide. Purified synthesized prodrugs were characterized by their M.P., TLC, IR, ¹H NMR, MS and elemental analysis. The purity of the synthesized prodrugs was monitored by HPLC. Synthesized prodrugs were subjected to acute oral toxicity studies, anti-inflammatory activity and reduced ulcerogenic activity. Marked reduction of ulcerogenic activity and anti-inflammatory activities were obtained in all cases as compared to Naproxen. Among synthesized prodrugs, viz. A-5, A-6 and A-8 showed significant anti-inflammatory activity and A-2 and A-5 showed reduced ulcerogenic activity compared to Naproxen. In acute oral toxicity studies, all synthesized prodrugs were found to be non toxic at dose of 2000 mg/kg.

Keywords

Naproxen, Prodrugs, Glycolamide Ester Conjugates, Characterization, Pharmacological Activity.

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C. R. Prakash ¹, S. Raja ², G. Saravanan ³, P. Dinesh Kumar ⁴, T. Panneer Selvam ⁵

Affiliations
1 Department of Pharmaceutical Chemistry, DCRM Pharmacy College, Inkollu. Andhra Pradesh, IN
2 Department of Pharmaceutical Chemistry, DCRM Pharmacy College, Inkollu, Andhra Pradesh, IN
3 Medicinal Chemistry Research Laboratory, Bapatla College of Pharmacy, Bapatla-522 101, (A.P), IN
4 Dep. of Pharmaceutics, Rahul Institute of Pharmaceutical Science and Research, Chirala-523157, (A.P.), IN
5 Department Pharmaceutical Chemistry, Srinivas College of Pharmacy, Mangalore-574142, Karnataka, IN

Abstract

In the present study, a series of novel Schiff bases of isatin were synthesized by condensation of imesatin with different aromatic aldehydes. The imesatins were synthesized by reaction of isatin with p-phenylenediamine. The chemical structures of the synthesized compounds were confirmed by means of IR, 1H-NMR, mass spectroscopy, and elemental analysis. These compounds were screened for antioxidant activity by DPPH radical scavenging activity. In this method, the compound 3-(4-(4-dimethylaminobenzylideneamino) phenylimino) indoline-2-one (5c) showed highest antioxidant activity because of the presence of electron donating group.

Keywords

Antioxidant, Isatin, Schiff Base.

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T. Panneer Selvam ¹, G. Saravanan ², C. R. Prakash ³, P. Dinesh Kumar ⁴

Affiliations
1 Department Pharmaceutical Chemistry, Srinivas College of Pharmacy, Mangalore-574142, Karnataka, IN
2 Medicinal Chemistry Research Lab, Bapatla College of Pharmacy, Bapatla-522101, Andhra Pradesh, IN
3 Department Pharmaceutical Chemistry, DCRM Pharmacy College, Inkollu-523167, Andhra Pradesh, IN
4 Department of Pharmaceutics, Rahul Institute of Pharmaceutical Science & Research, Chirala-523157, Andhra Pradesh, IN

Abstract

A series of 1-(4-substitutedphenyl)-3-phenyl-1H-pyrazole-4-carbaldehyde 4a-e has been synthesized and tested for their anti-inflammatory and analgesic activities. Formation of the pyrazole derivatives was achieved by treating vilsmeier-haack reagent. The newly synthesized compounds were evaluated for their anti-inflammatory and analgesic activities compared to indomethacin, flufenamic acid and diazepam as standard drugs. The detailed synthesis, spectroscopic and toxicity data are reported.

Keywords

Pyrazole, Anti-Inflammatory Activity, Analgesic Activity.

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G. Saravanan ¹, V. Alagarsamy ², C. R. Prakash ¹, P. Dinesh Kumar ¹, T. Panneer Selvam ¹

Affiliations
1 Medicinal Chemistry Research Laboratory, Bapatla College of Pharmacy, Bapatla-522101, (A.P), IN
2 Medicinal Chemistry Research Laboratory, M.N.R. College of Pharmacy, Sangareddy-502294, (A.P), IN

Abstract

Thiazoles have a long history of having number of pharmacological activities such as anti-microbial, analgesic and anti-inflammatory activities. Pyrazoles shows promising anti-microbial, analgesic and anti-inflammatory activities. In the present study, novel thiazoles (8a - 8j) were synthesized by incorporation of pyrazole moiety at 2^nd position of 2-hydrazinyl-N-(4-phenylthiazol-2-yl) acetamide (5) by treating with chalcones (7a-7j). The chemical structures of the synthesized compounds were confirmed by means of IR, ¹H-NMR, Mass spectral and Elemental analysis. All the spectral data were consistent with the assigned structure. The synthesized compounds were investigated for analgesic activity by tail immersion method in mice. All the synthesized compounds exhibited mild to good analgesic activities. Among the synthesized compounds, 2-(5-(4-dimethylaminophenyl)-3-phenyl-4,5-dihydropyrazol-1-yl)-N-(4- phenylthiazol-2-yl) acetamide (8c) and 2-(5-(4-methylphenyl)-3-phenyl-4,5-dihydropyrazol-1-yl)-N-(4-phenylthiazol- 2-yl) acetamide (8e) exhibited highest analgesic activity.

Keywords

Thiazole, Pyrazole, Chalcone and Analgesic Activity.

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