andhra Pradesh, India
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A series of 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3- substituted hydrazino thiazolo (2,3-b) quinazolines have been synthesized to meet the structural requirements essential for anti-inflammatory and antinociceptive properties. The synthesized series of heterocycles, 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazoline by the reaction of 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl thiazolo (2,3-b) quinazolin-3(2H)-one with appropriate hydrazine hydrate and ketones/aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid as presented in Scheme 1. Their antinociceptive activity were evaluated by tailflick technique, anti-inflammatory was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index determined by reported protocol. The compounds exhibited the lowest ulcer index (0.51 ± 1.63, 0.48 ± 1.28 and 0.50 ± 1.53, respectively. The 6,7,8,9-tetrahydro-5H-5-hydroxy phenylhydroxy-2-benzylidine-3-(N'-3- pentylidenehydrazino) thiazolo (2,3-b) quinazoline and 6,7,8,9-tetrahydro-5H-5- hydroxy phenyl-2-benzylidine-3-(N'-2-pentylidene- hydrazino) thiazolo (2,3-b) quinazoline exhibited the most potent antinociceptive and anti-inflammatory activities.

Nagabhushanam M.V.,DCRM Pharmacy College | Prabhakar C.H.,Chilukuri Balaji Pharmacy College
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2011

The object of this article is to investigate enhancement of the dissolution rate of Mefenamic acid (MA) using solid dispersion method. A series of solid dispersions of the drug MA using poly ethylene glycol 6000 (PEG 6000), poly vinyl pyrrolidone K-30 (PVP K-30), hydroxyl propyl methyl cellulose (HPMC) and micro crystalline cellulose (MCC) as carriers were prepared following the kneading and solvent evaporation methods. Dissolution studies using the USP XIV apparatus were performed for solid dispersions of MA. The FTIR spectra of samples were taken on the FTIR spectrophotometer using the KBr disk to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. IR spectroscopy showed no change in the structure of MA. Powder x-ray diffractometry was carried out to find out the changes in crystalline nature of the MA. The samples were analyzed by DSC using a Mettler Toledo S R System. Solid dispersions at 2:2:6 ratio of MA: HPMC: MCC, a 6.94 fold increase in the dissolution rate of MA was observed. Solid dispersions, prepared using HPMC showed greater improvement in dissolution profile of MA prepared by solvent evaporation technique. Thus, the solid dispersion technique can be successfully used for improvement of dissolution rate of MA.

Kishore Kumar S.,Dcrm Pharmacy College | Nagabhushanam M.V.,Dcrm Pharmacy College | Sambasiva Rao K.R.S.,Acharya Nagarjuna University
International Journal of Pharma and Bio Sciences | Year: 2013

The present study aimed at preparing fast dissolving oral films of zolmitriptan as a model drug which is used for the migraine treatment. Fast dissolving dosage forms have acquired great importance in pharmaceutical industry because of their unique properties. In the present research work various trials were carried out using different grades of HPMC E3, E6, and E15, maltodextrin DE6 and other polymers by solvent casting method. The prepared films were evaluated for film thickness, folding endurance, surface pH, morphological properties, %drug content and content uniformity, tensile strength, percent elongation, in vitro disintegration time and in vitro dissolution studies. The optimized formulation F23 prepared using HPMC E15 showed minimum disintegration time (10 sec), highest dissolution rate i.e. 99% of drug within 8 min and satisfactory physicochemical properties. The optimized film was evaluated for its bioavailability compared with pure drug as reference standard. Statistical analysis revealed that no significant difference between the bioavailability parameters of the film and the reference standard indicated that they exhibited comparable plasma level-time profiles. These findings suggest that the fast dissolving film containing zolmitriptan is considered to be potentially useful for the treatment of migraine where quick onset of action is desirable.

Prakash C.R.,DCRM Pharmacy College | Raja S.,Gandhi Institute of Technology and Management | Saravanan G.,Medicinal Chemistry Research Laboratory
Chinese Chemical Letters | Year: 2012

A new series of isatin semicarbazide derivatives (7a-7j) were synthesized and characterized by spectroscopic means and elemental analysis. Analgesic and anti-inflammatory screening was performed using tail-flick technique and the carrageenan-induced foot paw edema test respectively. The ulcerogenicity was also determined for all the compounds. Some of the compounds showed moderate enhancement of the activity. Among the synthesized derivatives, compound 7d showed higher analgesic, antiinflammatory and one-third of ulcer index of the reference drug. © 2012 Chinnasamy Rajaram Prakash.

Saravanan G.,Jawaharlal Nehru Technological University | Alagarsamy V.,M.R.Research | Prakash C.R.,DCRM Pharmacy College
Bioorganic and Medicinal Chemistry Letters | Year: 2012

Novel quinazolinone derivatives 5a-5n were designed, synthesized and screened for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by rotorod test. Compounds 5c, 5d, 5g, 5j and 5k were found active in the preliminary screening in MES model and/or scPTZ model. Further all these five compounds were administered to rats, 5c and 5d showed better activity than Phenytoin in oral route. Among all the title compounds tested, the most active one was 5c that revealed protection in MES at a dose of 30 mg/kg (ip) after 0.5 and 4 h. This molecule also provided protection in the scPTZ at a dose of 100 mg/kg (0.5 h) and 300 mg/kg (4 h). © 2012 Elsevier Ltd. All rights reserved.

Saravanan G.,Jawaharlal Nehru Technological University | Alagarsamy V.,M.R.Research | Prakash C.R.,DCRM Pharmacy College
Medicinal Chemistry Research | Year: 2013

With the aim of developing potent analgesic, anti-inflammatory, and antimicrobial agents a series of novel quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, 1H-NMR, mass spectroscopy and bases of elemental analysis. Tail-flick technique, carrageenan-induced foot paw edema test, and agar streak dilution test were performed for screening analgesic, anti-inflammatory, and in vitro antimicrobial activity, respectively. Moreover, all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to good analgesic, anti-inflammatory, and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds were discussed. Compound 2-(2-(4-(trifluoromethyl)benzylidene)hydrazinyl)-N-(4-(2-methyl-4-oxoquinazolin- 3(4H)-yl) phenyl) acetamide 5e was determined to be the most active compound. © 2012 Springer Science+Business Media, LLC.

Saravanan G.,Jawaharlal Nehru Technological University | Alagarsamy V.,M.R.Research | Prakash C.R.,DCRM Pharmacy College
Journal of Saudi Chemical Society | Year: 2015

A series of 1-(substitutedbenzylidene)-4-(4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl) phenyl)semicarbazide derivatives were synthesized with the aim of developing potential antimicrobials. It was characterized by FT-IR, 1H NMR, Mass spectroscopy and elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique and agar streak dilution method. All title compounds showed activity against the entire strain of microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds were well discussed. Based on the results obtained, compound 5j was found to be very active compared to the rest of the compounds which were subjected to antimicrobial assay. © 2011.

Prakash C.R.,DCRM Pharmacy College | Panneerselvam T.,DCRM Pharmacy College | Raja S.,Bharat Institute of Technology
Toxicological and Environmental Chemistry | Year: 2010

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, 13C-NMR, mass spectroscopy, and elemental analysis. These compounds were screened for antioxidant activity by DPPH, nitric oxide and hydrogen peroxide radical scavenging activity. In all the methods, the compound 3-(4-(3,4,5-trimethoxy benzylideneamino) phenylimino) indoline-2-one (5d) showed highest antioxidant activity because of the presence of electron donating groups and the compound 3-(4-(4-nitrobenzylideneamino)phenylimino) indoline-2-one (5f) showed the least activity because of the presence of an electron withdrawing group. © 2010 Taylor & Francis.

Yamini K.,DCRM Pharmacy College | Onesimus T.,DCRM Pharmacy College
International Journal of Pharma and Bio Sciences | Year: 2013

Herbal formulations have growing demand in the world market. The present work deals with the development and evaluation of the herbal Anti-Acne gel containing hydroalcoholic extract of Neem leaves (Azadirachta indica) and the fruits of Nutmeg (Myristica fragrance). The plants have been reported in the literature having good antimicrobial, anti-oxidant and anti-inflammatory activity. Various formulation batches i.e., F1 to F15 were prepared and evaluated for various parameters like colour, appearance, consistency, washability, pH, spreadability and antimicrobial activity.. Optimized formulation was compared with the marketed preparation. Amongst all the formulation studied batch F4 was found optimum for all the parameters. It is a very good attempt to establish the herbal gel containing hydro-alcoholic extract of neem leaves (Azadirachta indica) and fruits of nutmeg (Myristica fragrance).

Nagabhushanam M.V.,Dcrm Pharmacy College
Rasayan Journal of Chemistry | Year: 2010

β-Cyclodextrin (β-CD) and HP-β-Cyclodextrin (HP-β-CD) inclusion complexes of piroxicam (PRX) exhibited higher dissolution rates and dissolution efficiency values than the corresponding un-complexed drug. The feasibility of formulating the β-cyclodextrin and HP-β-cyclodextrin complexes of piroxicam (1:3) into tablet dosage forms is evaluated. Solid inclusion complexes of piroxicam prepared by kneading method were formulated into tablets by wet granulation and direct compression methods. All the tablets formulated employing β-cyclodextrin and HP-β-cyclodextrin complexes of piroxicam gave rapid and higher dissolution rates of when compared to that of piroxicam plain tablets. All the prepared tablets fulfilled the official (I.P.) disintegration time specification of uncoated tablets. Overall, tablets prepared by direct compression method disintegrate rapidly when compared to those prepared by wet granulation method. Analysis of dissolution data as per zero-order and first - order kinetic models indicated that the dissolution of piroxicam from all the tablets followed first-order kinetics. In both direct compression and wet granulation methods, tablets formulated employing cyclodextrin complexes (PRXT2, PRXT3, PRXT5, PRXT6) gave higher rates of dissolution (K1) and dissolution efficiency (DE30) values when compared to the corresponding tablets formulated with piroxicam as such (PRXT1, PRXT4). Among all the piroxicam tablets formulated, formulation PRXT2, which is based on PRX- βCD (1:3) kneaded complex, gave highest dissolution. A 17.0 fold increase in the dissolution rate of piroxicam was observed with PRXT2 when compared to its plain tablets (PRXT1).

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