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Patel K.,GLA Institute of Pharmaceutical Research | Gadewar M.,S.K.I.P.S | Patel D.K.,Banaras Hindu University
Chinese Journal of Integrative Medicine | Year: 2013

Plants have been used as a source for food material and natural remedies for the treatment of vast range of diseases. Nature provides us remedies for the treatment of various types of disorders ranging from simple ailments to complicated diseases. Plants are known to possess different pharmacological activities due to the presence of various phytoconstituents. Flavonoids are one of the main active phytoconstituents found in fruits, vegetables, wines, tea and cocoa. Flavonoids exhibit various pharmacological activities such as antioxidant, anti-inflammatory, anti-allergic, antibacterial, oestrogenic, cytotoxic antitumoural, hepatoprotective, antithrombotic and antiviral activity. Diosmetin (3′, 5, 7-trihydroxy-4′-methoxyflavone), the aglycone part of the flavonoid glycosides diosmin occurs naturally in citrus fruit. Although it is found in herbal medicines and plays an important role in the treatment of various ailments, only limited scientific researches have been conducted. The aim of this review is to collect all available scientific literature published on diosmetin and combine it into this paper. This review contains an overview of pharmacological activities, isolation techniques and analytical techniques for diosmetin. Thus, valuable information provided in the present review will help researchers in developing alternative methods for the treatment of diseases from diosmetin. © 2013 Chinese Association of the Integration of Traditional and Western Medicine and Springer-Verlag Berlin Heidelberg.


Rajak H.,Guru Ghasidas University | Veerasamy R.,AIMST University | Kharya M.,Dr Hari Singh Gour University | Mishra P.,GLA Institute of Pharmaceutical Research
Journal of Enzyme Inhibition and Medicinal Chemistry | Year: 2010

Two novel series of oxadiazole and oxadiazoline analogs possessing an indole nucleus were synthesized for their potential anti-inflammatory activity. The structures of the compounds were elucidated by elemental and spectral (IR, 1H-NMR, 13C-NMR, and MS) analysis. Most of the test compounds demonstrated appreciable anti-inflammatory activities. The anti-inflammatory activity of oxadiazoles at doses of 100mg/kg was shown by their ability to provide 2766%, 1432%, and 20-51%. protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. On the other hand, the anti-inflammatory properties of oxadiazolines at doses of 100mg/kg were reflected by their ability to provide 20-56%, 1126%, and 2547% protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. The ulcerogenic potential of the compounds was determined. Structureactivity relationships among synthesized compounds were also established. © 2010 Informa UK Ltd.


Upmanyu N.,Dr Hari Singh Gour University | Gupta J.,GLA Institute of Pharmaceutical Research | Shah K.,GLA Institute of Pharmaceutical Research | Mishra P.,GLA Institute of Pharmaceutical Research
Journal of Pharmacy and Bioallied Sciences | Year: 2011

Introduction: 1,2,4-triazoles and its derivatives have been reported to possess anti-inflammatory, analgesic, antimicrobial, anticancer, antitumor, antitubercular, anticonvulsant, openers of Ca-activated potassium (Maxi-K) channels, antiviral properties, hypoglycemic, anxiolytic and antidepressant activity. Therefore, 1,2,4-triazole seems to be an important pharmacophore. Materials and Methods: The synthesis of 4-(substituted ethanoyl) amino-3-mercapto-5-(4-methoxy) phenyl-1,2,4-triazoles (6a-o) were prepared following six step starting 4-methoxy benzoic acid and using different secondary amines and were characterized with the help of FT-IR, 1 H, 13 C NMR, FAB Mass and nitrogen analysis. These synthesized compounds (6a-o) were then evaluated for anti-inflammatory activity by carrageenan induced paw edema method.Out of these synthesized compounds, some (6f, i and k) were evaluated for antinociceptive activity by Hot plate method and Tail immersion method. Results and Discussion: The synthesis of 4-(substituted amino)-3-mercapto-5-(4-methoxy) phenyl-1,2,4-triazoles (6a-o) was accomplished. The IR spectra exhibited characteristic bands for C-N, C=N, SH and C=O at 1350-1360, 1511-1548, 2520-2594.3 and 1650-1719 cm -1. The C-O-C asymmetric and symmetric str. was at 1250-1254 and 1027-1079.3 cm -1 respectively. In 1 H-NMR spectra, a singlet of CONH was found in the range of δ 9.92-10.18 ppm and another singlet of thiol group was observed in the range of δ 8.63-9.92 ppm. A singlet of Ar-OCH 3 was also found between δ 3.57-3.91 ppm. In 13 C- NMR spectra, C-3 and C-5 of the 1,2,4 - triazole nucleus were observed in the range of δ 147-166.9 ppm. Carbonyl carbon and methylene carbon of -NHCOCH 2 N< were found between δ 166.5-177.5 and δ 47.1-62 ppm respectively. Acute toxicity study was donr following OECD-423 and cut-off dose was found to be between 1000-1500 mg/kg body weight. At the dose level of 100 mg/kg, 6f, 6i and 6k exhibited appreciable inhibition of oedema especially 6k exhibiting a percentage of oedema inhibition of 40.28%, which was comparable to that of the standard drug indomethacin (62.50% at 10mg/kg dose). Among the compounds tested, compound 6k exhibited good anti-nociceptive activity in both methods used. Pethidine (20mg/kg body weight s.c) is used as the standard drug. Conclusion: SAR of these synthesized compounds shows that substitution with heterocyclic moiety at C-2 of the acetamido group at position 4 of the 1,2,4-triazole produces appreciable activity as compared to substitution with aliphatic moieties since among all the synthesized compounds, the most active ones are 6f, 6i and 6k that have piperdine, 1-benzyl piperazine and morpholine group, respectively at C-2 of the acetamido group at position 4 of the 1,2,4-triazole.


Upmanyu N.,Dr Hari Singh Gour University | Kumar S.,Defence Research Development and Establishment | Shah K.,GLA Institute of Pharmaceutical Research | Mishra P.,GLA Institute of Pharmaceutical Research
Dhaka University Journal of Pharmaceutical Sciences | Year: 2012

Triazoles and triazoles with different substituent groups are found to possess diverse application in the field of medicine and industry. A series of 4-(substituted) ethanoylamino-3-mercapto-5-(4-substituted) phenyl-1,2,4- triazoles were synthesized as novel antimicrobial agents starting from different 4-substituted benzoic acids. The chemical structures of these newly synthesized compounds were elucidated by 1R, 1H NMR, 13C NMR, FAB+-mass spectral data and elemental analyses. The antimicrobial activity of title compounds were examined against two gram positive bacteria (Staphylococcus aureus, Bacillus subtilis), two gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and three fungi (Candida albicans, Aspergillus niger and Fusarium oxysporum) using disc diffusion method. Some of the compounds bearing methoxy group exhibited moderate to good antibacterial and antifungal activities.


Upmanyu N.,Dr Hari Singh Gour University | Kumar S.,Defence Research Development and Establishment | Shah K.,GLA Institute of Pharmaceutical Research | Mishra P.,GLA Institute of Pharmaceutical Research
Medicinal Chemistry Research | Year: 2012

Triazoles and its derivatives are found to possess diverse applications in the field of medicine and industry. A series of novel 1,2,4-triazole derivatives have been synthesized as novel antimicrobial agents starting from different 4-substituted benzoic acids. The chemical structures of these newly synthesized compounds were elucidated by Fourier transform infrared spectroscopy (FTIR), 1H NMR, 13C NMR, FAB?-MS spectral data, and elemental analysis. Their antimicrobial activities were investigated against four bacterial strains S. aureus (ATCC-25923), P. aeruginosa (ATCC-27853), E. coli (ATCC-8739), B. subtilis (ATCC-6633) and three fungal strains C. albicans (MTCC-227), A. niger (MTCC-3323), and F. oxysporum (MTCC-2087). Preliminary results indicate that some of them exhibit promising activities and deserve further consideration. © Springer Science+Business Media, LLC 2011.

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