Amol S Shah's research while affiliated with KLE College of Pharmacy and other places

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Publications (4)


ChemInform Abstract: Novel Imidazo[2,1-b][1,3,4]thiadiazole Carrying Rhodanine-3-acetic Acid as Potential Antitubercular Agents.
  • Article

March 2012

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72 Reads

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121 Citations

Bioorganic & Medicinal Chemistry Letters

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Kallanagouda R Alagawadi

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Pranali V Sonkusare

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Amol S Shah

The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacteriumtuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial activity. As part of our research program and with a aim of identifying new antitubercular drug candidates, a new class of 2-(trifluoromethyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazole derivatives has been synthesized by both conventional as well as microwave assisted method and evaluated for their in vitro antitubercular activity against M. tuberculosis H(37)Rv. Moreover, various drug-likeness properties of new compounds were predicted. Seven compounds from the series exhibited good activity with MIC in range 3.12-1.56μg/ml. The present study suggests that compounds 6b, 6c, 6d, 6e and 6f may serve as promising lead scaffolds for further generation of new anti-TB agents.

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Antiarthritic activity of various extracts of Mesua ferrea Linn. seed

December 2011

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129 Reads

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86 Citations

Journal of Ethnopharmacology

Mesua ferrea Linn. (Cluciaseae), Cobra's saffron, is named after the heaviness of its timber and is cultivated in tropical climates for its form, foliage, and fragrant flowers. It is prescribed in the Ayurvedic literature for the treatment of pain, inflammation, and rheumatic conditions. In present investigation, activity of Mesua ferrea and its evaluation in the formaldehyde and Complete Freund's Adjuvant (CFA)-induced arthritis in rats is reported. The extracts obtained from successive extraction were subjected to preliminary phytochemical investigation and antiarthritic activity was evaluated by inducing formaldehyde and CFA. Body weight changes and haematological parameters were measured. The results indicate that Mesua ferrea protects rats against formaldehyde and CFA induced arthritis. The body weight changes and haematological perturbations induced by CFA were maintained. The overall results indicated that Mesua ferrea exerts a potent protective effect against formaldehyde and adjuvant-induced arthritis in rats. These findings demonstrate that the present study validates the ethnomedicinal use of seeds of Mesua ferrea in the treatment of arthritis conditions.


Anti-inflammatory, analgesic and antipyretic properties of Thespesia populnea Soland ex. Correa seed extracts and its fractions in animal models

August 2011

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128 Reads

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66 Citations

Journal of Ethnopharmacology

Thespesia populnea Sol. ex Correa (Malvaceae) is commonly known as "Indian tulip tree". The plant has been used as an astringent, antibacterial, anti-inflammatory, antinociceptive and hepatoprotective in Indian system of traditional medicine. Thespesia populnea seeds were successively extracted by soxhlet extraction using petroleum ether (40-60 °C) (TPO) and ethanol (TPE). Unsaponifiable matter (TPOUM) and fatty acids were separated from seed oil. A GC-MS analysis of fatty acid methyl esters was carried out. Ethanolic extract was fractionated using CHCl(3), EtOAc, n-BuOH and H(2)O. Acute arthritis was induced by sub-plantar injection of carrageenan into the left hind paw of rats. The paw volume was measured using plethysmometer. Analgesic activity was assessed by heat induced pains (tail immersion model) and antipyretic activity assessed using brewers yeast-induced pyrexia model. Oral administration of TPO and TPE at 200 and 400 mg/kg b.w. and tested fractions at 200mg/kg significantly reduced carrageenan induced paw edema and brewers yeast-induced pyrexia. In tail immersion method also extracts and fractions showed significant analgesic activity. Amongst all fractions EtOAc showed most significant results. TPOUM showed significant anti-inflammatory and analgesic activity. GC-MS analyses showed the presence of fourteen fatty acids, predominant fatty acids were palmitic and stearic acid. These results highlighted anti-inflammatory, analgesic and antipyretic effects of Thespesia populnea seeds.

Citations (4)


... Thiadiazoles are vemembered heterocyclic compounds which are extensively applied in medicinal, agricultural, industrial, and polymer chemistry. In particular, 1,3,4-thiadiazole compounds are important owing to their characteristicsantiviral, 54 antitubercular, 55 anti-depressant, 56 anti-microbial, 57 and anticancer. 58 1,3,4-Thiadiazole derivatives have been used in the synthesis of different drugs like acetazolamide, 59 furidiazine, megazol, 60 etc. ...

Reference:

Green synthesis of thioamide derivatives in an environmentally benign deep eutectic solvent (DES)
Novel imidazo[2,1-b][1,3,4]thiadiazole carring rhodanine-3-acetic acid as potential antitubercular agents
  • Citing Article
  • January 2012

Bioorganic & Medicinal Chemistry Letters

... Thiazolidine,2-4-dione rings are found in various derivatives like pioglitazone, rosiglitazone, troglitazone, and pioglitazone, among other diabetic medications, are mostly administered to patients to regulate their blood sugar levels [4,5]. The synthesized compounds possess various types of biological activities like antimicrobial [6,7], anticancer [8,9], antiviral [10,11], anti-tubercular [12,13], anti-HIV *Address correspondence to this author at the Department of Pharmacy, Harlal Institute of Management and Technology (HIMT), Plot no-8, knowledge park-1, Greater Noida, Uttar Pradesh -201310, India; Tel: (+91)9999535644; E-mail: pushkarkumarray34@gmail.com [14,15], molluscicidal [16,17], and cerebroprotective [18,19]. It uniquely targets insulin registrant, a major physiologic dysfunction in type-2 diabetic patients, and hence significantly enhances glucose levels [20,21]. ...

ChemInform Abstract: Novel Imidazo[2,1-b][1,3,4]thiadiazole Carrying Rhodanine-3-acetic Acid as Potential Antitubercular Agents.
  • Citing Article
  • March 2012

Bioorganic & Medicinal Chemistry Letters

... Denaturation of these proteins leads to the development of inflammation [26]. Several agents, including substance like formaldehyde can destroy articular cartilage [26,27]. The arthritic effect produced by formaldehyde injection occurs in two different stages. ...

Antiarthritic activity of various extracts of Mesua ferrea Linn. seed
  • Citing Article
  • December 2011

Journal of Ethnopharmacology

... Non-steroidal anti-inflammatory drugs are used to relieve pain, fever, and inflammation while also protecting the cardiovascular system. However, the side effects of currently available anti-inflammatory medications, which include gastric ulcer, renal damage, bronchospasm, and cardiac problems, have limited their usage [37][38][39]. Due to the adverse effects of non-steroidal anti-inflammatory drugs and opioids, there is a high demand for the search for new drugs with fewer or no side effects [17a]. ...

Anti-inflammatory, analgesic and antipyretic properties of Thespesia populnea Soland ex. Correa seed extracts and its fractions in animal models
  • Citing Article
  • August 2011

Journal of Ethnopharmacology