Novel imidazo[2,1-b][1,3,4]thiadiazole carrying rhodanine-3-acetic acid as potential antitubercular agents.

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.

Antiarthritic activity of various extracts of Mesua ferrea Linn. seed.

ETHNOPHARMACOLOGICAL RELEVANCE: 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. OBJECTIVE: 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. MATERIALS AND METHODS: 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. RESULTS: 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. CONCLUSION: 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.

ETHNOPHARMACOLOGICAL RELEVANCE: 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. MATERIALS AND METHODS: 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. RESULTS: 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. CONCLUSION: These results highlighted anti-inflammatory, analgesic and antipyretic effects of Thespesia populnea seeds.