In an attempt to find a new and a safer drug for tuberculosis, we have synthesized a series of fluoronitrobenzothiazolopyrazolines for antitubercular activity. The series comprises three subclasses: fluorobenzothiazolopyrazolines (11a–f), fluoronitrobenzothiazolopyrazoline, nitro group at 5th position (12a–f) and 4th position (13a–f). All compounds were screened for their in‐vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain by using Middlebrook 7H‐9 broth. An introduction of NO2 group at 5th position of benzothiazole ring (12a–f) increased the antitubercular activity whereas introduction of NO2 group at 4th position (13a–f) was found to decrease the activity remarkably. Two compounds from each series showing good antitubercular activity were tested for cytotoxicity on THP‐1 cell lines and they showed low cytotoxicity.
A series of novel 5,6-unsubstituted thieno-[2,3-d]-pyrimidines has been synthesized and tested for growth inhibition of Mycobacterium tuberculosis H37Rv. Of twelve compounds synthesized eleven have shown antimycobacterial activity that differs in potency. Compounds 7b, 7c, 7d, 7e, 7f, and 7g exhibited good antimycobacterial activity. MIC values of the compounds tested were comparable with pyrazinamide. Six compounds which have shown good antimycobacterial activity were also subjected for cytotoxicity studies and were found to possess poor cytotoxicity. The study indicates the definite need for focusing attention on thienopyrimidines for further lead optimization.
An efficient plant regeneration protocol was developed for Artemisia annua, an aromatic medicinal herb. Nodal explants inoculated on MS supplemented with 4.44 μM BAP showed better growth response and produced 116.2 ± 0.1 microshoots of an average length 1.9 ± 0.3 cm after 35 days culture. The cluster of small shootlets were cultured on shoot elongation medium supplemented with 1.44 μM GA3 and 10% coconut milk (CM) showed shoot elongation up to 4.6 ± 0.7 cm. Roots were induced after transfer to half strength MS supplemented with 2.46 μM IBA produced 14.3 ± 0.2 roots with an average height of 4.3 ± 0.53 cm after 30 days. The rooted plantlets were transferred for hardening, 80 per cent of plantlets survived and resumed growth in the mixture of soil, vermiculite and farm yard manure (1 : 1 : 1).
Thienopyrimidines as Novel Inhibitors of Mycobacterium tuberculosis: Synthesis and in vitro Studies. -The compounds (X) are tested for growth inhibition of Mycobacterium tuberculosis H37Rv. The compounds (Xb)-(Xg) exhibit good antimycobacterial activity. They are also subject for cytotoxicity studies and possess poor cytotoxicity. -(RASHMI*, P.; NARGUND, L. V. G.; HAZRA, K.; CHANDRA, J. N. N. S.; Arch. Pharm. (Weinheim, Ger.) 344 (2011) 7, 459-465, http://dx.
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