The present article describes a facile one-pot synthesis of a series of eight pyrazolo[3,4-d]pyrimidines 4a-h which were evaluated for their in-vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using the Alamar-Blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in mg/mL. The compounds 4b, 4c, 4d, and 4g exhibited the best results (1.2 microg/mL) when compared with first-line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore, this class of compounds could be a good starting point to develop new lead compounds in the treatment of multidrug-resistant tuberculosis.

In the present investigation ethyl 2-(4-carboxyphenylazo)acetoacetate 1 on condensation with various aromatic aldehydes in ethanolic NaOH solution yielded the corresponding chalcones 2a-j. These chalcones were further reacted with urea in the presence of base in ethanol, which led to the formation of pyrimidine derivatives 3a-j. The newly synthesized heterocyles were characterized on the basis of their chemical properties and spectroscopic data. All newly synthesized compounds were evaluated for their antimycobacterial activities against Mycobacterium tuberculosis H 37 Rv.

Fused pyrimidine derivatives R 0515 Facile One-Pot Synthesis and Antimycobacterial Evaluation of Pyrazolo[3,4-d]pyrimidines. -All title compounds (IV) (8 examples) display significant antimycobacterial activity. Derivatives (IVb)-(IVe) exhibit the best results when compared with first-line drugs such as isoniazid and rifampicin. -(TRIVEDI, A.; DODIYA, D.; SURANI, J.; JARSANIA, S.; MATHUKIYA, H.; RAVAT, N.; SHAH*, V.; Arch. Pharm. (Weinheim, Ger.) 341 (2008) 7, 435-439; Dep. Chem., Saurashtra Univ., Rajkot 360 005, India; Eng.) -A. Forchert 44-167

dithiocarbamoyl]-6-arylamino-s-triazines. -Triazinyl dithiocarbamate derivatives of type (V) and (VII) are prepared and screened for their antibacterial and antifungal activities. All of them show significant antimicrobial activities. -(DESAI, R. M.; RAVAT, N. R.; SHAH*, V. H.; Indian J.