Anti-tubercular agents

Prathipati P, Ma NL, Keller TH (2008) Global Bayesian models for the prioritization of anti-tubercular agents. J Chem Inf Model 48 2362-2370... 

Shaguffa, Kumar A, Panda G, Siddiqi MI (2007) CoMFA and CoMSIA 3D-QSAR analysis of diaryloxy-methano-phenanthrene derivatives as anti-tubercular agents. J Mol Model 13 99-109... 

Hevener KE, Ball DM, Buolamwini JK, Lee RE (2008) Quantitative structure-activity relationship studies on nitrofuranyl anti-tubercular agents. Bioorg Med Chem 16 8042-8053... 

Ahn HC, Yang JH, Lee HB, Rhee YK, Lee YC. Effect of combined therapy of oral anti-tubercular agents on theophylline pharmacokinetics. Int J Tuberc Lung Dis 2000 4(8) 784-7. 

A typical hydrazine derivative in the pharmaceuticals sector is the anti-tubercular agent Neoteben ... 

Pneumococci resistant to penicillins, certain cephalosporins, and macrolides are increasingly common. These organisms generally are susceptible to vancomycin, the new fluoroquinolones, and cefotaxime or ceftriaxone. M. tuberculosis resistant to one or more first-hue anti-tubercular agents (e.g., isoniazid, rifampin, ethambutol, streptomycin, and pyrazinamide) have increased in frequency as well. This has been... 

Main directions of search of new anti-tubercular agents including derivatives of heterocycles 00KFZ(1)12. 

Oxazoles are known in natural products and also find wide incorporation into synthetic medicinal compounds. Oxazoles can be found in the natural products (-)-hennoxazole A (antiviral) and leucascandrolide A (cytotoxic and antifungal). Benzoxazoles and isoxazoles are less common in natural products. Pseudo-pteroxazole (benzoxazole-containing anti-tubercular agent) and ibotenic acid (isoxazole-containing neurotoxin) are two examples. 

Our motivation for investigating thioamide derivatives, which potentially can form N-H... S interactions, arises from the presence of the -N(H)-C(=S)- residue, and derivatives thereof, in several dmgs [20], see Scheme 6.2 for chemical structures of these species. Thus, the antithyroid drugs 6-n-propyl-thiouracil (I) and l-methyl-3//-imidazole-2-thione (II, Methimazole , also marketed as Tapazole ) feature the -N(H)-C(=S)- functional group [21]. Hyperthyroidism may be treated with 3-methyl-2-thioxo-4-imidazoline-l-carboxylate (III, Carbimazole ) which is metabolised in vivo to the active form, known as Methimazole [22]. Anti-tubercular agents containing the thioamide residue and which inhibit mycolic acid synthesis include 2-ethyl-thioisonicotinamide (IV, Ethionamide ) and its -propyl derivative (Prothionamide ) [23-25]. 

Quinazolinone derivatives have been reported with various biological and medicinal properties, such as inhibitors of the epidermal growth factor (EGF) receptors of tyrosine kinase, and as anticancer, antiviral, and anti-tubercular agents. They are also used as ligands for benzodiazepine and... 

N. Kishore, B.B. Mishra, V. Tripathi, V.K. Tiwari, Alkaloids as potential anti-tubercular agents, Fitoterapia 80 (2009) 149-163. 

Figure 2.21 1,2,3-Triazole linked carbazole analogues as anti tubercular agents.

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