- Synthesis, computational studies, antimycobacterial and antibacterial properties of pyrazinoic acid-isoniazid hybrid conjugates
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Benzotriazole and microwave mediated syntheses led to a new set of hybrid conjugates of pyrazinoic acid with isoniazid via amino acid linkers in excellent yields with retention of chirality. Microbiological screening of the synthesized conjugates revealed an exceptionally high activity against some of the pathogenic bacterial strains at low concentrations. Promising antimycobacterial properties were observed against tuberculous and non-tuberculous mycobacteria. Robust molecular models (2D-QSAR and 3D-pharmacophore) support the observed biological properties. Safety profile of the synthesized conjugates against human normal cell (RPE1) was evaluated by MTT technique.
- Panda, Siva S.,Girgis, Adel S.,Mishra, Bibhuti B.,Elagawany, Mohamed,Devarapalli, Venkatasai,Littlefield, William F.,Samir, Ahmed,Fayad, Walid,Fawzy, Nehmedo G.,Srour, Aladdin M.,Bokhtia, Riham M.
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p. 20450 - 20462
(2019/07/09)
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- Synthesis and structure-activity relationship studies of cytotoxic anhydrovinblastine amide derivatives
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A series of 3-demethoxycarbonyl-3-amide methyl anhydrovinblastine derivatives (5b-24b) was designed, synthesized, and evaluated for their proliferation inhibition activities against two tumor cell lines (A549 and HeLa). Most of the amide anhydrovinblastin
- Shao, Yong,Zhang, Han-Kun,Ding, Hong,Quan, Hai-Tian,Lou, Li-Guang,Hu, Li-Hong
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experimental part
p. 1170 - 1177
(2011/03/20)
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- Preparation of polyfunctional acyl azides
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(Chemical Equation Presented) A general synthesis of acyl azides from the corresponding N-acyl benzotriazoles is described. The procedure affords acyl azides in good yields and avoids the use of acid activators and NO+ equivalents typically emp
- Katritzky, Alan R.,Widyan, Khalid,Kirichenko, Kostyantyn
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p. 5802 - 5804
(2008/02/09)
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- Solid-phase preparation of amides using N-acylbenzotriazoles
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Wang resin linked amines were efficiently converted into amides using acylbenzotriazoles. Cleavage of resins gave the desired amides 7Aa-Gf in 30-99% yields with good to excellent purities.
- Katritzky, Alan R,Rogovoy, Boris V,Kirichenko, Nataliya,Vvedensky, Vladimir
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p. 1809 - 1811
(2007/10/03)
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- N-acylbenzotriazoles: Neutral acylating reagents for the preparation of primary, secondary, and tertiary amides
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Readily available N-acylbenzotriazoles 2a-q efficiently acylate aqueous ammonia and primary and secondary amines to give primary, secondary, and tertiary amides in good to excellent yields. The wide applicability of the procedure is illustrated by the preparation of (i) α-hydroxyamides from α-hydroxy acids and of (ii) perfluoroalkylated amides.
- Katritzky,He,Suzuki
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p. 8210 - 8213
(2007/10/03)
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- Sulfonyl derivatives of benzotriazole: Part 1. A novel approach to the activation of carboxylic acids
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1-Acylbenzotriazoles (8, R = Me, Et, n-Bu and Ph) are prepared in good yields by fusion of benzotriazole and acid chlorides at 80 - 100°C. In cases when the corresponding acid chlorides are not available, 1-acylbenzotriazoles are conveniently available from 1-(1-methanesulfonyl) benzotriazole and the respective carboxylic acids as illustrated by the preparation of 2-, 3-, and 4-pyridoyl-, 2-pyrrolylcarbonyl- and 2-furoyl-benzotriazole in yields of 80 - 95%. Preparations of two sulfonyl derivatives of benzotriazole are also described.
- Katritzky, Alan R.,Shobana,Pernak, Juliusz,Afridi,Fan, Wei-Qiang
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p. 7817 - 7822
(2007/10/02)
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