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Antimycobacterial potential of novel hydrazone derivatives
Indian Journal of Chemistry, Section B ( IF 0.456 ) Pub Date : 2020-06-22
Sachin H Rohane, Ashlesha J Chauhan

Molecular docking of 1 to 51 compounds has been performed in Small-Molecule Drug Discovery Suite of Schrödinger. Fifty one compounds have been targeted on 2NSD and 2X22 involved in tuberculosis activity. Aryloxy moiety on refluxing with chloroethyl acetate in the presence of potassium carbonate and acetone has yielded ethyl aryloxy acetate (A), which have been reacted with hydrazine hydrate to produce aryloxyacetyl hydrazine (B), which on treatment with aromatic aldehydes or ketones yield hydrazones (C). The novel series of compounds have been elucidated on the basis of spectral studies and screened for antimycobacterial activity. The compounds are significantly sensitive at concentration 50 and 100 μg/mL. Compound 11 shows sensitivity at 25 μg/mL. The antibacterial activity is strongly connected with the position of the substituent on aromatic aldehyde or ketones in relation to the hydrazide skeleton.

中文翻译:

新型衍生物的抗分枝杆菌潜力

1至51种化合物的分子对接已在Schrödinger的小分子药物发现套件中进行。已经有51种化合物针对参与结核病活性的2NSD和2X22。在碳酸钾和丙酮存在下与乙酸氯乙酯回流时产生的芳氧基部分产生乙基芳氧基乙酸酯(A),已与水合肼反应生成芳氧基乙酰基肼(B),经芳族醛或酮处理后生成yield( C)。在光谱研究的基础上阐明了该系列新化合物并筛选了抗分枝杆菌活性。这些化合物在浓度为50和100μg/ mL时非常敏感。化合物11在25μg/ mL下显示出敏感性。
更新日期:2020-07-28
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