Synthesis, characterization and antibiotic evaluation of various biologically active derivatives of 4-Alkylpyrimidine-5-carbonitrile

Q2 Chemistry Current Chemistry Letters Pub Date : 2023-01-01 DOI:10.5267/j.ccl.2023.3.002

P. H. Thanki, Dhaval V. Hingrajiya, J. Modha, Jalpa H. Vadgama

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Abstract

Extensive research work has been published on Tetrahydro and Dihydropyrimidine derivatives. Pyrimidine-5-Carbonitrile and its analogs have demonstrated a large number of activities. Some 6-Halogenosubstituted pyrimidine analogs have also been reported to be biologically active to a certain extent, but the literature survey reveals not much report on 6-alkylated pyrimidine derivatives. Targeting enhancement in biologically useful properties of a lead molecule through the association of it with active pharmacophoric groups or molecules is a conventional method in pharmaceutical research. With an aim to explore a better useful Dihydropyrimidine derivative, a newer 4-Alkylated-1,6-dihydropyrimidine analog (1) has been prepared. The lead molecule (1) has further been converted to amine derivative (2), hydrazino derivative (3) tri substituted s-triazinyl derivative (4), sulphonamide (5), Schiff’s base (6), a thiazolidinones (7), and 2-Azetidinones (8) respectively using various methods. Compounds 2, 4, 5, and 7 showed 50% and 8 showed 100% bacterial inhibition at 32μg/mL in single-point bacterial inhibition against various bacterial strains.

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4-烷基嘧啶-5-碳腈各种生物活性衍生物的合成、表征及抗生素评价

关于四氢嘧啶和二氢嘧啶衍生物的大量研究工作已经发表。嘧啶-5-碳腈及其类似物已显示出大量的活性。一些6-卤代嘧啶类似物也被报道有一定的生物活性，但文献调查显示，6-烷基化嘧啶衍生物的报道不多。通过与活性药理基团或分子的结合，靶向性地增强导联分子的生物学有用特性是药物研究中的一种常规方法。为了寻找更有效的二氢嘧啶衍生物，制备了一种新的4-烷基化-1,6-二氢嘧啶类似物(1)。铅分子(1)又通过各种方法分别转化为胺衍生物(2)、肼衍生物(3)、三取代s-三嗪基衍生物(4)、磺胺(5)、希夫碱(6)、噻唑烷酮(7)和2-叠氮二酮(8)。化合物2、4、5、7在32μg/mL单点抑菌效果为50%，8在32μg/mL单点抑菌效果为100%。

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来源期刊

Current Chemistry Letters Chemistry-Chemistry (all)

CiteScore

4.90

自引率

0.00%

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审稿时长

20 weeks

期刊介绍： The "Current Chemistry Letters" is a peer-reviewed international journal which aims to publish all the current and outstanding research articles, reviews and letters in chemistry including analytical chemistry, green chemistry, inorganic chemistry, organic chemistry, physical chemistry, etc. This journal is dedicated to serve all academic and industrial researchers and scientists who are expert in all major advances in chemistry research. The journal aims to provide the most complete and reliable source of information on current developments in these fields. The emphasis will be on publishing quality articles rapidly and openly available to researchers worldwide. Please note readers are free to read, download, copy, distribute, print, search, or link to the full texts of articles published on this journal. Current Chemistry Letters is an open access journal, which provides instant access to the full text of research papers without any need for a subscription to the journal where the papers are published. Therefore, anyone has the opportunity to copy, use, redistribute, transmit/display the work publicly and to distribute derivative works, in any sort of digital form for any responsible purpose, subject to appropriate attribution of authorship. Authors who publish their articles may also maintain the copyright of their articles.