5(4H)‐Oxazolones as Novel Antitubercular Agents: Synthesis, Characterisation and Structure Activity Study

Abstract

In search of novel anti tubercular agents, a series of twelve 4-(substituted benzylidene)-2-ptolyloxazol-5(4H)-ones (5a-5l) has been synthesized, characterised and subjected to evaluate their antitubercular activity for the first time against Mycobacterium tuberculosis H37Rv (ATCC 27294). The out-put of these studies disclosed that all the synthesized target molecules of the series displayed good to moderate activity with MIC values ranging 2-32 mg/mL in comparison with the standard first line antitubercular drugs Rifampicin and Isoniazid. Compound 5e with three methoxy groups meta to each other, is the most distinctive compound identified amongst the series, because of its remarkable in vitro antitubercular activity and thus may act as a promising lead molecule for further explorations.

Highly Diastereo‐ and Enantioselective Aza‐Mannich Addition of Oxazolones to N‐Boc Protected α‐Amido Sulfones Catalyzed by Bifunctional Thiourea‐modified Cinchona Alkaloid

“…Over the last few years, azlactone core which makes a prominent structure of number of well-established marked drugs such as rilmenidine, furazolidone etc has attracted considerable attention of the medicinal chemistry community for the biological activities such as anticancer, [1] antidiabetic, [2] antimicrobial, [3] analgesic, [4] anti-inflammatory, [5] muscle relaxant, [6] neuroleptic, [7] antitubercular, [8] antiangiogenic, [9] immunomodulator, [10] cardiotonic, [11] cyclooxygenase-2 inhibitor, [12] Acetylcholine esterase inhibitor, [13] and tyrosinase inhibitor, [14] etc. In addition, these azlactone derivatives have been used in order to produce different kinds of polymers and nanomaterials which presented great development in the last decade.…”

Синтез 4-арилиден-2-арил-5(4H)-оксазолонов c применением системы Boc2o/пиридин

“…Представители этого ряда соединений имеют широкий спектр биологической активности. В частности, они обладают антибактериальным [12], противогрибковым [12], антипролиферативным [12], противотуберкулезным [13], антиоксидантным [14] действием, противовоспалительной [15] активностью, также ингибируют моноацилглицеринлипазу [16], тирозиназу [13] и т.д. В связи с этим синтез ААО представляет особый интерес.…”