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Design, Synthesis and Characterisation of Novel Carbazole Linked Propeonones


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1 Department of Pharmaceutical Chemistry, Azad College of Pharmacy, Moinabad-Chilkur Road, Hyderabad-500075, India
     

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Natural products derived from plants or microbes play a major role in drug discovery as a source of original bioactive structures and offer models for rational drug design. The promising natural anti-mycobacterials include carbazole alkaloids, such as Clausine and Micromeline isolated independently from several sources and were shown to have potent antitubercular activity. In recent years, carbazole alkaloids are playing important role in discovering new antitubercular leads against non-resistant and multi-drug resistant strains of M. tuberculosis. Few among them are 7-hydroxymukonal (IX, MIC 25lg/mL), Clausine K (MIC: 100lg/mL), and Micromeline (MIC: 31.5lg/mL). Knölker screened a series of carbazole alkaloids for their in vitro anti-TB activity. It appeared that anti-TB activity is highly sensitive to subtle changes in substitution around the carbazole ring system. Herein we report the synthesis of Nine Novel Carbazole linked propeonones in excellent yields via N-Methylation of Carbazole followed by Friedel's crafts acylation of N-methyl carbazole. All the compounds were characterised by Spectroscopic methods.

Keywords

Carbazole Alkaloids, Anti-TB Activity, Carbazole Linked Propeonones and N-Methylation.
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  • Design, Synthesis and Characterisation of Novel Carbazole Linked Propeonones

Abstract Views: 59  |  PDF Views: 5

Authors

Kouser Unnisa
Department of Pharmaceutical Chemistry, Azad College of Pharmacy, Moinabad-Chilkur Road, Hyderabad-500075, India
Tahseen Sameena
Department of Pharmaceutical Chemistry, Azad College of Pharmacy, Moinabad-Chilkur Road, Hyderabad-500075, India
Habeeba Sulthana
Department of Pharmaceutical Chemistry, Azad College of Pharmacy, Moinabad-Chilkur Road, Hyderabad-500075, India
Hafsa Siddiqua
Department of Pharmaceutical Chemistry, Azad College of Pharmacy, Moinabad-Chilkur Road, Hyderabad-500075, India
Maimunna Khatoon
Department of Pharmaceutical Chemistry, Azad College of Pharmacy, Moinabad-Chilkur Road, Hyderabad-500075, India

Abstract


Natural products derived from plants or microbes play a major role in drug discovery as a source of original bioactive structures and offer models for rational drug design. The promising natural anti-mycobacterials include carbazole alkaloids, such as Clausine and Micromeline isolated independently from several sources and were shown to have potent antitubercular activity. In recent years, carbazole alkaloids are playing important role in discovering new antitubercular leads against non-resistant and multi-drug resistant strains of M. tuberculosis. Few among them are 7-hydroxymukonal (IX, MIC 25lg/mL), Clausine K (MIC: 100lg/mL), and Micromeline (MIC: 31.5lg/mL). Knölker screened a series of carbazole alkaloids for their in vitro anti-TB activity. It appeared that anti-TB activity is highly sensitive to subtle changes in substitution around the carbazole ring system. Herein we report the synthesis of Nine Novel Carbazole linked propeonones in excellent yields via N-Methylation of Carbazole followed by Friedel's crafts acylation of N-methyl carbazole. All the compounds were characterised by Spectroscopic methods.

Keywords


Carbazole Alkaloids, Anti-TB Activity, Carbazole Linked Propeonones and N-Methylation.