title: Identification of 1-[4-Benzyloxyphenyl)-but-3-enyl]-1H-azoles as New Class of Antitubercular and Antimicrobial Agents.
abstract: A series of 1-[(4-benzyloxyphenyl)-but-3-enyl]-1H-azoles has been identified as potent antitubercular agents against Mycobacterium tuberculosis. Synthesis of compounds involved acid catalyzed ring-opening of cyclopropyl ring of phenyl cyclopropyl methanols followed by nucleophilic attack of the azoles on the carbocation intermediates. Several of the compounds 26, 34, and 36 exhibited significant antitubercular activities with MIC value as low as 1.56, 1.56, and 0.61 μg/mL, respectively, comparable to many standard drugs. These compounds were also screened against other strains of bacteria and fungi, and few of them showed good antifungal activity against A. fumigatus, responsible for lung infection.
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Namrata
authors.initials: N
authors.lastname: Anand
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: K K G
authors.initials: KK
authors.lastname: Ramakrishna
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Munna P
authors.initials: MP
authors.lastname: Gupt
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Vinita
authors.initials: V
authors.lastname: Chaturvedi
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Shubhra
authors.initials: S
authors.lastname: Singh
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Kishore K
authors.initials: KK
authors.lastname: Srivastava
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Prapunjika
authors.initials: P
authors.lastname: Sharma
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Niyati
authors.initials: N
authors.lastname: Rai
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Ravishankar
authors.initials: R
authors.lastname: Ramachandran
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: A K
authors.initials: AK
authors.lastname: Dwivedi
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Varsha
authors.initials: V
authors.lastname: Gupta
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Brijesh
authors.initials: B
authors.lastname: Kumar
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Smriti
authors.initials: S
authors.lastname: Pandey
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Praveen K
authors.initials: PK
authors.lastname: Shukla
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Shailandra K
authors.initials: SK
authors.lastname: Pandey
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Jawahar
authors.initials: J
authors.lastname: Lal
authors.affiliation: Academy of Scientific and Innovative and Research, Division of Medicinal & Process Chemistry, Drug Target Discovery and Development, Microbiology, Molecular and Structural Biology, Pharmaceutics, Sophisticated Analytical Instrumentation Facility, Fermentation Technology, Pharmacokinetics & Metabolism, Central Drug Research Institute , CSIR, Chattar Manzil, Mahatma Gandhi Marg, Lucknow 226001, India.
authors.forename: Rama Pati
authors.initials: RP
authors.lastname: Tripathi
keywords: Antitubercular agents; Mycobacterium tuberculosis; azoles; cyclopropyl methanols