Justice Ks Hegde Medical Academy

Deralakatte, India

Justice Ks Hegde Medical Academy

Deralakatte, India

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Karuvalam R.P.,Kannur University | Haridas K.R.,Kannur University | Nayak S.K.,Indian Institute of Science | Guru Row T.N.,Indian Institute of Science | And 3 more authors.
European Journal of Medicinal Chemistry | Year: 2012

A series of (2-aminothiazol-4-yl)methylester (5a-t) derivatives were synthesized in good yields and characterized by 1H NMR, 13C NMR, mass spectral and elemental analyses. The crystal structure of 5a was evidenced by X-ray diffraction study. The compounds were evaluated for their preliminary in vitro antibacterial, antifungal activity and were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain. The synthesized compounds displayed interesting antimicrobial activity. © 2012 Elsevier Masson SAS. All rights reserved.


Karuvalam R.P.,Kannur University | Haridas K.R.,Kannur University | Shetty S.N.,Justice Ks Hegde Medical Academy
Journal of the Chilean Chemical Society | Year: 2012

A convenient method using TMSCl (20 mol%) and microwave-induced technique for the synthesis of various benzimidazole is described. This has reduced the reaction time drastically as well as improved the yield when compared to conventional heating. The synthesized compounds were evaluated for their in vitro antibacterial and antifungal activities against four strains each. Preliminary results indicated that, compounds 3e, 3f, 3g, 3k, 3m, 3n and 3o demonstrated very good antimicrobial activity, comparable to the first line standard drugs. The most effective compounds have exhibited activity at MIC of 6.25 μg/mL. © 2012 Sociedad Chilena de Química.


Karuvalam R.P.,Kannur University | Pakkath R.,Kannur University | Haridas K.R.,Kannur University | Rishikesan R.,and Research Center | Kumari N.S.,Justice Ks Hegde Medical Academy
Medicinal Chemistry Research | Year: 2013

In this article, we report herein the SAR studies of a series of (1H-indol-3-yl)alkyl-3-(1H-indol-3-yl)propanamide 10(a-j), 11(a-j). The synthesized compounds were evaluated for their preliminary in vitro antibacterial, antifungal activity and were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain. The synthesized compounds displayed interesting antimicrobial activity. © 2013 Springer Science+Business Media New York.


Ranjith P.K.,Kannur University | Rajeesh P.,Kannur University | Haridas K.R.,Kannur University | Susanta N.K.,Indian Institute of Science | And 3 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

In this Letter, we report the structure-activity relationship (SAR) studies on series of positional isomers of 5(6)-bromo-1-[(phenyl)sulfonyl]-2-[(4- nitrophenoxy)methyl]-1H-benzimidazoles derivatives 7(a-j) and 8(a-j) synthesized in good yields and characterized by 1H NMR, 13C NMR and mass spectral analyses. The crystal structure of 7a was evidenced by X-ray diffraction study. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, (Gram-positive), Escherichia coli and Klebsiella pneumoniae (Gram-negative), antifungal activity against Candida albicans, Aspergillus flavus and Rhizopus sp. and antitubercular activity against Mycobacterium tuberculosis H37Rv, Mycobacterium smegmatis, Mycobacterium fortuitum and MDR-TB strains. The synthesized compounds displayed interesting antimicrobial activity. The compounds 7b, 7e and 7h displayed significant activity against Mycobacterium tuberculosis H37Rv strain. © 2013 Elsevier Ltd. All rights reserved.


Ranjith P.K.,Kannur University | Pakkath R.,Kannur University | Haridas K.R.,Kannur University | Kumari S.N.,Justice Ks Hegde Medical Academy
European Journal of Medicinal Chemistry | Year: 2014

In this paper we report the SAR studies of a series of N-(4-(4-chloro-1H- imidazol-1-yl)-3-methoxyphenyl)amide and N-(4-(4-chloro-1H-imidazol-1-yl)-3- methoxyphenyl)sulfonamide derivatives 6(a-o) and 7(a-o), were synthesized in good yields and characterized by 1H NMR, 13C NMR and mass spectral analyses. The preparation of the key intermediate highlights an optimized palladium catalyzed (Pd2(dba)3/RuPhos) Buchwald cross-coupling of intermediate 2 and 3. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, (Gram-positive), Escherichia coli and Klebsiella pneumoniae (Gram-negative), antifungal activity against Candida albicans, Aspergillus flavus and Rhizopus sp. and antitubercular activity against Mycobacterium tuberculosis H37Rv, Mycobacterium smegmatis, Mycobacterium fortuitum and MDR-TB strains. The synthesized compounds displayed interesting antimicrobial activity. The compounds 7d, 7f, 7h and 7n displayed significant activity against Mycobacterium tuberculosis H37Rv strain. © 2013 Elsevier Masson SAS. All rights reserved.


PubMed | Justice Ks Hegde Medical Academy and Kannur University
Type: | Journal: European journal of medicinal chemistry | Year: 2014

In this paper we report the SAR studies of a series of N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide and N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)sulfonamide derivatives 6(a-o) and 7(a-o), were synthesized in good yields and characterized by (1)H NMR, (13)C NMR and mass spectral analyses. The preparation of the key intermediate highlights an optimized palladium catalyzed (Pd(dba)/RuPhos) Buchwald cross-coupling of intermediate 2 and 3. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, (Gram-positive), Escherichia coli and Klebsiella pneumoniae (Gram-negative), antifungal activity against Candida albicans, Aspergillus flavus and Rhizopus sp. and antitubercular activity against Mycobacterium tuberculosis H37Rv, Mycobacterium smegmatis, Mycobacterium fortuitum and MDR-TB strains. The synthesized compounds displayed interesting antimicrobial activity. The compounds 7d, 7f, 7h and 7n displayed significant activity against Mycobacterium tuberculosis H37Rv strain.


Thomas K.D.,Anthem Biosciences Pvt. Ltd | Thomas K.D.,National Institute of Technology Karnataka | Adhikari A.V.,National Institute of Technology Karnataka | Shetty N.S.,Justice Ks Hegde Medical Academy
European Journal of Medicinal Chemistry | Year: 2010

A new series of [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2,3-triazol-4-yl] methanamine derivatives were synthesized starting from 4-methoxyaniline through multi-step reactions. The title compounds 5a-y were prepared by treating the azide intermediate 4 with propargyl bromide and different alkyl/heterocyclic amines in a sequential three component synthesis. All the new compounds were characterized by spectral and elemental analyses. The newly synthesized final compounds were evaluated for their in vitro antibacterial and antifungal activities against pathogenic strains. The preliminary screening results indicated that most of the compounds demonstrated moderate to very good antibacterial and antifungal activities, comparable to the first-line drugs. Twenty five new derivatives of [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2,3- triazol-4-yl] methanamine have been synthesized and the most effective compounds have MIC of 6.25 μg/mL, which are in comparable with present antibiotics. © 2010 Elsevier Masson SAS. All rights reserved.


Paniraj A.S.,University of Mysore | Paniraj A.S.,Advinus Therapeutics Ltd | Rai K.M.L.,University of Mysore | Bhat P.V.,Advinus Therapeutics Ltd | And 4 more authors.
Der Pharma Chemica | Year: 2011

New 5-halo-4, 6-dimethoxy-2-(alkoxy or aryloxy) pyrimidines (4a-r) were prepared from 5-halo-4,6-dialkoxy,2-methylsulfonylpyrimidine. The structure of newly synthesized compounds was characterized by their spectral date. The newly synthesized compounds were evaluated for their anmicrobial and antifungal studies. Some of the compounds showed moderate to good activity.

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