Microcare Laboratory

Sūrat, India

Microcare Laboratory

Sūrat, India
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Monga V.,Rajendra Institute of Technology and science | Goyal K.,Laureate Institute of Pharmacy | Steindel M.,Federal University of Santa Catarina | Rajani D.P.,Microcare Laboratory | Rajani S.D.,Microcare Laboratory
Medicinal Chemistry Research | Year: 2014

A series of chalcones (1-8) were prepared by Claisen-Schmidt condensation of 3-nitroacetophenone with various aldehydes. These chalcones on cyclization with hydrazine hydrate in the presence of glacial acetic acid, hydrazine hydrate in absolute ethanol and ethyl acetoacetate in the presence of barium hydroxide gave corresponding N-acetyl pyrazolines (9-16 ), N-unsubstituted pyrazolines (17-19) and cyclohexenone derivatives (20-22). All the synthesized compounds were evaluated for their in vitro antibacterial and antifungal activity by using broth microdilution method, and many compounds showed promising activity against various tested bacteria and fungi. Among various tested compounds, 16 and 19 exhibited strongest activities against Streptococcus pyogenes and Pseudomonas aeruginosa; both have MIC value of 25 μg/mL, which is fourfold greater than the standard drug. Many compounds showed good activity against Candida albican. Analogs 11, 12, 15-17 and 19 displayed two- to fivefold greater activity against C. albican as compared to the standard drug. Results of antitubercular evaluation revealed that compounds 4 and 19 displayed strong antimycobacterial activity against H 37Rv having MIC of 25 and 62.5 lg/mL, respectively. All analogs were found to be inactive against Leishmania braziliensis except analogs 4 and 5 which exhibited strong leishmanicidal activity against Leishmania promastigotes with IC50 values of 9.3 and 8.9 μg/mL, respectively. © Springer Science+Business Media 2013.


Mungra D.C.,Sardar Patel University | Patel M.P.,Sardar Patel University | Rajani D.P.,Microcare Laboratory | Patel R.G.,Sardar Patel University
European Journal of Medicinal Chemistry | Year: 2011

A new class of β-aryloxyquinolines 3a-i and their pyrano[3,2-c] chromene derivatives 6a-r incorporating a validated molecular target has been synthesized via a nucleophilic displacement and a one-pot multicomponent reaction respectively. In vitro antimicrobial activity of the synthesized compounds were investigated against a representative panel of pathogenic strains specifically Bacillus subtilis, Clostridium tetani, Streptococcus pneumoniae, Escherichia coli, Salmonella typhi, Vibrio cholera, Aspergillus fumigatus and Candida albicans. Compounds 3c, 3e, 3g, 6f, 6l and 6q exhibited excellent antibacterial activity while compound 6p exhibited more potent antifungal activity than that of first line standard drugs. In vitro antituberculosis activity was evaluated against Mycobacterium tuberculosis H37Rv and compound 6f is emerged as the promising antimicrobial member with better antitubercular activity. Majority of the compounds appears to be better antimicrobials but poor antituberculars. © 2011 Elsevier Masson SAS. All rights reserved.


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
Medicinal Chemistry Research | Year: 2013

In an attempt to find new agents to fight against microbial infections, a series of coumarin-based 1,3,4-oxadiazol-2ylthio-N-phenyl/benzothiazolyl acetamides was synthesized starting from coumarin-3-carboxylic acid ethyl ester obtained through Knoevenagel and Pinner reaction. In vitro antimicrobial activity against several bacteria (S. aureus, B. cereus, E. coli, P. aeruginosa, K. pneumoniae, S. typhi, P. vulgaris, S. flexneri), fungi (A. niger, A. fumigatus, A. clavatus, C. albicans) and antimycobacterial activity against Mycobacterium tuberculosis H37Rv strain was assessed. This study shows to what extent the presence of various electron withdrawing/donating substituents on the phenyl or benzothiazole ring affects the activity profiles of the newer molecules. The relationship between activity profiles (MICs, 3.12-25 μg/mL) and the lipophilic character (LogP) of the prepared products is also discussed and the MIC values of the active conjugates seem to correlate to some extent with the lipophilicity profiles. Two (5e and 6c) of the final analogues displayed promising antimycobacterial activity at 12.5 μg/mL of MIC, half fold potent to the standard drug pyrazinamide (6.25 μg/mL). Compounds were characterized by IR, 1H NMR, 13C NMR spectroscopy and elemental analysis. © 2012 Springer Science+Business Media, LLC.


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
Journal of Fluorine Chemistry | Year: 2011

A series of 2-[4-cyano-(3-trifluoromethyl)phenyl amino)]-4-(4-quinoline/ coumarin-4-yloxy)-6-(fluoropiperazinyl)-s-triazines has been synthesized by a simple and efficient synthetic protocol. The antimicrobial activity of the compounds was studied against several bacteria (Staphylococcus aureus MTCC 96, Bacillus cereus MTCC 619, Escherichia coli MTCC 739, Pseudomonas aeruginosa MTCC 741, Klebsiella pneumoniae MTCC 109, Salmonella typhi MTCC 733, Proteus vulgaris MTCC 1771, Shigella flexneria MTCC 1457) and fungi (Aspergillus niger MTCC 282, Aspergillus fumigatus MTCC 343, Aspergillus clavatus MTCC 1323, Candida albicans MTCC 183) using paper disc diffusion technique and agar streak dilution method. Newly synthesized compounds were also tested for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using BACTEC MGIT and Lowenstein-Jensen MIC method. © 2011 Elsevier B.V.


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Patel P.K.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
European Journal of Medicinal Chemistry | Year: 2012

To affiliate multiple bioactivities in a compact heteronuclei, two series of benzimidazole based 1,3,4-oxadiazoles were synthesized and assessed in vitro for their efficacy as antimicrobial agents against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, Shigella flexneri), four fungi (Aspergillus niger, Aspergillus fumigatus, Aspergillus clavatus, Candida albicans) and Mycobacterium tuberculosis H37Rv and best results were observed amongst the N-benzothiazolyl aetamide series. The lipophilicity (LogP) influence on the biological profile (MICs) of the prepared products was also discussed. Upon biological screening, it was observed that the majority of the compounds were found to possess a significant broad spectrum antimicrobial (3.12-25 μg/mL of MIC) and antitubercular (6.25-25 μg/mL of MIC) potential. The structural assignments of the new products were done on the basis of IR, 1H NMR, 13C NMR spectroscopy and elemental analysis. © 2012 Elsevier Masson SAS. All rights reserved.


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Pannecouque C.,Rega Institute for Medical Research | And 2 more authors.
Future Medicinal Chemistry | Year: 2012

Background: The acquirement of resistance by microorganisms to the antimicrobial arsenal is a threat to public health. A recent WHO report estimated that 1.3 million HIV-negative people and 0.38 million HIV-positive people died from TB in 2009. Various forms of cancer account for a high percentage of deaths in both women (breast cancer) and men (prostate cancer). Results & discussion: In vitro activity assessment of newly constructed s-triazines against a panel of microorganisms including bacteria, fungi and Mycobacteria demonstrated that the compounds are of immense attraction for impending drug discovery. They were further examined for in vitro activity against breast cancer and prostate cancer cell lines, as well as HIV-1 (III B) and HIV-2 (ROD) viral strains. Proposed structural confirmation studies by IR, H NMR, 13C NMR, 19F NMR spectroscopy and elemental analysis were in accordance. Conclusion: Activity profiles of the products may contribute considerably to future drug-discovery studies. © 2012 Future Science Ltd.


Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
European Journal of Medicinal Chemistry | Year: 2011

A series of novel s-triazine analogs were synthesized and characterized by IR, 1H NMR, 13C NMR, 19F NMR spectroscopy and elemental analysis. Preliminary screening of target compounds against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, Shigella flexneria), four fungi (Aspergillus niger, Aspergillus fumigatus, Aspergillus clavatus, Candida albicans) and Mycobacterium tuberculosis H37Rv indicated that 5d, 5h, 5n, 5p, 5q, 5r, 5s, 5t and 5u were the most active compounds among twenty one studied. Thus, they were further subjected to in vitro biological evaluation against human prostate cancer cell line (DU-145) and the results indicate that two compounds 5n and 5s were markedly active. © 2011 Elsevier Masson SAS. All rights reserved.


Patel A.B.,Sardar Vallabhbhai National Institute of Technology, Surat | Patel R.V.,Sardar Vallabhbhai National Institute of Technology, Surat | Kumari P.,Sardar Vallabhbhai National Institute of Technology, Surat | Rajani D.P.,Microcare Laboratory | Chikhalia K.H.,Gujarat University
Medicinal Chemistry Research | Year: 2013

Two series of bis(3,5-dimethylpiperidinyl)-1,3,5-triazinyl)-N-(phenyl/ benzothiazolyl)-acetamides were synthesized so as to investigate their antimicrobial and antimycobacterial actions. Intermediate 4-(4,6-bis(3,5- dimethylpiperidin-1-yl)-1,3,5-triazin-2-yl)aniline was synthesized by palladium-catalyzed Suzuki cross-coupling reaction to furnish C-C bond formation to s-triazine ring. Pharmacological screening against eight bacteria (S. aureus, B. cereus, E. coli, P. aeruginosa, K. pneumoniae, S. typhi, P. vulgaris, and S. flexneri), four fungi (A. niger, A. fumigatus, A. clavatus, and C. albicans), and Mycobacterium tuberculosis H37Rv was examined and the effects of various substituents on biological profiles (MIC, 1.56-50 μg/mL) of final analogues were investigated. Four (8c, 8i, 9d, 9j) of the final analogues displayed antimycobacterial activity (3.12-6.25 μg/mL) equipotent to standard drugs. © 2012 Springer Science+Business Media, LLC.


Patel N.B.,Veer Narmad South Gujarat University | Khan I.H.,Veer Narmad South Gujarat University | Rajani S.D.,Microcare Laboratory
European Journal of Medicinal Chemistry | Year: 2010

The triazole analogs were obtained via. multistep synthesis sequence beginning with ethyl nicotinoate 3 which on treatment with hydrazine hydrate yields nicotinoyl hydrazide 4. Intermolecular cyclisation of 4 with 4-methylbenzoic acid in presence of phosphorous oxy chloride affords 2-(3-pyridyl)-5-(4-methylphenyl)-1,3,4-oxadiazole 5. Condensation of 5 with various substituted 2-hydrazino benzothiazole 2a-j results in 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-substituted-1,3-benzothiazol-2-amino) -4H-1,2,4-triazole 6a-j analogs. All the compounds have been characterized by elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data. In vitro antitubercular activity was carried out against Mycobacterium tuberculosis H 37Rv strain using Lowenstein-Jensen medium and antimicrobial activity against various bacteria and fungi using broth microdilution method. Compounds 2e, 6a, 6b, 6c, 6d, 6g, 6h and 6i emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antituberculars. Compound 6j showed better antitubercular activity compared to rifampicin. 3-(3-Pyridyl)-5-(4-methylphenyl) -4-(N-substituted-1,3-benzothiazol-2-amino)-4H-1,2,4-triazole 6a-j were synthesized and their antitubercular activity against H 37Rv and antimicrobial activities have been tested. © 2010 Elsevier Masson SAS. All rights reserved.


Patel M.C.,P.A. College | Nilesh N.G.,P.A. College | Rajani D.P.,Microcare Laboratory
Der Pharma Chemica | Year: 2011

Novel (3E)-3-[[4-(Aryl or Alkyl sulfonyl, Aryl carbonyl and Heteroaryl) piperazin-1-yl] methylene] chroman-4-one and N-[1-(Aryl or Alkyl sulfonyl, Aryl carbonyl and Heteroaryl) -4-piperidyl]-6-methyl-4-oxo-chromene-3-carboxamide were synthesized and identified by spectroscopic techniques like NMR, IR, MS and elemental analysis. Antibacterial study of the same derivatives were done using bacterial model like E. coli, P.aeruginosa, S. aureus, and S.Pyogenus and antifungal study of the same were carried out using Candida albicans, A. Niger and A.Clavatus. Results show that the compound having 3-chloropropane sulfonyl type linkage has shown good activity against the bacterial strains, while some of the derivatives have shown moderate improvement in activity against pathogenic strains.

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