@article { ISI:000231712000007, title = {Synthesis of bile acid dimers linked with 1,2,3-triazole ring at C-3, C-11, and C-24 positions}, journal = {Synlett}, number = {14}, year = {2005}, month = {SEP}, pages = {2155-2158}, publisher = {GEORG THIEME VERLAG KG}, type = {Article}, address = {RUDIGERSTR 14, D-70469 STUTTGART, GERMANY}, abstract = {

1,3-Dipolar cycloaddition of propargyl ester of a bile acid to an azide group attached at different positions of another bile acid gave three new 1,2,3-triazole-containing dimeric analogues in excellent yields.

}, keywords = {1, 2, 3-dipolar cycloaddition, 3-Triazole, Bile acids, Click chemistry, steroidal dimers}, issn = {0936-5214}, doi = {10.1055/s-2005-872223}, author = {Aher, Nilkanth G. and Pore, VS} } @article { ISI:000241967600018, title = {Design and synthesis of fluconazole/bile acid conjugate using click reaction}, journal = {Tetrahedron}, volume = {62}, number = {48}, year = {2006}, month = {NOV}, pages = {11178-11186}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, type = {Article}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

Novel fluconazole/bile acid conjugates were designed and their regioselective synthesis was achieved in very high yield via Cu(I) catalyzed intermolecular 1,3-dipolar cycloaddition. These new molecules showed good antifungal activity against Candida species. (c) 2006 Elsevier Ltd. All rights reserved.

}, keywords = {1, 2, 3-Triazole, Antifungal agent, bile acid, Click chemistry, fluconazole/bile acid conjugate}, issn = {0040-4020}, doi = {10.1016/j.tet.2006.09.021}, author = {Pore, Vandana S. and Aher, Nilkanth G. and Kumar, Manish and Shukla, Praveen K.} } @article { ISI:000252235900014, title = {Design, synthesis, and micellar properties of bile acid dimers and oligomers linked with a 1,2,3-triazole ring}, journal = {Tetrahedron}, volume = {63}, number = {52}, year = {2007}, month = {DEC}, pages = {12927-12934}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, type = {Article}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

1,3-Dipolar cycloaddition of propargyl esters of bile acids to azide group attached at different positions of bile acids gave dimers, trimer, and tetramer linked with 1,2,3-triazole. These dimeric and oligomeric structures were able to solubilize hydrophilic dye-cresol red, in nonpolar solvent. (c) 2007 Elsevier Ltd. All rights reserved.

}, issn = {0040-4020}, doi = {10.1016/j.tet.2007.10.042}, author = {Aher, Nilkanth G. and Pore, Vandana S. and Patil, Sachin P.} } @article { ISI:000269760900028, title = {Design and synthesis of bile acid-based amino sterols as antimicrobial agents}, journal = {Bioorganic \& Medicinal Chemistry Letters}, volume = {19}, number = {18}, year = {2009}, month = {SEP}, pages = {5411-5414}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

New bile acid-based amino sterols were synthesized in good yields from C-3 beta-oxiranes as key intermediates. These derivatives were evaluated for their in vitro antimicrobial properties against human pathogens. These compounds showed better antibacterial activity as compared to antifungal activity. Compounds 21 and 22 showed comparable antibacterial activity to gentamicin against Staphylococcus aureus with IC(50) values of 5.14 and 4.46 mu g/mL. This is the first report for the synthesis of C-3 beta-oxiranes on the steroids having A/B cis ring junction and these oxiranes have been used for the synthesis of amino sterols 17, 18, 21, and 22. (C) 2009 Elsevier Ltd. All rights reserved.

}, keywords = {Amino sterols, Antibacterial agent, bile acid, Oxirane}, issn = {0960-894X}, doi = {10.1016/j.bmcl.2009.07.117}, author = {Aher, Nilkanth G. and Pore, Vandana S. and Mishra, Nripendra N. and Shukla, Praveen K. and Gonnade, Rajesh G.} } @article { ISI:000269337500025, title = {Stereoselective construction of steroidal side chain from 16-dehydropregnenolone acetate}, journal = {Synlett}, number = {12}, year = {2009}, month = {JUL}, pages = {2005-2009}, publisher = {GEORG THIEME VERLAG KG}, address = {RUDIGERSTR 14, D-70469 STUTTGART, GERMANY}, abstract = {

Stereoselective construction of steroidal side chain at C-20 having {\textquoteleft}natural{\textquoteright} configuration using 16-dehydropregnalone acetate (16-6PA) as a starting material has been carried out. Palladium-catalyzed carbon-carbon bond-forming Heck reaction between C-20 vinyl iodide with methyl acrylate and transfer hydrogenation with triethylsilane and Pd/C are the key steps for stereoselective side-chain synthesis.

}, keywords = {16-dehydropregnenolone acetate, Heck coupling, stereoselectivity, steroidal side chain, transfer hydrogenation}, issn = {0936-5214}, doi = {10.1055/s-0029-1217521}, author = {Aher, Nilkanth G. and Gonnade, Rajesh G. and Pore, Vandana S.} } @article { ISI:000262707000040, title = {Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues}, journal = {Bioorganic \& Medicinal Chemistry Letters}, volume = {19}, number = {3}, year = {2009}, month = {FEB}, pages = {759-763}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

Fluconazole based novel mimics containing 1,2,3-triazole were designed and synthesized as antifungal agents. Their antifungal activities were evaluated in vitro by measuring the minimal inhibitory concentrations (MICs). Compounds 12, 15, and 16 were found to be more potent against Candida fungal pathogens than control drugs fluconazole and amphotericin B. The studies presented here provide structural modi. cation of fluconazole to give 1,2,3-trazole containing molecules. Furthermore, these molecules were evaluated in vivo against Candida albicans intravenous challenge in Swiss mice and antiproliferative activities were tested against human hepatocellular carcinoma Hep3B and human epithelial carcinoma A431. It was found that compound 12 resulted in 97.4\% reduction in fungal load in mice and did not show any profound proliferative effect at lower dose (0.001 mg/ml). (C) 2008 Elsevier Ltd. All rights reserved.

}, keywords = {1, 2, 3-Triazole, Antifungal agent, bile acid, Conjugates, Fluconazole}, issn = {0960-894X}, doi = {10.1016/j.bmcl.2008.12.026}, author = {Aher, Nilkanth G. and Pore, Vandana S. and Mishra, Nripendra N. and Kumar, Awanit and Shukla, Praveen K. and Sharma, Aanchal and Bhat, Manoj K.} }