@article { ISI:000359956500020, title = {First regioselective iodocyclization reaction of 3-aryl-5-(prop-2-ynylthio)-1H-1,2,4-triazoles}, journal = {Tetrahedron Letters}, volume = {56}, number = {36}, year = {2015}, month = {SEP}, pages = {5140-5144}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

The regioselective iodocyclization reaction of 3-aryl-5-(prop-2-ynylthio)-1H-1,2,4-triazoles is described for the first time. The iodocyclization reaction of 3-aryl-5-(prop-2-ynylthio)-1H-1,2,4-triazoles using molecular iodine afforded diiodo-compound which on Cul-catalyzed intramolecular C-N coupling reaction gave six-membered 2-aryl-51141,2,4]triazolo[5,1-b][1,3]thiazines, whereas, the five membered 3-aryl-5,6-dihydrothiazolo[2,3-c][1,2,4]triazoles were obtained exclusively when the iodocyclization reaction of 3-aryl-5-(prop-2-ynylthio)-1H-1,2,4-triazoles was carried out using NIS. (C) 2015 Elsevier Ltd. All rights reserved.

}, keywords = {Iodocyclization, Regloselective, Thiazine, Triazole}, issn = {0040-4039}, doi = {10.1016/j.tetlet.2015.07.006}, author = {Rode, Navnath D. and Sonawane, Amol D. and Garud, Dinesh R. and Joshi, Rohini R. and Joshi, Ramesh A. and Likhite, Anjali P.} } @article { ISI:000365222000045, title = {Regioselective and diastereoselective iodocyclization reaction of alkene-thioureas: an efficient approach to bicyclic beta-lactams}, journal = {New Journal of Chemistry}, volume = {39}, number = {12}, year = {2015}, month = {SEP}, pages = {9422-9428}, publisher = {ROYAL SOC CHEMISTRY}, address = {THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND}, abstract = {

Bicyclic beta-lactams, i.e. 3-thia-1-dethiacephams, were synthesized via a highly regioselective and diastereoselective iodocyclization reaction of alkene-thioureas with molecular iodine. Furthermore, the structure of 3-thia-1-dethiacepham was confirmed by a chemical method, the dehydrohalogenation reaction using DBU.

}, issn = {1144-0546}, doi = {10.1039/c5nj01963j}, author = {Garud, Dinesh R. and Sonawane, Amol D. and Auti, Jyoti B. and Rode, Navnath D. and Ranpise, Vinod R. and Joshi, Rohini R. and Joshi, Ramesh A.} } @article {44091, title = {Synthesis, biological evaluation, and molecular docking studies of novel 3-aryl-5-(alkyl-thio)-1H-1,2,4-triazoles derivatives targeting Mycobacterium tuberculosis}, journal = {Chemical Biology \& Drug Design}, volume = {90}, year = {2017}, month = {DEC}, pages = {1206-1214}, type = {Article}, abstract = {A small library of new 3-aryl-5-(alkyl-thio)-1H-1,2,4-triazoles was synthesized and screened for the antimycobacterial potency against Mycobacterium tuberculosis H37Ra strain and Mycobacterium bovis BCG both in active and dormant stage. Among the synthesized library, 25 compounds exhibited promising anti-TB activity in the range of IC(50)0.03-5.88g/ml for dormant stage and 20 compounds in the range of 0.03-6.96g/ml for active stage. Their lower toxicity (>100g/ml) and higher selectivity (SI=>10) against all cancer cell lines screened make them interesting compounds with potential antimycobacterial effects. Furthermore, to rationalize the observed biological activity data and to establish a structural basis for inhibition of M.tuberculosis, the molecular docking study was carried out against a potential target MTB CYP121 which revealed a significant correlation between the binding score and biological activity for these compounds. Cytotoxicity and in vivo pharmacokinetic studies suggested that 1,2,4-triazole analogues have an acceptable safety index, in vivo stability and bio-availability.}, doi = {10.1111/cbdd.13040}, author = {Rode, Navnath D. and Sonawane, Amol D. and Nawale, Laxman and Khedkar, Vijay M. and Joshi, Ramesh A. and Likhite, Anjali P. and Sarkar, Dhiman and Joshi, Rohini R.} } @article {48770, title = {Metal-free isoamyl nitrite mediated efficient synthesis of 1,2,4-oxadiazoles}, journal = {Tetrahedron Letters}, volume = {125}, year = {2023}, month = {JUL}, pages = {154616}, type = {Article}, abstract = {

We report herein, a metal-free isoamyl nitrite mediated efficient synthesis of 1,2,4-oxadiazoles by one pot cycloaddition reaction of aldoximes with nitriles. The structure of the 1,2,4-oxadiazole derivatives was confirmed by studies of spectral analysis. Current methodology provides a novel pathway to access 1,2,4-oxadiazole derivatives.\& COPY; 2023 Elsevier Ltd. All rights reserved.

}, keywords = {1, 2, 4-Oxadiazole, Aldoxime, Cycloaddition, Isoamyl nitrite}, issn = {0040-4039}, doi = {10.1016/j.tetlet.2023.154616}, author = {Galave, Sharad A. and Kadam, Kishorkumar S. and Sonawane, Amol D. and Pansare, Vaibhav R. and Garud, Dinesh R.} }