@article { ISI:000234092500005, title = {Convenient synthesis of the enantiomerically pure beta-blocker (S)-betaxolol using hydrolytic kinetic resolution}, journal = {Tetrahedron-Asymmetry}, volume = {16}, number = {23}, year = {2005}, month = {NOV}, pages = {3802-3806}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, type = {Article}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

Enantiopure (S)-betaxolol was prepared in an extremely simple and practical way using hydrolytic kinetic resolution of a terminal epoxide by Jacobsen{\textquoteright}s catalyst. High enantiomeric purity (99\% ee) has been achieved and the method is amenable to industrial scale-up. (c) 2005 Elsevier Ltd. All rights reserved.

}, issn = {0957-4166}, doi = {10.1016/j.tetasy.2005.10.028}, author = {Joshi, Ramesh A. and Garud, Dinesh R. and Muthukrishnan, Murugan and Joshi, Rohini R. and Gurjar, M. K.} } @article { ISI:000238072500037, title = {Pictet-Spengler cyclization in room temperature ionic liquid: a convenient access to tetrahydro beta-carbolines}, journal = {Journal of Heterocyclic Chemistry}, volume = {43}, number = {3}, year = {2006}, month = {MAY}, pages = {767-772}, publisher = {HETERO CORPORATION}, type = {Article}, address = {PO BOX 170, PROVO, UT 84603-0170 USA}, abstract = {

1,2,3,4-Tetrahydro-beta-carbolines have been synthesized in moderate to good yields in short reaction time using the ionic liquid [bbim] BF4 as reaction medium and promoter. There was no need for the use of an additional catalyst normally employed in Pictet-Spengler condensation.

}, issn = {0022-152X}, author = {Muthukrishnan, Murugan and More, Shivaji V. and Garud, Dinesh R. and Ramana, C. V. and Joshi, Rohini R. and Joshi, Ramesh A.} } @article { ISI:000244054900016, title = {Concise synthesis of beta-blockers (S)-metoprolol and (S)-betaxolol using hydrolytic kinetic resolution}, journal = {Tetrahedron}, volume = {63}, number = {8}, year = {2007}, month = {FEB}, pages = {1872-1876}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, type = {Article}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

Enantiopure (S)-metoprolol and (S)-betaxolol were prepared in an extremely simple and practical way using Jacobsen{\textquoteright}s hydrolytic kinetic resolution of terminal epoxides in isopropanol. (c) 2007 Elsevier Ltd. All rights reserved.

}, keywords = {beta-blockers, betaxolol, Hydrolytic kinetic resolution, metoprolol}, issn = {0040-4020}, doi = {10.1016/j.tet.2006.12.016}, author = {Muthukrishnan, Murugan and Garud, Dinesh R. and Joshi, Rohini R. and Joshi, Ramesh A.} } @article { ISI:000343624300030, title = {First iodocyclization reaction of allene-thioureas: an efficient approach to bicyclic beta-lactams}, journal = {Tetrahedron Letters}, volume = {55}, number = {43}, year = {2014}, month = {OCT}, pages = {5998-6000}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

The regioselective iodocyclization reaction of allene-thioureas is described, for the first time, for the synthesis of bicyclic beta-lactams. The substitution at the allenyl part heavily influenced the iodocyclization reaction. The iodocyclization reaction of the unsubstituted allene-thioureas afforded six-membered 3-thia-1-dethiacephems whereas, the substituted allene-thiourea afforded seven-membered thiazepines along with five-membered isopenams. (C) 2014 Elsevier Ltd. All rights reserved.

}, keywords = {Allene, beta-Lactams, Iodocyclization, Regioselective, thiourea}, issn = {0040-4039}, doi = {10.1016/j.tetlet.2014.09.004}, author = {Garud, Dinesh R. and Jadhav, Amol R. and Lahore, Santosh V. and Kahar, Nilesh M. and Joshi, Rohini R. and Joshi, Ramesh A. and Koketsu, Mamoru} } @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 { ISI:000366209800015, title = {Synthesis of 3-Thia-1-dethiacephems via Regioselective Iodocyclization Reaction}, journal = {Synthesis-Stuttgart}, volume = {47}, number = {24}, year = {2015}, month = {DEC}, pages = {3956-3962}, publisher = {GEORG THIEME VERLAG KG}, address = {RUDIGERSTR 14, D-70469 STUTTGART, GERMANY}, abstract = {

The key N-homopropargylthiourea intermediates, N-substituted 2-oxo-4-propargylazetidine-1-carbothioamides, were prepared by the reaction of a 4-propargylazetidin-2-one with isothiocyanates. Bicyclic -lactams, i.e. 3-thia-1-dethiacephems, were prepared via highly regioselective iodocyclization reaction of N-substituted 2-oxo-4-propargylazetidine-1-carbothioamides with molecular iodine at room temperature in moderate to excellent yields. A variety of functional groups were well tolerated under the reaction conditions.

}, keywords = {-lactams, 3-thia-1-dethiacephems, Iodocyclization, Regioselective, thiourea}, issn = {0039-7881}, doi = {10.1055/s-0035-1560350}, author = {Garud, Dinesh R. and Rode, Navnath D. and Bathe, Sagar R. and Ranpise, Vinod S. and Joshi, Ramesh A. and Joshi, Rohini R. and Koketsu, Mamoru} } @article {46359, title = {Non nucleoside reverse transcriptase inhibitors, molecular docking studies and antitubercular activity of thiazolidin-4-one derivatives}, journal = {Current Computer-Aided Drug Design}, volume = {15}, year = {2019}, month = {JAN}, pages = {433-444}, type = {Article}, abstract = {

Background: Management of Co-existence of Acquired immunodeficiency syndrome and Tuberculosis has become a global challenge due to the emergence of resistant strains and pill burden. Objective: Hence the aim of the present work was to design and evaluate compounds for their dual activity on HIV-1 and Tuberculosis (TB). Methods: A series of seven, novel Thiazolidin-4-one derivatives were synthesized and evaluated for their anti-HIV and anti-tubercular activity along with Molecular docking studies. All the seven compounds displayed promising activity against the replication of HIV-1 in cell-based assays. The four most active compounds were further evaluated against X4 tropic HIV-1(UG)(070) and R5 tropic HIV-1(vB59) primary isolates. The binding affinity of all the designed compounds for HIV-RT and Mycobacterium tuberculosis Enol Reductase (MTB InhA) was gauged by molecular docking studies which revealed crucial thermodynamic interactions governing their binding. Results: The CC50 values for the test compounds were in the range of, 15.08-34.9 mu g/ml, while the IC50 values were in the range of 16.1-27.13(UG(070); X4) and 12.03-23.64 (VB59; R5) mu g/ml. The control drug Nevirapine (NVP) exhibited CC50 value of 77.13 mu g/ml and IC50 value of 0.03 mu g/ml. Amongst all these compounds, compound number 3 showed significant activity with a TI value of 2.167 and 2.678 against the HIV-1 X4 and the R5 tropic virus respectively. In anti-mycobacterial screening, the compounds proved effective in inhibiting the growth of both log phase and starved MTB cultures. Conclusion: Compound 3 has been found to be active against HIV-1 as well as MTB.

}, keywords = {anti-HIV-1 activity, Antitubercular activity, human immunodeficiency virus-1, Molecular docking, Non nucleoside reverse transcriptase, thiazolidin-4-ones}, issn = {1573-4099}, doi = {10.2174/1573409915666181221102903}, author = {Chitre, Trupti S. and Patil, Shital M. and Sujalegaonkar, Anagha G. and Asgaonkar, Kalyani D. and Khedkar, Vijay M. and Garud, Dinesh R. and Jha, Prakash C. and Gaikwad, Sharddha Y. and Kulkarni, Smita and Choudhari, Amit and Sarkar, Dhiman} } @article {46713, title = {Efficient method for the synthesis of quinoxaline derivatives catalyzed by titanium silicate-1}, journal = {Research on Chemical Intermediates}, volume = {46}, year = {2020}, month = {DEC}, pages = {5219-5230}, type = {Article}, abstract = {

A series of quinoxaline derivatives were efficiently synthesized by convenient and simple procedure in excellent yields using 1 wt.\% of titanium silicate (TS-1) catalyzed reaction of 1,2-diamines and 1,2-diketones in methanol at room temperature. This reaction is scalable to multigram scale and the catalyst is recyclable. [GRAPHICS] .

}, keywords = {2-Diketones, Aromatic 1, o-Phenylenediamine, Quinoxaline, Room temperature, Titanium silicate-1}, issn = {0922-6168}, doi = {10.1007/s11164-020-04258-w, Early Access Date = SEP 2020}, author = {Chandrachood, Pranav S. and Jadhav, Amol R. and Garud, Dinesh R. and Deshpande, Nirmala R. and Puranik, Vedavati G. and Kashalkar, Rajashree V.} } @article {47125, title = {In silico studies, synthesis and antitubercular activity of some novel quinoline - azitidinone derivatives}, journal = {Current Computer-Aided Drug Design}, volume = {17}, year = {2021}, month = {JAN}, pages = {134-143}, type = {Article}, abstract = {

Background: Diarylquinolines like Bedaquiline have shown promising antitubercular activity by their action of Mycobacterial ATPase. Objective: The structural features necessary for a good antitubercular activity for a series of quinoline derivatives were explored through computational chemistry tools like QSAR and combinatorial library generation. In the current study, 3-Chloro-4-(2-mercaptoquinoline-3-yl)-1-substitutedphenylazitidin-2-one derivatives have been designed and synthesized based on molecular modeling studies as anti-tubercular agents. Methods: 2D and 3D QSAR analyses were used to designed compounds having a quinoline scaffold. The synthesized compounds were evaluated against active and dormant strains of Mycobacterium tuberculosis (MTB) H37 Ra and Mycobacterium bovis BCG. The compounds were also tested for cytotoxicity against MCF-7, A549 and Panc-1 cell lines using MTT assay. The binding affinity of designed compounds was gauged by molecular docking studies. Results: Statistically significant QSAR models generated by the SA-MLR method for 2D QSAR exhibited r(2) = 0.852, q(2) = 0.811, whereas 3D QSAR with SA-kNN showed q(2) = 0.77. The synthesized compounds exhibited MIC in the range of 1.38-14.59(mu g/ml). These compounds showed some crucial interaction with MTB ATPase. Conclusion: The present study has shown some promising results which can be further explored for lead generation.

}, keywords = {combilib, Molecular docking, mycobacterial ATPase, QSAR, Quinoline}, issn = {1573-4099}, doi = {10.2174/1573409916666200129095952}, author = {Chitre, Trupti S. and Asgaonkar, Kalyani D. and Vikhe, Amrut B. and Patil, Shital M. and Garud, Dinesh R. and Khedkar, Vijay M. and Sarkar, Dhiman and Nawale, Laxman U. and Yeware, Amar} } @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.} }