01364nas a2200253   4500008004100000022001400041245009200055210006900147260011700216300001200333520037600345653001300721653002900734653003900763653001700802653002300819100002300842700002600865700002100891700002600912700002600938700002800964856011800992       2009                        eng d  a1424-637600aAmmonium metavanadate: an effective catalyst for synthesis of alpha-hydroxyphosphonates0 aAmmonium metavanadate an effective catalyst for synthesis of alp  aC/O ALAN R KATRITZKY, UNIV FLORIDA, DEPT CHEMISTRY, PO BOX 117200, GAINESVILLE, FL 32611 USAbARKAT USA INCcDEC  a138-1483 a<p>Ammonium metavanadate (NH(4)VO(3)) is an inexpensive, efficient and mild catalyst for the synthesis of alpha-hydroxyphosphonate derivatives by the reaction of various aryl or heteroaryl aldehydes with triethylphosphite at room temperature. This method affords the alpha-hydroxyphosphonates in short reaction times, under solvent-free conditions, and in high yield.</p>10aAldehyde10aalpha-hydroxyphosphonate10aAmmonium metavanadate (NH(4)VO(3))10aSolvent-free10aTriethyl phosphite1 aSonar, Swapnil, S.1 aKategaonkar, Amol, H.1 aWare, Madhav, N.1 aGill, Charansingh, H.1 aShingate, Bapurao, B.1 aShingare, Murlidhar, S.  uhttps://library.ncl.res.in/content/ammonium-metavanadate-effective-catalyst-synthesis-alpha-hydroxyphosphonates-000962nas a2200181   4500008004100000022001400041245006000055210005700115260008000172300001200252490000700264520031500271100002400586700002600610700002600636700002600662856009200688       2009                        eng d  a0971-162700aGreen and sustainable approach to BIS-(INDOLYL) alkanes0 aGreen and sustainable approach to BISINDOLYL alkanes  aC-85 SECTOR-B, ALIGANJ SCHEME, LUCKNOW, INDIA 226020 USAbDR R S VARMAcJAN  a279-2820 v183 a<p>An efficient, high yielding, green and mild method has been developed for the synthesis of bis (indolyl) methanes using dodecylsulphonic acid as an effective surfactant type Bronsted acid catalyst in aq media. The method is excellent for various new bis-(indolyl) methanes derived from pyrazolaldehydes.</p>1 aGholap, Somnath, S.1 aWakchaure, Prasad, B.1 aPandhare, Gajanan, R.1 aGill, Charansingh, H.  uhttps://library.ncl.res.in/content/green-and-sustainable-approach-bis-indolyl-alkanes-001475nas a2200241   4500008004100000022001400041245011000055210006900165260007300234300001000307490000700317520058300324653003300907653001400940653002200954653001500976100002200991700002301013700002101036700002001057700002601077856013001103       2012                        eng d  a1350-417700aUltrasound assisted one pot synthesis of imidazole derivatives using diethyl bromophosphate as an oxidant0 aUltrasound assisted one pot synthesis of imidazole derivatives u  aPO BOX 211, 1000 AE AMSTERDAM, NETHERLANDSbELSEVIER SCIENCE BVcJAN  a94-960 v193 a<p>A one pot, three-component condensation of benzoin/benzyl, an aldehyde, and ammonium acetate using diethyl bromophosphate as a mild oxidant is achieved to form trisubstituted imidazole compounds. Under ultrasound irradiation, a smooth condensation occurs to get the 2, 4, 5-triaryl-1H-imidazole compounds in good to excellent yields. The study explores the scope and limitation of diethyl bromophosphate as an oxidant and suggests advantages, viz., simplicity of operation, reduction in time, and an increase in product yields. (C) 2011 Elsevier B.V. All rights reserved.</p>10aDiethyl bromophosphate (DEP)10aImidazole10aOne pot synthesis10aUltrasound1 aNagargoje, Deepak1 aMandhane, Priyanka1 aShingote, Savita1 aBadadhe, Pravin1 aGill, Charansingh, H.  uhttps://library.ncl.res.in/content/ultrasound-assisted-one-pot-synthesis-imidazole-derivatives-using-diethyl-bromophosphate-001798nas a2200349   4500008004100000022001400041245013200055210006900187260009200256300001400348490000800362520061500370653000600985653000600991653001700997653002201014653001801036653001601054653000901070653002901079100002401108700001801132700001601150700002001166700002001186700001701206700002101223700002501244700002201269700002601291856013101317       2015                        eng d  a1042-650700aSynthesis, antioxidant, anti-inflammatory, and antimicrobial screening of newer thiophene-fused arylpyrazolyl 1,3,4-oxadiazoles0 aSynthesis antioxidant antiinflammatory and antimicrobial screeni  a4 PARK SQUARE, MILTON PARK, ABINGDON OX14 4RN, OXON, ENGLANDbTAYLOR & FRANCIS LTDcNOV  a1803-18130 v1903 a<p>A series of newer 1,3,4-oxadiazole derivatives 3a-h, 5a-h containing a thiophene fused with pyrazole moiety of pharmacological significance have been synthesized. The compounds were characterized by H-1 NMR, IR, and mass spectral techniques. The compounds were screened for their in vitro antioxidant, anti-inflammatory and antimicrobial activities. Among them, Compounds 3b (EC50-14.98) and 3f (EC50-12.21) showed significant antioxidant activity. Compound 3a (EC50-15.23) showed good anti-inflammatory activity. Compound 3d was found as the most active derivative against bacterial and fungal strains.</p>10a110a310a4-Oxadiazole10aAnti-inflammatory10aAntimicrobial10aAntioxidant10aEC5010aThiophene-fused pyrazole1 aMahajan, Pravin, S.1 aNikam, Mukesh1 aChate, Asha1 aNimbalkar, Urja1 aPatil, Vrushali1 aBobade, Anil1 aChaudhari, Abhay1 aDeolankar, Dattatray1 aJavale, Balasaheb1 aGill, Charansingh, H.  uhttps://library.ncl.res.in/content/synthesis-antioxidant-anti-inflammatory-and-antimicrobial-screening-newer-thiophene-fused-002318nas a2200265   4500008004100000022001400041245006800055210006600123260007100189300001200260490000600272520144900278653002201727653001701749653001701766653001201783653002201795100002401817700002201841700002301863700002301886700001901909700002601928856009801954       2016                        eng d  a1948-587500aSynthesis and antitubercular activity of new benzo[b]thiophenes0 aSynthesis and antitubercular activity of new benzobthiophenes  a1155 16TH ST, NW, WASHINGTON, DC 20036 USAbAMER CHEMICAL SOCcAUG  a751-7560 v73 a<p>In vitro and ex vivo efficacies of four series of benzo[b]thiophene-2-carboxylic acid derivatives were studied against Mycobacterium tuberculosis H37Ra (MTB). Benzo[b]thiophenes were also tested in vitro against multidrug resistant Mycobacterium tuberculosis H37Ra (MDR-MTB), and 7b was found to be highly active against A- and DMDR-MTB/MTB (MIC ranges 2.73-22.86 mu g/mL). The activity of all benzo[b]-thiophenes against M. bovis BCG (BCG) was also assessed grown under aerobic and under conditions of oxygen depletion. Compounds 8c and 8g showed significant activity with MICs of 0.60 and 0.61 mu g/mL against dormant BCG. The low cytotoxicity and high selectivity index data against human cancer cell lines, HeLa, Panc-1, and THP-1 indicate the potential importance of the development of benzo[b]thiophene-based 1,3-diketones and flavones as lead candidates to treat mycobacterial infections. Molecular docking studies into the active site of DprE1 (Decaprenylphosphoryl-beta-n-ribose-2'-epimerase) enzyme revealed a similar binding mode to native ligand in the crystal structure thereby helping to understand the ligand protein interactions and establish a structural basis for inhibition of MTB. In summary, its good activity in in vitro and ex vivo model, as well as its activity against multidrug-resistant M. tuberculosis H37Ra in a potentially latent state, makes 7b an attractive drug candidate for the therapy of tuberculosis.</p>10aBenzo[b]thiophene10aCytotoxicity10aM. Bovis BCG10aMDR-MTB10aMolecular docking1 aMahajan, Pravin, S.1 aNikam, Mukesh, D.1 aNawale, Laxman, U.1 aKhedkar, Vijay, M.1 aSarkar, Dhiman1 aGill, Charansingh, H.  uhttps://library.ncl.res.in/content/synthesis-and-antitubercular-activity-new-benzobthiophenes02019nas a2200265   4500008004100000022001400041245015300055210006900208260007400277300001400351490000700365520100300372653002201375653001601397653001801413653002101431653003601452100002401488700002201512700002301534700002101557700001901578700002601597856013001623       2016                        eng d  a0922-616800aSynthesis, biological evaluation and molecular docking studies of N-acylheteroaryl hydrazone derivatives as antioxidant and anti-inflammatory agents0 aSynthesis biological evaluation and molecular docking studies of  aVAN GODEWIJCKSTRAAT 30, 3311 GZ DORDRECHT, NETHERLANDSbSPRINGERcMAR  a2707-27290 v423 a<p>In search of new therapeutics with greater potency, three new series of 3-methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carbohydrazide derivatives have been synthesized and evaluated for their in vitro antioxidant and anti-inflammatory activities. The hydrazones bearing a core pyrazole, chromone and tetrazolo[1,5-a]quinoline scaffold showed promising activities. Interestingly, compounds 3a (EC50 = 06.00 +/- A 2.36) and 5c (EC50 = 07.21 +/- A 0.67) showed the most potent antioxidant activity, while compounds 3a (EC50 = 10.25 +/- A 1.08), 7b (EC50 = 10.50 +/- A 0.99) and 7c (EC50 = 11.18 +/- A 0.15) showed significant anti-inflammatory activity. Furthermore, molecular docking studies also revealed a significant correlation between the binding score and biological activity for these compounds to describe the molecular basis for the structure activity relationship (SAR) results. As these compounds are good cyclooxygenase inhibitors, isoenzyme inhibitory potency studies are warranted.</p>10aAnti-inflammatory10aAntioxidant10aDocking study10aN-Acylhydrazones10aStructure-activity relationship1 aMahajan, Pravin, S.1 aNikam, Mukesh, D.1 aKhedkar, Vijay, M.1 aJha, Prakash, C.1 aSarkar, Dhiman1 aGill, Charansingh, H.  uhttps://library.ncl.res.in/content/synthesis-biological-evaluation-and-molecular-docking-studies-n-acylheteroaryl-hydrazone-101364nas a2200193   4500008004100000245016500041210006900206260000800275300001400283490000700297520060700304100002400911700002200935700001900957700001700976700002400993700002601017856012701043       2017                        eng d00aOrganocatalyzed efficient one-pot synthesis, biological evaluation, and molecular docking studies of 4,4-(Arylmethylene)bis-(3-methyl-1-phenyl-1H-pyrazol-5-ols)0 aOrganocatalyzed efficient onepot synthesis biological evaluation  cMAR  a1109-11200 v543 aThe synthesis of 4,4-(arylmethylene)bis-(3-methyl-1-phenyl-1H-pyrazol-5-ol) derivatives catalyzed by ?-proline is a simple, versatile, and efficient method. In vitro antioxidant, anti-inflammatory, and antimicrobial activities of compounds 4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i, 4j were studied. Furthermore, to rationalize the observed anti-inflammatory activity data, molecular docking study has been performed against COX-2 enzyme which revealed a good binding affinity for these molecules and could provide an insight into the various bonded and non-bonded interactions guiding their binding affinity.1 aMahajan, Pravin, S.1 aNikam, Mukesh, D.1 aKhedkar, Vijay1 aJha, Prakash1 aBadadhe, Pravin, V.1 aGill, Charansingh, H.  uhttps://library.ncl.res.in/content/organocatalyzed-efficient-one-pot-synthesis-biological-evaluation-and-molecular-docking