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Items: 1 to 50 of 61

1.

Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir.

A M Subbaiah M, Mandlekar S, Desikan S, Ramar T, Subramani L, Annadurai M, Desai SD, Sinha S, Jenkins SM, Krystal MR, Subramanian M, Sridhar S, Padmanabhan S, Bhutani P, Arla R, Singh S, Sinha J, Thakur M, Kadow JF, Meanwell NA.

J Med Chem. 2019 Apr 11;62(7):3553-3574. doi: 10.1021/acs.jmedchem.9b00002. Epub 2019 Apr 2.

PMID:
30938524
2.

Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.

Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB 3rd, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH.

ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. doi: 10.1021/acsmedchemlett.8b00439. eCollection 2019 Mar 14.

PMID:
30891130
3.

Relative quantitation of endogenous proteins by quadrupole-time of flight and tandem mass spectrometry.

Gautam SS, Wagh S, Babu S, Gudihal R, Rajagopalan S, Kole P, Mandlekar S, Subramanian M.

J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Feb 1;1106-1107:11-18. doi: 10.1016/j.jchromb.2018.12.023. Epub 2018 Dec 28. No abstract available.

PMID:
30615973
4.

Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.

Subbaiah MAM, Meanwell NA, Kadow JF, Subramani L, Annadurai M, Ramar T, Desai SD, Sinha S, Subramanian M, Mandlekar S, Sridhar S, Padmanabhan S, Bhutani P, Arla R, Jenkins SM, Krystal MR, Wang C, Sarabu R.

J Med Chem. 2018 May 10;61(9):4176-4188. doi: 10.1021/acs.jmedchem.8b00277. Epub 2018 Apr 25.

PMID:
29693401
5.

Spotting of external calibration standards on blank dried blood spots as a resource-sparing protocol.

Nigam A, Kole P, Kurawattimath V, Mandlekar S, Subramanian M.

Bioanalysis. 2017 Oct;9(19):1441-1450. doi: 10.4155/bio-2017-0143. Epub 2017 Oct 21.

PMID:
29056076
6.

LC-MS determination of triazolam and its hydroxy metabolites in mouse dried blood spots: application to transgenic mouse pharmacokinetic studies.

Kole P, Rao A, Kurawattimath V, Mandlekar S.

Bioanalysis. 2017 Jul;9(13):987-1000. doi: 10.4155/bio-2017-0067. Epub 2017 Jul 10.

PMID:
28692308
7.

Comparative Evaluation of Plasma Bile Acids, Dehydroepiandrosterone Sulfate, Hexadecanedioate, and Tetradecanedioate with Coproporphyrins I and III as Markers of OATP Inhibition in Healthy Subjects.

Shen H, Chen W, Drexler DM, Mandlekar S, Holenarsipur VK, Shields EE, Langish R, Sidik K, Gan J, Humphreys WG, Marathe P, Lai Y.

Drug Metab Dispos. 2017 Aug;45(8):908-919. doi: 10.1124/dmd.117.075531. Epub 2017 Jun 2.

PMID:
28576766
8.

Unmasking the Role of Uptake Transporters for Digoxin Uptake Across the Barriers of the Central Nervous System in Rat.

Taskar KS, Mariappan TT, Kurawattimath V, Singh Gautam S, Radhakrishna Mullapudi TV, Sridhar SK, Kallem RR, Marathe P, Mandlekar S.

J Cent Nerv Syst Dis. 2017 Mar 15;9:1179573517693596. doi: 10.1177/1179573517693596. eCollection 2017.

9.

Selective IKur Inhibitors for the Potential Treatment of Atrial Fibrillation: Optimization of the Phenyl Quinazoline Series Leading to Clinical Candidate 5-[5-Phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl]pyridine-3-sulfonamide.

Gunaga P, Lloyd J, Mummadi S, Banerjee A, Dhondi NK, Hennan J, Subray V, Jayaram R, Rajugowda N, Umamaheshwar Reddy K, Kumaraguru D, Mandal U, Beldona D, Adisechen AK, Yadav N, Warrier J, Johnson JA, Sale H, Putlur SP, Saxena A, Chimalakonda A, Mandlekar S, Conder M, Xing D, Gupta AK, Gupta A, Rampulla R, Mathur A, Levesque P, Wexler RR, Finlay HJ.

J Med Chem. 2017 May 11;60(9):3795-3803. doi: 10.1021/acs.jmedchem.6b01889. Epub 2017 Apr 28.

PMID:
28418664
10.

Coproporphyrin-I: A Fluorescent, Endogenous Optimal Probe Substrate for ABCC2 (MRP2) Suitable for Vesicle-Based MRP2 Inhibition Assay.

Gilibili RR, Chatterjee S, Bagul P, Mosure KW, Murali BV, Mariappan TT, Mandlekar S, Lai Y.

Drug Metab Dispos. 2017 Jun;45(6):604-611. doi: 10.1124/dmd.116.074740. Epub 2017 Mar 21.

PMID:
28325716
11.

Metabolite Identification, Reaction Phenotyping, and Retrospective Drug-Drug Interaction Predictions of 17-Deacetylnorgestimate, the Active Component of the Oral Contraceptive Norgestimate.

Ahire D, Sinha S, Brock B, Iyer R, Mandlekar S, Subramanian M.

Drug Metab Dispos. 2017 Jun;45(6):676-685. doi: 10.1124/dmd.116.073940. Epub 2017 Mar 10.

PMID:
28283499
12.

Single jugular vein cannulated rats may not be suitable for intravenous pharmacokinetic screening of high logP compounds.

Gaud N, Kumar A, Matta M, Kole P, Sridhar S, Mandlekar S, Holenarsipur VK.

Eur J Pharm Sci. 2017 Mar 1;99:272-278. doi: 10.1016/j.ejps.2016.12.025. Epub 2016 Dec 26.

PMID:
28034694
13.

A Novel Liquid Chromatography Tandem Mass Spectrometry Method for the Estimation of Bilirubin Glucuronides and its Application to In Vitro Enzyme Assays.

Putluru SP, Matta MK, Ahire D, Subramanian M, Sinz M, Mandlekar S.

Drug Metab Lett. 2017;10(4):264-269. doi: 10.2174/1872312810666161124143522.

PMID:
27908259
14.

Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor.

Finlay HJ, Johnson JA, Lloyd JL, Jiang J, Neels J, Gunaga P, Banerjee A, Dhondi N, Chimalakonda A, Mandlekar S, Conder ML, Sale H, Xing D, Levesque P, Wexler RR.

ACS Med Chem Lett. 2016 Jun 9;7(9):831-4. doi: 10.1021/acsmedchemlett.6b00117. eCollection 2016 Sep 8.

15.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.

Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF.

J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13.

16.

Coproporphyrins in Plasma and Urine Can Be Appropriate Clinical Biomarkers to Recapitulate Drug-Drug Interactions Mediated by Organic Anion Transporting Polypeptide Inhibition.

Lai Y, Mandlekar S, Shen H, Holenarsipur VK, Langish R, Rajanna P, Murugesan S, Gaud N, Selvam S, Date O, Cheng Y, Shipkova P, Dai J, Humphreys WG, Marathe P.

J Pharmacol Exp Ther. 2016 Sep;358(3):397-404. doi: 10.1124/jpet.116.234914. Epub 2016 Jun 17.

PMID:
27317801
17.

Absolute quantification of imipramine and its metabolites in vivo utilizing calibrators from radiolabeled in vitro incubations.

Bhutani P, Shah D, Varkhede N, Mandlekar S, Chacko S, Subramanian M.

Bioanalysis. 2016 Feb;8(4):297-309. doi: 10.4155/bio.15.259. Epub 2016 Feb 5.

PMID:
26847656
18.

Diclofenac and Its Acyl Glucuronide: Determination of In Vivo Exposure in Human Subjects and Characterization as Human Drug Transporter Substrates In Vitro.

Zhang Y, Han YH, Putluru SP, Matta MK, Kole P, Mandlekar S, Furlong MT, Liu T, Iyer RA, Marathe P, Yang Z, Lai Y, Rodrigues AD.

Drug Metab Dispos. 2016 Mar;44(3):320-8. doi: 10.1124/dmd.115.066944. Epub 2015 Dec 29.

PMID:
26714763
19.

Prediction of pH dependent absorption using in vitro, in silico, and in vivo rat models: Early liability assessment during lead optimization.

Saxena A, Shah D, Padmanabhan S, Gautam SS, Chowan GS, Mandlekar S, Desikan S.

Eur J Pharm Sci. 2015 Aug 30;76:173-80. doi: 10.1016/j.ejps.2015.05.006. Epub 2015 May 8.

PMID:
25960252
20.

Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.

Carter PH, Brown GD, Cherney RJ, Batt DG, Chen J, Clark CM, Cvijic ME, Duncia JV, Ko SS, Mandlekar S, Mo R, Nelson DJ, Pang J, Rose AV, Santella JB 3rd, Tebben AJ, Traeger SC, Xu S, Zhao Q, Barrish JC.

ACS Med Chem Lett. 2015 Mar 4;6(4):439-44. doi: 10.1021/ml500505q. eCollection 2015 Apr 9.

21.

Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: in vitro, in situ intestinal perfusion and portal vein cannulation models.

Holenarsipur VK, Gaud N, Sinha J, Sivaprasad S, Bhutani P, Subramanian M, Singh SP, Arla R, Paruchury S, Sharma T, Marathe P, Mandlekar S.

Biopharm Drug Dispos. 2015 Sep;36(6):385-397. doi: 10.1002/bdd.1950. Epub 2015 May 4.

PMID:
25832562
22.

A systematic evaluation of solubility enhancing excipients to enable the generation of permeability data for poorly soluble compounds in Caco-2 model.

Shah D, Paruchury S, Matta M, Chowan G, Subramanian M, Saxena A, Soars MG, Herbst J, Haskell R, Marathe P, Mandlekar S.

Drug Metab Lett. 2014;8(2):109-18.

PMID:
25429513
23.

Electrophilicity of pyridazine-3-carbonitrile, pyrimidine-2-carbonitrile, and pyridine-carbonitrile derivatives: a chemical model to describe the formation of thiazoline derivatives in human liver microsomes.

Sinha S, Ahire D, Wagh S, Mullick D, Sistla R, Selvakumar K, Cortes JC, Putlur SP, Mandlekar S, Johnson BM.

Chem Res Toxicol. 2014 Dec 15;27(12):2052-61. doi: 10.1021/tx500256j. Epub 2014 Dec 2.

PMID:
25372409
24.

Role of hepatic blood flow and metabolism in the pharmacokinetics of ten drugs in lean, aged and obese rats.

Subramanian M, Kurawattimath V, Pocha K, Freeden C, Rao I, Mariappan TT, Marathe PH, Vikramadithyan RK, Abraham P, Kulkarni CP, Katnapally P, Nutakki R, Paruchury S, Bhutani P, Mandlekar S.

Xenobiotica. 2014 Dec;44(12):1108-16. doi: 10.3109/00498254.2014.932470. Epub 2014 Jun 20.

PMID:
24947446
25.

Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Mo R, Yang MG, Xiao Z, Zhao Q, Mandlekar S, Cvijic ME, Charo IF, Barrish JC, Decicco CP, Carter PH.

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1843-5. doi: 10.1016/j.bmcl.2014.02.013. Epub 2014 Feb 21.

26.

Estimation of the unbound brain concentration of P-glycoprotein substrates or nonsubstrates by a serial cerebrospinal fluid sampling technique in rats.

Mariappan TT, Kurawattimath V, Gautam SS, Kulkarni CP, Kallem R, Taskar KS, Marathe PH, Mandlekar S.

Mol Pharm. 2014 Feb 3;11(2):477-85. doi: 10.1021/mp400436d. Epub 2014 Jan 9.

PMID:
24380373
27.

Expression and characterization of cynomolgus monkey cytochrome CYP3A4 in a novel human embryonic kidney cell-based mammalian system.

Selvakumar S, Bhutani P, Ghosh K, Krishnamurthy P, Kallipatti S, Selvam S, Ramarao M, Mandlekar S, Sinz MW, Rodrigues AD, Subramanian M.

Drug Metab Dispos. 2014 Mar;42(3):369-76. doi: 10.1124/dmd.113.055491. Epub 2013 Dec 13.

PMID:
24335510
28.

Practical and economical implementation of online H/D exchange in LC-MS.

Shah RP, Garg A, Putlur SP, Wagh S, Kumar V, Rao V, Singh S, Mandlekar S, Desikan S.

Anal Chem. 2013 Nov 19;85(22):10904-12. doi: 10.1021/ac402339s. Epub 2013 Nov 8.

PMID:
24117319
29.

Characterization of recombinantly expressed rat and monkey intestinal alkaline phosphatases: in vitro studies and in vivo correlations.

Subramanian M, Paruchury S, Singh Gautam S, Pratap Singh S, Arla R, Pahwa S, Jana S, Katnapally P, Yoganand V, Lakshmaiah B, Mazumder Tagore D, Ghosh K, Marathe P, Mandlekar S.

Drug Metab Dispos. 2013 Jul;41(7):1425-32. doi: 10.1124/dmd.113.051987. Epub 2013 Apr 30.

PMID:
23633529
30.

Insight into tissue unbound concentration: utility in drug discovery and development.

Mariappan TT, Mandlekar S, Marathe P.

Curr Drug Metab. 2013 Mar;14(3):324-40. Review.

PMID:
23167621
31.

Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis.

Cavallaro CL, Briceno S, Chen J, Cvijic ME, Davies P, Hynes J Jr, Liu RQ, Mandlekar S, Rose AV, Tebben AJ, Van Kirk K, Watson A, Wu H, Yang G, Carter PH.

J Med Chem. 2012 Nov 26;55(22):9643-53. doi: 10.1021/jm300896d. Epub 2012 Oct 17.

PMID:
23075267
32.

A simplified protocol employing elacridar in rodents: a screening model in drug discovery to assess P-gp mediated efflux at the blood brain barrier.

Kallem R, Kulkarni CP, Patel D, Thakur M, Sinz M, Singh SP, Mahammad SS, Mandlekar S.

Drug Metab Lett. 2012 Jun 1;6(2):134-44.

PMID:
23061481
33.

Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone.

Carter PH, Brown GD, King SR, Voss ME, Tebben AJ, Cherney RJ, Mandlekar S, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Decicco CP.

Bioorg Med Chem Lett. 2012 May 1;22(9):3311-6. doi: 10.1016/j.bmcl.2012.03.007. Epub 2012 Mar 10.

PMID:
22475558
34.

A modified serial blood sampling technique and utility of dried-blood spot technique in estimation of blood concentration: application in mouse pharmacokinetics.

Kurawattimath V, Pocha K, Mariappan TT, Trivedi RK, Mandlekar S.

Eur J Drug Metab Pharmacokinet. 2012 Mar;37(1):23-30. doi: 10.1007/s13318-011-0066-5. Epub 2011 Sep 25. Erratum in: Eur J Drug Metab Pharmacokinet. 2011 Dec;36(4):263.

PMID:
21948266
35.

Prodrug design to improve pharmacokinetic and drug delivery properties: challenges to the discovery scientists.

Jana S, Mandlekar S, Marathe P.

Curr Med Chem. 2010;17(32):3874-908. Review.

PMID:
20858214
36.

gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Mo R, Meyer DT, Voss ME, Yang MG, Santella JB 3rd, Duncia JV, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Mandlekar S, Cvijic ME, Barrish JC, Decicco CP, Carter PH.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2425-30. doi: 10.1016/j.bmcl.2010.03.035. Epub 2010 Mar 10.

PMID:
20346664
37.

Role of phase II drug metabolizing enzymes in cancer chemoprevention.

Jana S, Mandlekar S.

Curr Drug Metab. 2009 Jul;10(6):595-616. Epub 2009 Jul 15. Review.

PMID:
19702535
38.

Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.

Cherney RJ, Mo R, Meyer DT, Nelson DJ, Lo YC, Yang G, Scherle PA, Mandlekar S, Wasserman ZR, Jezak H, Solomon KA, Tebben AJ, Carter PH, Decicco CP.

J Med Chem. 2008 Feb 28;51(4):721-4. doi: 10.1021/jm701488f. Epub 2008 Jan 31.

PMID:
18232650
39.

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.

Santella JB 3rd, Gardner DS, Yao W, Shi C, Reddy P, Tebben AJ, DeLucca GV, Wacker DA, Watson PS, Welch PK, Wadman EA, Davies P, Solomon KA, Graden DM, Yeleswaram S, Mandlekar S, Kariv I, Decicco CP, Ko SS, Carter PH, Duncia JV.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):576-85. Epub 2007 Nov 22.

PMID:
18096386
40.

Development of an in vivo rat screen model to predict pharmacokinetic interactions of CYP3A4 substrates.

Mandlekar SV, Rose AV, Cornelius G, Sleczka B, Caporuscio C, Wang J, Marathe PH.

Xenobiotica. 2007 Sep;37(9):923-42.

PMID:
17896322
41.
42.

Selective inhibition of eosinophil influx into the lung by small molecule CC chemokine receptor 3 antagonists in mouse models of allergic inflammation.

Das AM, Vaddi KG, Solomon KA, Krauthauser C, Jiang X, McIntyre KW, Yang XX, Wadman E, Welch P, Covington M, Graden D, Yeleswaram K, Trzaskos JM, Newton RC, Mandlekar S, Ko SS, Carter PH, Davies P.

J Pharmacol Exp Ther. 2006 Jul;318(1):411-7. Epub 2006 Apr 13.

PMID:
16614169
43.

Matrix metalloproteinase-activated doxorubicin prodrugs inhibit HT1080 xenograft growth better than doxorubicin with less toxicity.

Albright CF, Graciani N, Han W, Yue E, Stein R, Lai Z, Diamond M, Dowling R, Grimminger L, Zhang SY, Behrens D, Musselman A, Bruckner R, Zhang M, Jiang X, Hu D, Higley A, Dimeo S, Rafalski M, Mandlekar S, Car B, Yeleswaram S, Stern A, Copeland RA, Combs A, Seitz SP, Trainor GL, Taub R, Huang P, Oliff A.

Mol Cancer Ther. 2005 May;4(5):751-60.

44.

Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.

Cherney RJ, Duan JJ, Voss ME, Chen L, Wang L, Meyer DT, Wasserman ZR, Hardman KD, Liu RQ, Covington MB, Qian M, Mandlekar S, Christ DD, Trzaskos JM, Newton RC, Magolda RL, Wexler RR, Decicco CP.

J Med Chem. 2003 May 8;46(10):1811-23.

PMID:
12723945
46.

Induction of xenobiotic enzymes by the MAP kinase pathway and the antioxidant or electrophile response element (ARE/EpRE).

Kong AN, Owuor E, Yu R, Hebbar V, Chen C, Hu R, Mandlekar S.

Drug Metab Rev. 2001 Aug-Nov;33(3-4):255-71. Review.

PMID:
11768769
47.

Mechanisms of tamoxifen-induced apoptosis.

Mandlekar S, Kong AN.

Apoptosis. 2001 Dec;6(6):469-77. Review.

PMID:
11595837
48.

Signal transduction events elicited by cancer prevention compounds.

Kong AN, Yu R, Hebbar V, Chen C, Owuor E, Hu R, Ee R, Mandlekar S.

Mutat Res. 2001 Sep 1;480-481:231-41. Review.

PMID:
11506817
49.

Resveratrol inhibits phorbol ester and UV-induced activator protein 1 activation by interfering with mitogen-activated protein kinase pathways.

Yu R, Hebbar V, Kim DW, Mandlekar S, Pezzuto JM, Kong AN.

Mol Pharmacol. 2001 Jul;60(1):217-24.

PMID:
11408617

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