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Items: 1 to 50 of 60

1.

In vivo pharmacokinetic/pharmacodynamic targets of levonadifloxacin against Staphylococcus aureus in a neutropenic murine lung infection model.

Bhagwat SS, Periasamy H, Takalkar SS, Chavan R, Tayde P, Kulkarni A, Satav J, Zope V, Patel M.

Antimicrob Agents Chemother. 2019 Jun 17. pii: AAC.00909-19. doi: 10.1128/AAC.00909-19. [Epub ahead of print]

PMID:
31208999
2.

The Novel β-Lactam Enhancer Zidebactam Augments the In Vivo Pharmacodynamic Activity of Cefepime in a Neutropenic Mouse Lung Acinetobacter baumannii Infection Model.

Bhagwat SS, Periasamy H, Takalkar SS, Palwe SR, Khande HN, Patel MV.

Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02146-18. doi: 10.1128/AAC.02146-18. Print 2019 Apr.

PMID:
30670419
3.

A Sensitive Assay for Proteases in Bioaerosol Samples: Characterization and Quantification of Airborne Proteases in Salmon Industry Work Environments.

Bang BE, Malla N, Bhagwat SS, Aasmoe L, Winberg JO.

Ann Work Expo Health. 2018 Oct 15;62(8):942-952. doi: 10.1093/annweh/wxy050.

PMID:
29947734
4.

Strategic Approaches to Overcome Resistance against Gram-Negative Pathogens Using β-Lactamase Inhibitors and β-Lactam Enhancers: Activity of Three Novel Diazabicyclooctanes WCK 5153, Zidebactam (WCK 5107), and WCK 4234.

Papp-Wallace KM, Nguyen NQ, Jacobs MR, Bethel CR, Barnes MD, Kumar V, Bajaksouzian S, Rudin SD, Rather PN, Bhavsar S, Ravikumar T, Deshpande PK, Patil V, Yeole R, Bhagwat SS, Patel MV, van den Akker F, Bonomo RA.

J Med Chem. 2018 May 10;61(9):4067-4086. doi: 10.1021/acs.jmedchem.8b00091. Epub 2018 Apr 20.

5.

New Antimicrobial Agents  …  but No Susceptibility Tests!

Ambler JE, Krause KM, Steenbergen JN, Scangarella-Oman NE, Miller LA, Bhagwat SS, Serio AW, Chesnel L, Mahoney NM, Motyl MR, Critchley IA, Iaconis JP, Stone GG, Alder J, Xerri L, McCurdy SP, van Veenhuyzen DF, Grossman T, Echols RM, Williams G, Bradford PA.

Clin Infect Dis. 2016 Dec 1;63(11):1530-1531. Epub 2016 Aug 31. No abstract available.

PMID:
27581762
6.

Purification of serratiopeptidase from Serratia marcescens NRRL B 23112 using ultrasound assisted three phase partitioning.

Pakhale SV, Bhagwat SS.

Ultrason Sonochem. 2016 Jul;31:532-8. doi: 10.1016/j.ultsonch.2016.01.037. Epub 2016 Jan 30.

PMID:
26964980
7.

Mixed exposure to bacterial lipopolysaccharide and seafood proteases augments inflammatory signalling in an airway epithelial cell model (A549).

Bhagwat SS, Larsen AK, Seternes OM, Bang BE.

Toxicol Ind Health. 2016 Nov;32(11):1866-1874. doi: 10.1177/0748233715590914. Epub 2016 Jul 9.

PMID:
26149191
8.

Total polyphenolic contents and in vitro antioxidant properties of eight Sida species from Western Ghats, India.

Subramanya MD, Pai SR, Upadhya V, Ankad GM, Bhagwat SS, Hegde HV.

J Ayurveda Integr Med. 2015 Jan-Mar;6(1):24-8. doi: 10.4103/0975-9476.146544.

9.

Salmon and king crab trypsin stimulate interleukin-8 and matrix metalloproteinases via protease-activated receptor-2 in the skin keratinocytic HaCaT cell line.

Bhagwat SS, Larsen AK, Winberg JO, Seternes OM, Bang BE.

Food Chem Toxicol. 2014 Jul;69:303-11. doi: 10.1016/j.fct.2014.04.030. Epub 2014 Apr 30.

PMID:
24795235
10.

CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.

James J, Ruggeri B, Armstrong RC, Rowbottom MW, Jones-Bolin S, Gunawardane RN, Dobrzanski P, Gardner MF, Zhao H, Cramer MD, Hunter K, Nepomuceno RR, Cheng M, Gitnick D, Yazdanian M, Insko DE, Ator MA, Apuy JL, Faraoni R, Dorsey BD, Williams M, Bhagwat SS, Holladay MW.

Mol Cancer Ther. 2012 Apr;11(4):930-41. doi: 10.1158/1535-7163.MCT-11-0645. Epub 2012 Feb 7.

11.

4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.

Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14.

PMID:
21807507
12.

Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.

Abraham S, Hadd MJ, Tran L, Vickers T, Sindac J, Milanov ZV, Holladay MW, Bhagwat SS, Hua H, Ford Pulido JM, Cramer MD, Gitnick D, James J, Dao A, Belli B, Armstrong RC, Treiber DK, Liu G.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5296-300. doi: 10.1016/j.bmcl.2011.07.027. Epub 2011 Jul 14.

PMID:
21802948
13.

Kinase inhibitor selectivity.

Bhagwat SS.

Curr Opin Investig Drugs. 2009 Dec;10(12):1266-8. No abstract available.

PMID:
19943198
14.

Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.

Chao Q, Sprankle KG, Grotzfeld RM, Lai AG, Carter TA, Velasco AM, Gunawardane RN, Cramer MD, Gardner MF, James J, Zarrinkar PP, Patel HK, Bhagwat SS.

J Med Chem. 2009 Dec 10;52(23):7808-16. doi: 10.1021/jm9007533.

PMID:
19754199
15.

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q, Sprankle KG, Patel HK, Levis M, Armstrong RC, James J, Bhagwat SS.

Blood. 2009 Oct 1;114(14):2984-92. doi: 10.1182/blood-2009-05-222034. Epub 2009 Aug 4.

16.

Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.

Patel HK, Grotzfeld RM, Lai AG, Mehta SA, Milanov ZV, Chao Q, Sprankle KG, Carter TA, Velasco AM, Fabian MA, James J, Treiber DK, Lockhart DJ, Zarrinkar PP, Bhagwat SS.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5182-5. doi: 10.1016/j.bmcl.2009.07.024. Epub 2009 Jul 9.

PMID:
19646870
17.

In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.

Bhagwat SS, McGhee P, Kosowska-Shick K, Patel MV, Appelbaum PC.

Antimicrob Agents Chemother. 2009 Feb;53(2):811-3. doi: 10.1128/AAC.01150-08. Epub 2008 Nov 24. Erratum in: Antimicrob Agents Chemother. 2009 Mar;53(3):1298.

18.

Substituted 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones as novel anti-MRSA agents: synthesis, SAR, and in-vitro assessment.

Diwakar SD, Bhagwat SS, Shingare MS, Gill CH.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4678-81. doi: 10.1016/j.bmcl.2008.07.007. Epub 2008 Jul 9.

PMID:
18650090
19.

Kinase inhibitors for the treatment of inflammatory and autoimmune disorders.

Bhagwat SS.

Purinergic Signal. 2009 Mar;5(1):107-15. doi: 10.1007/s11302-008-9117-z. Epub 2008 Jun 21.

20.

4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.

Matulenko MA, Paight ES, Frey RR, Gomtsyan A, DiDomenico S Jr, Jiang M, Lee CH, Stewart AO, Yu H, Kohlhaas KL, Alexander KM, McGaraughty S, Mikusa J, Marsh KC, Muchmore SW, Jakob CL, Kowaluk EA, Jarvis MF, Bhagwat SS.

Bioorg Med Chem. 2007 Feb 15;15(4):1586-605. Epub 2006 Dec 20.

PMID:
17197188
21.

Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.

Muchmore SW, Smith RA, Stewart AO, Cowart MD, Gomtsyan A, Matulenko MA, Yu H, Severin JM, Bhagwat SS, Lee CH, Kowaluk EA, Jarvis MF, Jakob CL.

J Med Chem. 2006 Nov 16;49(23):6726-31.

PMID:
17154503
23.

Chlorination of aromatic compounds in micellar media: regioselectivity.

Samant BS, Saraf YP, Bhagwat SS.

J Colloid Interface Sci. 2006 Oct 1;302(1):207-13. Epub 2006 Jun 13.

PMID:
16806254
24.

Synthesis of new series of 1-Aryl-1,4-dihydro-4-oxo-6-methyl pyridazine-3-carboxylic acid as potential antibacterial agents.

Nagawade RR, Khanna VV, Bhagwat SS, Shinde DB.

Eur J Med Chem. 2005 Dec;40(12):1325-30. Epub 2005 Aug 29.

PMID:
16126308
25.

Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3-d]pyrimidines as adenosine kinase inhibitors.

Perner RJ, Lee CH, Jiang M, Gu YG, Didomenico S, Bayburt EK, Alexander KM, Kohlhaas KL, Jarvis MF, Kowaluk EL, Bhagwat SS.

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2803-7. Epub 2005 Apr 25.

PMID:
15911258
26.

5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine: structure-activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors.

Matulenko MA, Lee CH, Jiang M, Frey RR, Cowart MD, Bayburt EK, Didomenico S, Gfesser GA, Gomtsyan A, Zheng GZ, McKie JA, Stewart AO, Yu H, Kohlhaas KL, Alexander KM, McGaraughty S, Wismer CT, Mikusa J, Marsh KC, Snyder RD, Diehl MS, Kowaluk EA, Jarvis MF, Bhagwat SS.

Bioorg Med Chem. 2005 Jun 1;13(11):3705-20.

PMID:
15863000
27.

Effect of Lomodex-MgSO(4) in the prevention of reperfusion injury following unilateral testicular torsion: an experimental study in rats.

Adivarekar PK, Bhagwat SS, Raghavan V, Bandivdekar AH.

Pediatr Surg Int. 2005 Mar;21(3):184-90. Epub 2005 Feb 15.

PMID:
15711960
28.

Antistaphylococcal activity of WCK 771, a tricyclic fluoroquinolone, in animal infection models.

Patel MV, De Souza NJ, Gupte SV, Jafri MA, Bhagwat SS, Chugh Y, Khorakiwala HF, Jacobs MR, Appelbaum PC.

Antimicrob Agents Chemother. 2004 Dec;48(12):4754-61.

29.

In vitro activity of the new quinolone WCK 771 against staphylococci.

Jacobs MR, Bajaksouzian S, Windau A, Appelbaum PC, Patel MV, Gupte SV, Bhagwat SS, De Souza NJ, Khorakiwala HF.

Antimicrob Agents Chemother. 2004 Sep;48(9):3338-42.

30.

Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors.

Gomtsyan A, Didomenico S, Lee CH, Stewart AO, Bhagwat SS, Kowaluk EA, Jarvis MF.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4165-8.

PMID:
15261263
31.

Lead identification of a potent benzopyranone selective estrogen receptor modulator.

McKie JA, Bhagwat SS, Brady H, Doubleday M, Gayo L, Hickman M, Jalluri RK, Khammungkhune S, Kois A, Mortensen D, Richard N, Sapienza J, Shevlin G, Stein B, Sutherland M.

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3407-10.

PMID:
15177442
32.

5,6,7-trisubstituted 4-aminopyrido[2,3-d]pyrimidines as novel inhibitors of adenosine kinase.

Perner RJ, Gu YG, Lee CH, Bayburt EK, McKie J, Alexander KM, Kohlhaas KL, Wismer CT, Mikusa J, Jarvis MF, Kowaluk EA, Bhagwat SS.

J Med Chem. 2003 Nov 20;46(24):5249-57.

PMID:
14613327
33.

Effects of SP500263, a novel selective estrogen receptor modulator, on bone, uterus, and serum cholesterol in the ovariectomized rat.

Sutherland MK, Brady H, Gayo-Fung LM, Leisten J, Lipps SG, McKie JA, O'Leary E, Patnaik N, Anderson DW, Bhagwat SS, Stein B.

Calcif Tissue Int. 2003 Jun;72(6):710-6.

PMID:
14563000
34.

Synthesis and structure-activity relationships of 5-heteroatom-substituted pyridopyrimidines as adenosine kinase inhibitors.

Gfesser GA, Bayburt EK, Cowart M, DiDomenico S, Gomtsyan A, Lee CH, Stewart AO, Jarvis MF, Kowaluk EA, Bhagwat SS.

Eur J Med Chem. 2003 Mar;38(3):245-52.

PMID:
12667691
35.

Design, synthesis, and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors.

Gomtsyan A, Didomenico S, Lee CH, Matulenko MA, Kim K, Kowaluk EA, Wismer CT, Mikusa J, Yu H, Kohlhaas K, Jarvis MF, Bhagwat SS.

J Med Chem. 2002 Aug 15;45(17):3639-48.

PMID:
12166937
36.

Effects of SP500263, a novel, potent antiestrogen, on breast cancer cells and in xenograft models.

Brady H, Desai S, Gayo-Fung LM, Khammungkhune S, McKie JA, O'Leary E, Pascasio L, Sutherland MK, Anderson DW, Bhagwat SS, Stein B.

Cancer Res. 2002 Mar 1;62(5):1439-42.

37.

Differential response of estrogen receptors alpha and beta to SP500263, a novel potent selective estrogen receptor modulator.

Brady H, Doubleday M, Gayo-Fung LM, Hickman M, Khammungkhune S, Kois A, Lipps S, Pierce S, Richard N, Shevlin G, Sutherland MK, Anderson DW, Bhagwat SS, Stein B.

Mol Pharmacol. 2002 Mar;61(3):562-8.

PMID:
11854436
38.

SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase.

Bennett BL, Sasaki DT, Murray BW, O'Leary EC, Sakata ST, Xu W, Leisten JC, Motiwala A, Pierce S, Satoh Y, Bhagwat SS, Manning AM, Anderson DW.

Proc Natl Acad Sci U S A. 2001 Nov 20;98(24):13681-6.

39.

Synthesis and biological evaluation of clitocine analogues as adenosine kinase inhibitors.

Lee CH, Daanen JF, Jiang M, Yu H, Kohlhaas KL, Alexander K, Jarvis MF, Kowaluk EL, Bhagwat SS.

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2419-22.

PMID:
11549437
40.

Pyridopyrimidine analogues as novel adenosine kinase inhibitors.

Zheng GZ, Lee C, Pratt JK, Perner RJ, Jiang MQ, Gomtsyan A, Matulenko MA, Mao Y, Koenig JR, Kim KH, Muchmore S, Yu H, Kohlhaas K, Alexander KM, McGaraughty S, Chu KL, Wismer CT, Mikusa J, Jarvis MF, Marsh K, Kowaluk EA, Bhagwat SS, Stewart AO.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2071-4.

PMID:
11514141
41.

Discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido[2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor..

Lee CH, Jiang M, Cowart M, Gfesser G, Perner R, Kim KH, Gu YG, Williams M, Jarvis MF, Kowaluk EA, Stewart AO, Bhagwat SS.

J Med Chem. 2001 Jun 21;44(13):2133-8.

PMID:
11405650
42.

Anti-inflammatory effects of ABT-702, a novel non-nucleoside adenosine kinase inhibitor, in rat adjuvant arthritis.

Boyle DL, Kowaluk EA, Jarvis MF, Lee CH, Bhagwat SS, Williams M, Firestein GS.

J Pharmacol Exp Ther. 2001 Feb;296(2):495-500.

PMID:
11160636
43.

Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.

Cowart M, Lee CH, Gfesser GA, Bayburt EK, Bhagwat SS, Stewart AO, Yu H, Kohlhaas KL, McGaraughty S, Wismer CT, Mikusa J, Zhu C, Alexander KM, Jarvis MF, Kowaluk EA.

Bioorg Med Chem Lett. 2001 Jan 8;11(1):83-6.

PMID:
11140740
44.

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin- 3-yl)pyrido[2,3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties. II. In vivo characterization in the rat.

Kowaluk EA, Mikusa J, Wismer CT, Zhu CZ, Schweitzer E, Lynch JJ, Lee CH, Jiang M, Bhagwat SS, Gomtsyan A, McKie J, Cox BF, Polakowski J, Reinhart G, Williams M, Jarvis MF.

J Pharmacol Exp Ther. 2000 Dec;295(3):1165-74.

PMID:
11082454
46.

Gene-regulating protein kinases as important anti-inflammatory targets.

Bhagwat SS, Manning AM, Hoekstra MF, Lewis A.

Drug Discov Today. 1999 Oct;4(10):472-479.

PMID:
10481143
47.

Adenosine kinase inhibitors.

Kowaluk EA, Bhagwat SS, Jarvis MF.

Curr Pharm Des. 1998 Oct;4(5):403-16. Review.

PMID:
10197052
48.

Isolated jejunal varices.

Bhagwat SS, Borwankar SS, Ramadwar RH, Naik AS, Gajaree GI.

J Postgrad Med. 1995 Apr-Jun;41(2):43-4.

49.
50.

Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.

Bhagwat SS, Gude C, Boswell C, Contardo N, Cohen DS, Dotson R, Mathis J, Lee W, Furness P, Zoganas H.

J Med Chem. 1992 Nov 13;35(23):4373-83.

PMID:
1447738

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