Raghunath B. Bhosale

PEG mediated synthesis and pharmacological evaluation of some fluoro substituted pyrazoline derivatives as antiinflammatory and analgesic agents.

A new series of fluoro substituted pyrazoline derivatives 5a-g and 6a-g were synthesized in good to excellent yield from the corresponding pyrazole chalcones, 4a-g, by using polyethylene glycol-400 (PEG-400) as an alternative reaction medium. The newly synthesized compounds were characterized and screened for their in vivo antiinflammatory and analgesic activity. Compounds 5g and 6g were found to be more potent than standard drug Diclofenac and six other compounds 5b, 5c, 5f, 6b, 6c and 6f showed significant antiinflammatory activity as compared to standard drug. Compounds 5c, 5d, 5e, 5f, 6c, 6d, 6e and 6f showed significant analgesic activity as compared to standard drug Aspirin.

An improved procedure for synthesis of some new 1,3-diaryl-2-propen-1-ones using PEG-400 as a recyclable solvent and their antimicrobial evaluation

An improved procedure for synthesis of some new 1,3-diaryl-2-propen-1-ones using PEG-400 as a recyclable solvent and their antimicrobial evaluation A simple and convenient route is described for the synthesis of novel hetero 1,3-diaryl-2-propen-1-ones (chalcones) by using recyclable PEG-400 as an alternative reaction solvent. The reaction is clean with excellent yield, shorter reaction time and reduces the use of volatile organic compounds (VOCs). All the synthesized compounds were evaluated for their antimicrobial activities against several pathogenic representatives. Poboljšan postupak sinteze nekih novih 1,3-diaril-2-propen-1-ona koristeći PEG-400 kao reciklirajuće otapalo i njihovo antimikrobno vrednovanje Opisana je jednostavna i pogodna metoda sinteze novih hetero 1,3-diaril-2-propen-1-ona (kalkona) koristeći poli(etilenglikol) (PEG-400) kao alternativno otapalo. Reakcija je jednoznačna, a uporaba hlapljivih organskih otapala je smanjena. Iskorištenja na produktima su visoka, a reakcijska vremena kraća. Svi sintetizirani spojevi testirani su na antimikrobno djelovanje na nekoliko patogenih mikroorganizama.

PEG mediated synthesis and biological evaluation of asymmetrical pyrazole curcumin analogues as potential analgesic, anti-inflammatory and antioxidant agents.

The new series of asymmetrical pyrazole curcumin analogues 4a–g were synthesized by using polyethylene glycol (PEG‐400) as a green reaction medium and evaluated for their in vivo analgesic and in vitro antioxidant (H2O2, DPPH, Ferrous reducing power and Nitric oxide scavenging activity) and anti‐inflammatory activities. All the compounds synthesized 4a–g showed the potential to demonstrate analgesic activity as compared to the standard ibuprofen. Among the tested series, compounds 4e and 4b exhibited good hydrogen peroxide scavenging activity as compared to the standard butylated hydroxy toluene (BHT). Compounds 4b, 4d, 4f, and 4g showed good DPPH free radical scavenging activity. Compounds 4b, 4c, 4d, 4e and 4g showed excellent ferrous‐reducing power activity, whereas all the compounds showed better nitric oxide scavenging activity than standard ascorbic acid. Additionally, all the synthesized compounds were also screened for their in vitro anti‐inflammatory activity. Compounds 4b, 4d, 4f and 4g showed good anti‐inflammatory activity as compared to standard diclofenac sodium.

Multicomponent One-Pot Synthesis of Substituted Hantzsch Thiazole Derivatives Under Solvent Free Conditions

Thiazole derivatives were prepared by one-pot procedure by the reaction of α-haloketones, thiourea and substituted o-hydroxybenzaldehyde under environmentally solvent free conditions.

One-pot PEG-mediated syntheses of 2-(2-hydrazinyl) thiazole derivatives: novel route

ABSTRACT Thiazoles are important sulfur-containing molecules that are widely used in diverse fields such as pharmaceuticals, agrochemicals, and material sciences. This is the first report on the PEG-300-mediated one-pot synthesis of 2-(2-hydrazinyl) thiazole derivatives from ketones, thiosemicarbazide, and α-halo ketones. Here PEG-300 acts as a solvent as well as supporting catalyst. Formation of compounds was confirmed by IR, 1H NMR, 13C NMR, and mass spectroscopic studies. A series of 2-(2-hydrazinyl) Thiazole derivatives have been synthesized from substituted ketones, thiosemicarbazide & α-halo ketones using PEG-300 as a reaction medium via one-pot approach. GRAPHICAL ABSTRACT

Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors

1,3-oxazine nucleus and thiazolyl group features prominently in many biologically important natural products as well as bioactive molecules. A series of novel 2-thiazolyl substituted-2,3-dihydro-1H-naphtho [1,2-e][1,3]oxazine derivatives were designed and synthesized based on their structure-activity relationships (SARs) from 2-naphthol, substituted thiazolyl amines and formalin through ring closure by one-pot three component reaction. These derivatives were first evaluated for their inhibitory effect on HIV-1 Reverse Transcriptase (RT) enzyme activity. Out of 14 compounds, 4 showed potent inhibition of HIV-1 RT activity at significantly low concentration. Docking studies of these molecules revealed their high affinity binding to several amino acids of HIV-1 RT which are less sensitive to point mutations. Furthermore, anti-HIV activity of these molecules was analysed in a CD4+ T cell-line, which indicates that Therapeutic Index (TI) of some of these compounds is better than Zidovudine and Efavirenz, known HIV-1 RT inhibitors. Taken together, our studies report for the first time some novel naphthoxazine derivatives with significant TI, which is through inhibition of HIV-1 RT activity.