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1.
Chem Sci ; 14(42): 11809-11817, 2023 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-37920349

RESUMO

A novel synthesis of aryl-substituted, enantioenriched fulvenes from an oxidative Heck cascade and rearrangement of a carboxy-substituted spiro[4.4]nonatriene is disclosed. Mechanistic investigations with density functional theory (DFT) calculations and empirical results support the net transformation occurring through a novel Pd(ii)-mediated 1,5-vinyl shift from a vinyl-palladium intermediate that terminates with protodepalladation. This spiro-to-fused bicycle conversion tolerates a range of electron-rich and deficient arylboronic acids to give a range of mono- and diaryl substituted annulated fulvenes in moderate to good yields and enantiomeric ratios. Overall, this work connects two classes of molecules with a rich history in physical organic chemistry.

2.
Anticancer Agents Med Chem ; 18(1): 38-45, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-28003000

RESUMO

BACKGROUND: A number of benzimidazole derivatives such as benomyl and carbendazim have been known for their potential role as agricultural fungicides. Simultaneously carbendazim has also been found to inhibit proliferation of mammalian tumor cells specifically drug and multidrug resistant cell lines. OBJECTIVE: To understand the dual role of Carbendazim as a fungicide and an anticancer agent, the study has been planned referring to the earlier studies in literature. RESULTS: Studies carried out with fungal and mammalian cells have highlighted the potential role of carbendazim in inhibiting proliferation of cells, thereby exhibiting therapeutic implications against cancer. Because of its promising preclinical antitumor activity, Carbendazim had undergone phase I clinical trials and is under further clinical investigations for the treatment of cancer. A number of theoretical interactions have been pinpointed. There are many anticancer drugs in the market, but their usefulness is limited because of drug resistance in a significant proportion of patients. The hunger for newer drugs drives anticancer drug discovery research on a global platform and requires innovations to ensure a sustainable pipeline of lead compounds. CONCLUSION: Current review highlights the dual role of carbendazim as a fungicide and an anticancer agent. Further, the harmful effects of carbendazim and emphasis upon the need for more pharmacokinetic studies and pharmacovigilance data to ascertain its clinical significance, have also been discussed.


Assuntos
Antineoplásicos/farmacologia , Benzimidazóis/farmacologia , Carbamatos/farmacologia , Fungicidas Industriais/farmacologia , Neoplasias/tratamento farmacológico , Animais , Antineoplásicos/química , Benzimidazóis/química , Carbamatos/química , Proliferação de Células/efeitos dos fármacos , Fungicidas Industriais/química , Humanos , Neoplasias/patologia
3.
Surg Endosc ; 28(11): 3059-67, 2014 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24879143

RESUMO

OBJECTIVE: Laparoscopic cholecystectomy (LC), a gold standard procedure can be done without energized dissection (ED). We did a randomized study for the outcomes of LC done with ED or without ED, i.e., with cold dissection (CD). METHODS AND PROCEDURES: At a tertiary level institution, open-ended prospective-randomized control study was conducted between September 2008 and June 2013. Consecutive, unselected, consenting candidates for LC were enrolled following standard ethics, informed consent, anesthesia, and clinical pathway protocol. They were allocated to control group (LC with ED) or study group (LC with CD, as per our published technique with the option for rescue ED). The study points were based upon Clavien-Dindo grading of postoperative complications. They were either, peri-operative events potentially affecting, hospital stay (Grade I) or Grade II-V, e.g., peri-operative hemodynamic instability, needing intervention/blood transfusion, injury to biliary ducts/hollow viscous, postoperative biliary leak, postoperative re-intervention, re-hospitalization, mortality, and any adverse event during a 90-day follow-up period. The data were prospectively collected in an integrated "hospital information system" that could be retrieved only by independent external coordinators. RESULTS: Demographics, co-morbidities, and gallbladder inflammation profile of the control group (n = 361) and study group (n = 384) were comparable. There was no rescue ED usage in the study group. Hospital stay (Grade I adverse outcome dependent) was longer, i.e., 1.6 ± 1.03 in the control versus 1.35 ± 1.2 days in the study group (p < 0.001). Grade II-IV complications were significantly more (p < 0.009) in control group. There was one common bile duct (CBD) injury in each group. The index bilio-enteric anastomosis for CBD injury in control group failed and needed a revision with multiple interventions. There was one grade V adverse outcome, i.e., mortality in the control group. CONCLUSION: Avoiding the use of ED in LC is associated with better outcomes.


Assuntos
Colecistectomia Laparoscópica/métodos , Dissecação/métodos , Colecistite/cirurgia , Ducto Colédoco/lesões , Feminino , Humanos , Complicações Intraoperatórias/epidemiologia , Tempo de Internação , Complicações Pós-Operatórias/etiologia , Período Pós-Operatório , Estudos Prospectivos , Terapia por Ultrassom
5.
Recent Pat Biotechnol ; 7(3): 172-8, 2013 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-24182324

RESUMO

Bacteriocins produced by lactic acid bacteria are of keen interest to the food industry for their bio-preservative potential and antimicrobial properties. The increasing demand for high quality 'safe' foods which are not extensively processed has created a niche for natural food preservatives. The bacteriocins (produced by bacteria) derived their name after the genera that produce them, hence bacteriocins produced by genus Pediococcus are known as Pediocin. Pediocins are antimicrobial peptides which show a strong activity against food spoilage and pathogenic bacteria, also are thermostable in nature as well as stable over a wide range of pH. Pediocin produced by Pediococcus acidilactici, has been generally recognized as safe (GRAS). The current review summarizes about the progress made on the Pediocin research from patent perspective along with the immense potential of these Pediococcus derived bacteriocins not only as antimicrobial, biopreservative and probiotic agents but also for the treatment of cancer, body odors and other health promoting actions. The relevant patents have been listed and briefly analyzed to upgrade and benefit food industries by prolonging the shelf life of various products.


Assuntos
Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Bacteriocinas/química , Bacteriocinas/farmacologia , Conservantes de Alimentos/química , Indústria Alimentícia , Patentes como Assunto , Pediococcus/metabolismo
6.
Indian J Surg ; 74(3): 234-41, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-23730050

RESUMO

Progress in surgical practice has paralleled the civilizational evolution. Surgery has progressed from being the last resort in saving life to being form and function preserver. Post-renaissance Industrial age gave an impetus to this march of surgery. The currently on going digital technological revolution has further catalysed this march. Having achieved the stabilized and acceptable clinical outcomes, the surgeon has embarked on a journey of improving patient reported outcomes (PRO). Improvement in PROs with the advent of laparoscopic surgery with the attendant emphasis on minimising invasion has led to debates about invasion being just parietal or holistic in physiological sense. There is a concern that parietal invasiveness shouldn't be a trade-off for compromised clinical outcomes. Single Incision Laparoscopic Surgery (SILS) in its current avatar with current instrumentation seems to be an enthusiastic bandwagon rolling on with the cosmetic benefits acting as veil to hide the potential clinical concerns. History of surgical innovations is riddled with tales of vindictiveness and vicissitude. Lest the same fate befalls SILS we would do better to examine the SILS bandwagon in its current form till the emerging technologies address the current concerns.

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