Diketo Analogues and Their Significance

Diketo Analogues and Their SignificanceINTRODUCTION healthful chemistry is the tell apart of science, which has remarkable value for subtraction of novel do drugss with intense therapeutic activity. It concerns with discovery, teaching, recognition and interpretation of mode of action of biologically busy compounds at molecular level.The molecular biological revolution and progressive mapping of human genome engender created a refreshful biochemical and biostructural world order.1These developments have provided spick-and-span challenges and opportunities for drug research in general and drug name in particular. Pure organic compounds, natural or synthetic products argon the headman source of agents for the cure, the mitigation or the prevention of disease today. The major objectives of the medicative chemists ar transformation of pathobiochemical and physiological data into a chemical lyric poem with the aim of designing molecules interacting specifically with the dera iled or degenerating processes in the diseased organisms.The development of chemotherapy during past 60 years constitute one of most of import therapeutic advances in history of medicine and disinfectant drugs are the sterling(prenominal) contribution of chip in century to therapeutics2. Potential therapeutic targets are beingness disclosed with increasing frequency and the exponential growth will overcompensate during the next decades.In this situation there is a need for fast and effective target validation and for accelerated lead discovery procedures. native chemists are increasingly directing their attention towards synthetic aspects of biomolecules and biologically active compounds, biosynthesized by plants and animals.Many of import biochemical compounds and drugs of natural origin subscribe heterocyclic ring structures. Many of them are employed in treatment of many infectious diseases due to their specific activity, but their use in treatment is attributed to the ir inherent toxicity to various pathogens.DIKETO ANALOGUES AND THEIR SIGNIFICANCEAntibacterialThe quinolones3 are well known synthetic antibacterial agents with di keto moiety whatsoever examples are Ciprofloxacin (1) Norfloxacin (2).Boteva4 et al synthesized some Halogen Substituted 4,5-dibenzoyl-1-phenyl-1H-pyrrole-2,3-dione derivatives (2-6) evaluated for Antibacterial Activity.Anti HIVThe firstly report of a class of compounds that inhibit HIV integrase appeared in 1992. Aurin tricarboxylic acids and derivatives were goaded to inhibit 3 processing of viral cDNA with moderate iC50 determine of 10-50micromolar.Thus the 1st pharmacophore with integrase inhibitory activity was determined i.e. aromatic go with multiple hydroxyl substituents positioned on same ring or present close together in a 3D space if ring stack on top of each other. Since then considerable bill of work has been carried out in developing electric potential inhibitors of integrase taking the preceding(p renominal) compounds as leads.Presently there is only one FDA approved drug used as integrase inhibitor i.e. Raltegravir or Isentress, (7) approved in 2007. Elvitegravir (8) is another potential integrase inhibitor which is in phase III clinical trial5.THIOPHENE ANALOGS AND THEIR SIGNIFICANCEThiophene (9) and its derivatives are an important class of heterocyclic compounds possessing broad biological activities, such as anti-inflammatory6, analgesic6, antioxidant7, antitubercular8, antidepressant9, sedative9, antiamoebic10, spoken analgesic11, antimetabolite12, and antineoplastic properties13.AntimicrobialsThiophene analogues have been known as antibacterials. In the year 2007 Stephane et al14 inform the synthesis and antibacterial activity of arylbenzothiophenes (10) and diarylthiophenes. (11)(10) (11)In the year 2010 Kavitha P N et al15 report the antimicrobial activity of 3- amino-2- mercapto-5,6,7,8-tetrahydrobenzo(b)thieno2,3-dpyrimidin-4(3H)-ones (12-17) by using B. subtilu s, K. pneumonia and A. niger.Desai Akshay et al16 reported the synthesis of 2-thiophene-2- ethylthioureido-4- morpholino-6-(aryl) ureido-s-triazines.(18-23) These analogs were evaluated for their antimicrobial activity using S. typhi, C. albicans.Bhuiyan Md. Mosharef Hossain et al17 reported synthesis of 4-hydrazino-2- mehylthio-5-ethyl-6- methylthieno 2,3-d pyrimidine (24) which is evaluated as antimicrobial agent by using B.cereus, V.cholerae, A.alternate.(24)Shiradkar M. et al18 reported synthesis of N-3-(substituted)-7H- 1,2,4 triazolo 3,4-b 1,3,4 thiadiazine / thiadiazol-4,5,6,7- tetrahydrobenzob thiophenes (25-32) as favorable antimicrobial agents by using E.coli, S.aureus, A.nigar.Ahmed M. M. et al19 reported synthesis of 4-(substituted)-7-cyano- 6-phenyl aminothieno 3,2-d pyrimidins (33-34) and evaluated as true(p) antimicrobial agents by using B.subtilis and St.aureus, compared with reference drug Amoxicillin.The 6-methyl-2-phenyl-3-(substituted)-3H-thieno3,2-d pyrimidin- 4-ones (35-38) has been reported by Chander Mohan et al20 and evaluated for antimicrobial activity by using B. subtilis, E.coli, P.aeruginosa compared with standard drug Ciprofloxacin.Bhuiyan Md. Mosharef Hossain et al21 reported synthesis of thieno3,2-e imidazo1,2-c pyrimidin-2(3H)ones (39) which was evaluated for antimicrobial activity against B. cereus, S.typhi and A.alternatacompare to reference drugs Ampicillin with Nystatin.(39)Shetty Nitin kumar et al22 reported synthesis of 8,9,10,11-tetrahydro1benzothieno3,2-e 1,2,4triazolo 1,5- cpyrimidine -8-ones (40-42) and evaluated for antibacterial activity against B. subtilis comparable to ampicilin.References Larsen PK, Liljefors T, Madsen U, editors. Text book of drug design and discovery. 3rd ed. London Taylor Francis 2002.Rang HP, Dale MM, Ritter JM Pharmacology, 4th edition Churchill Livingstone, Edinburgh, 1999 648Wilson Gisvold, Textbook of Organic Medicinal and Pharmaceutical Chemistry, 10th edition, Lippincott publication Philadelpia 196-203.A.A Boteva, O. P. Krasnykh, S.S.Dubrovina, M. I. Vakhrin, E.B. Babushkina, T.F. Odegova, I.V. 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