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We have developed a simple and facile synthesis for azapeptides on solid support without any side reaction. The azaGly is inserted by in situ reaction of disuccinimidyl carbonate with free amine followed by treatment of hydrazine hydrate at room temperature. The new series of peptidomimetics was prepared by azaGly scanning of heptapeptide Arg\u2010Pro\u2010Arg\u2010Nle\u2010Tyr\u2010Dap\u2010Nle (<jats:bold>Akt\u201001<\/jats:bold>), a GSK\u20103\u03b2\u2010derived Akt inhibitor. The azaGly\u2010appended peptides showed significant improvement in biological activity and serum stability, with retention of conformation as evidenced by NMR and CD studies. The results clearly demonstrate that azaGly\u2010appended peptides are new peptidomimetics. Their synthesis makes this approach highly useful for the development of novel peptidomimetics of therapeutic potential.<\/jats:p>","DOI":"10.1002\/cbic.201700031","type":"journal-article","created":{"date-parts":[[2017,4,5]],"date-time":"2017-04-05T16:03:04Z","timestamp":1491408184000},"page":"1061-1065","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":9,"title":["AzaGly\u2010Appended Peptidomimetics Structurally Related to PTR6154 as Potential PKB\/Akt Inhibitors"],"prefix":"10.1002","volume":"18","author":[{"given":"Shalini","family":"Singh","sequence":"first","affiliation":[{"name":"Medicinal and Process Chemistry Division CSIR\u2013Central Drug Research Institute  Lucknow Uttar Pradesh 226031 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Richa","family":"Shrivastava","sequence":"additional","affiliation":[{"name":"Toxicology Division CSIR\u2013Central Drug Research Institute  Lucknow Uttar Pradesh 226031 India"},{"name":"Academy of Scientific and Innovative Research  New Delhi 11000 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gajendra","family":"Singh","sequence":"additional","affiliation":[{"name":"NMR Centre SAIF CSIR\u2013Central Drug Research Institute  Lucknow Uttar Pradesh 226031 India"},{"name":"Academy of Scientific and Innovative Research  New Delhi 11000 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rafat","family":"Ali","sequence":"additional","affiliation":[{"name":"Medicinal and Process Chemistry Division CSIR\u2013Central Drug Research Institute  Lucknow Uttar Pradesh 226031 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ravi","family":"Sankar\u2005Ampapathi","sequence":"additional","affiliation":[{"name":"NMR Centre SAIF CSIR\u2013Central Drug Research Institute  Lucknow Uttar Pradesh 226031 India"},{"name":"Academy of Scientific and Innovative Research  New Delhi 11000 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Smrati","family":"Bhadhuria","sequence":"additional","affiliation":[{"name":"Toxicology Division CSIR\u2013Central Drug Research Institute  Lucknow Uttar Pradesh 226031 India"},{"name":"Academy of Scientific and Innovative Research  New Delhi 11000 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wahajul","family":"Haq","sequence":"additional","affiliation":[{"name":"Medicinal and Process Chemistry Division CSIR\u2013Central Drug Research Institute  Lucknow Uttar Pradesh 226031 India"},{"name":"Academy of Scientific and Innovative Research  New Delhi 11000 India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2017,5,11]]},"reference":[{"key":"e_1_2_2_1_1","doi-asserted-by":"publisher","DOI":"10.1021\/ar8000603"},{"key":"e_1_2_2_2_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm9013532"},{"key":"e_1_2_2_3_1","doi-asserted-by":"publisher","DOI":"10.1002\/cbdv.201100093"},{"key":"e_1_2_2_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/0196-9781(95)02005-H"},{"key":"e_1_2_2_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0957-4166(00)00250-0"},{"key":"e_1_2_2_6_1","doi-asserted-by":"publisher","DOI":"10.1055\/s-1989-27269"},{"key":"e_1_2_2_7_1","doi-asserted-by":"publisher","DOI":"10.1039\/P19760000244"},{"key":"e_1_2_2_8_1","unstructured":"\u00a0"},{"key":"e_1_2_2_9_2","doi-asserted-by":"publisher","DOI":"10.1016\/0960-894X(96)00308-3"},{"key":"e_1_2_2_10_2","doi-asserted-by":"publisher","DOI":"10.1016\/0968-0896(96)00153-8"},{"key":"e_1_2_2_11_1","doi-asserted-by":"publisher","DOI":"10.1021\/jacs.5b04590"},{"key":"e_1_2_2_12_1","doi-asserted-by":"publisher","DOI":"10.4155\/fmc.11.74"},{"key":"e_1_2_2_13_1","doi-asserted-by":"publisher","DOI":"10.1021\/ol901423c"},{"key":"e_1_2_2_14_1","doi-asserted-by":"publisher","DOI":"10.1021\/jo102422x"},{"key":"e_1_2_2_15_1","doi-asserted-by":"publisher","DOI":"10.1021\/ja00907a036"},{"key":"e_1_2_2_16_1","unstructured":"\u00a0"},{"key":"e_1_2_2_17_2","doi-asserted-by":"publisher","DOI":"10.1111\/j.1399-3011.1992.tb00311.x"},{"key":"e_1_2_2_18_2","doi-asserted-by":"publisher","DOI":"10.1039\/p19930002843"},{"key":"e_1_2_2_19_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm020209i"},{"key":"e_1_2_2_20_1","doi-asserted-by":"publisher","DOI":"10.1021\/jo9906173"},{"key":"e_1_2_2_21_1","unstructured":"\u00a0"},{"key":"e_1_2_2_22_2","doi-asserted-by":"publisher","DOI":"10.1021\/cc050043h"},{"key":"e_1_2_2_23_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0040-4039(00)00534-7"},{"key":"e_1_2_2_24_1","doi-asserted-by":"publisher","DOI":"10.1002\/bip.21103"},{"key":"e_1_2_2_25_1","unstructured":"K. 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